Octrooi (aanvraag): 2037617 I
COSMETIC COMPOSITION
CROSS-REFERENCE TO RELATED APPLICATION[0001] This application claims the benefit of priority to U.S. Provisional Patent
Application Serial Nos. 63/500,388 filed May 5, 2023 entitled “Cosmetic Composition”; 63/500,382 filed May 5, 2023 entitled “Fragrance Compositions”; 63/614,226 filed December 22, 2023 entitled “Cosmetic Composition”; and NL 2035921 filed May 5, 2023 entitled “Cosmetic Composition”, the disclosure of each of which is incorporated herein in its entirety by reference.
BACKGROUND OF THE INVENTION[0002] With conventional cosmetic products. a user typically must choose between a product that is easily removable and a product that remains on the skin for long periods of time (eg, an entire day). Although easily-removable products can be rapidly removed by, for example, washing with soap and water, a user may find themselves repeatedly reapplying the product throughout the day, as the product may also be inadvertently removed by sweat and contact with clothing or the like. On the other hand, typical long-lasting cosmetic products are less subject to inadvertent removal, but may be difficult to wash off and may require the use of organic solvents or other harsh cosmetic removers. Accordingly, there is a continuing need in the art for cosmetic compositions that remain on the skin for extended periods of time, while being easily-removable by washing with soap and water. Transfer-resistant cosmetics typically employ a film forming polymer to provide a long-wearing film of the skin, lips, hair or lashes and to aid in spreading and adhering the formulation to the surface. Such film forming polymers may include polymers such as organosiloxanes, including polydimethylsiloxane (PDMS or
Dimethicone), utilized due to their excellent spreading properties and biological inertness.
More recently, the properties of silicone polymers have been modified by copolymerization with other polymers, such as polyurethanes, ethylenically unsaturated monomers or polymers thereof, and the like. For example, in U.S. Patent Pub. 2008/0019932, the disclosure of which is hereby incorporated by reference, Revlon describes color cosmetic compositions comprising
Octrooi (aanvraag): 2037617 2 “at least one silicone film forming polymer, at least one pigment, and at least one dispersant that aids in dispersion of the pigment and silicone film forming polymer in the composition.”
[0003] Aesthetic conditions of the skin are frequently associated with natural or environmental causes, such as the process of aging (i.e. intrinsic aging), exposure to the sun, or the resulting ultraviolet radiation therefrom (i.e., extrinsic aging), and the like. Other factors, such as improper care and/or diet, stress, nutritional deficiencies, repeated facial movement and genetic predisposition also contribute to the development of adverse skin conditions, such as fine lines, frown lines, folds, furrows and wrinkles.
[0004] Skin aging and wrinkling is a multifactor process. The formation of lines and wrinkles can be attributed to both extrinsic and intrinsic causes. Extrinsic causes include exposure to ultraviolet radiation and unquenched reactive oxygen species, smoke and other pollutants. Intrinsic factors include degradation of the skin matrix, loss of volume (fat and bone) and muscle tone.
[0005] With each smile, squint, laugh, or frown, the contraction of facial muscles causes dynamic wrinkles to appear on the face. In chronologically-younger skin, these lines dissipate quickly and are not prominent. However, with age, the lines become deeper and appear more noticeable. Most commonly, they are manifested as deep furrows between the eyebrows (“frown lines”), at the sides of the eyes (“crow's feet”), and across the forehead (“glabellar lines”).
[6006] The biochemistry and biomechanics of skeletal muscle contraction are well- characterized. Contraction is initiated by an electric signal (action potential) transmitted by the motor neuron. At the neuromuscular junction, the action potential causes vesicles to release the neurotransmitter acetylcholine (“Ach”) which, in tarn, diffuses across the synapse between the nerve ending and the sarcolemma, the membrane of muscle fibers. ACh binds to ACh receptors, triggering the action potential to spread, and causing a release of calcium ions. The biochemistry and biomechanics of skeletal muscle contraction are well-characterized. Contraction is initiated by an electric signal (action potential) transmitted by the motor neuron. At the neuromuscular junction, the action potential causes vesicles to release the neurotransmitter acetylcholine (“Ach”) which, in turn, diffuses across the synapse between the nerve ending and the sarcolemma, the membrane of muscle fibers. ACh binds to ACh receptors, triggering the action potential to spread, and causing a release of calcium ions. Muscle groups
Octrooi (aanvraag): 2037617 3 differ in their sensitivity to muscle relaxants. Muscles in the periorbital and glabellar areas are particularly sensitive to ACh and thus susceptible to effective treatment by agents that block
Ach release. See, e.g., the review article published by L. Vimal and O. Oladapo, “Pharmacology of Non-Depolarising Muscle Relaxants” in Issue 5, Article 7 of Update in 5S Anaesthesia, the electronic educational journal of World Anaesthesia and the World Federation of Societies of Anaesthesiologists. http://www.nda.ox.ac.uk/wisa/html/u05/u05_012 htm accessed Jun. 20, 2007 New ingredients for use as effective, active agents in compositions and formulations for application, preferably topical application, to the skin are advantageous to the industry and the consumer for a variety of uses in the areas of skin care treatment and therapy, and personal use products. Nelupure (INCI: Propanediol (and) Glycerin (and) Nymphaea
Caerulea Flower Extract (and) Nelumbo Nucifera Flower Extract, used interchangeably as trade name Nelupure; INCI; “lotus flower extract”; and/or “lotus flower extract blend and/or constituents thereof” throughout) is a blended extract from two types of lotus flower, the
Egyptian Lotus (Nymphaea caerulea) and the Sacred Lotus (Nelumbo nucifera). It has been speculated that Nelupure (INCI: Propanediol (and) Glycerin (and) Nymphaea Caerulea Flower
Extract (and) Nelumbo Nucifera Flower Extract) acts via leptin-receptor inhibition to regulate the sebaceous glands, preventing the excess of sebum production and inflammatory processes that cause skin blemishes, and may also act to inhibit acetylcholine release.
[0007] Unwind Sacred Lotus, marketed by the Naolys company, is a material consisting of active plant cells from Nelumbo nucifera whose action has been described as " modulating the skin’s neuro-system, Sacred Lotus cells have a relaxing effect that helps to restore the skin’s original balance.” https://www.unifect.com/products/unwind-sacred-lotus/
SUMMARY OF THE DISCLOSURE[0008] Various aspects disclosed relate to a cosmetic composition comprising any of the components disclosed herein. The present disclosure provides compositions and methods comprising lotus newly found to be effective to treat, including prevent, reduce, ameliorate, and/or eliminate, signs and results of dermatological aging of skin, especially wrinkles and fine lines, and/or to improve the aesthetic appearance of skin. Further these constituents are provided for use in compositions and methods to treat, including prevent, ameliorate, and/or reduce, hyperhidrosis (or sweating or perspiration) and its associated effects. More specifically,
Octrooi (aanvraag): 2037617 4 the active constituents (also referred to as active agents, components, ingredients, reagents, or compounds herein) are extracts of the lotus flower and/or blends of extracts of various species of the lotus family such as but not limited to Nelupure (INCI: Propanediol (and) Glycerin (and)
Nymphaea Caerulea Flower Extract (and) Nelumbo Nucifera Flower Extract), obtained from plants and the like, of the Nelimbo family. These plant materials have been newly found to provide treatment for wrinkles, fine lines and other signs of dermatological aging (i.e., intrinsic aging) or sunlight exposure of the skin (i.e., extrinsic aging), as well for use for reducing sweating, possibly by virtue of their effect at the neuromuscular junction (NMJ) of muscle and nerve cells and tissue, and at the fibers of the sweat glands to inhibit acetylcholine release, e.g., at the NMI, thereby relaxing or decontracting muscles, e.g., facial expression muscles.
[0009] It has been found that the incorporation of an active ingredient capable of reducing integument sebum production and/or integument sweat production may yield a cosmetic composition capable of remaining on the skin for extended periods of time. The present disclosure provides a longwear composition that includes an active component, The active component can include a material that may inhibit integument sebum and/or sweat production. In one aspect, the active ingredient may downregulate integument sebum and/or sweat production via leptin receptor inhibition. In another aspect, the active ingredient downregulates integument sebum and/or sweat production via competitive inhibition of cell surface leptin receptor activity. In another aspect, the active ingredient may downregulate integument sebum and/or sweat production via nicotinic acetylcholine receptor (nAchR) downregulation. In another aspect, the active ingredient may downregulate integument sebum production via competitive inhibition of nAchR activity. In another aspect, the active ingredient may inhibit acetylcholine release.
[00910] In certain aspects, the skin in need of the disclosed composition(s), may be skin having excess sebum. In a further aspect of a method for treating skin with excess sebum, the skin benefit may selected from the group consisting of: restoration of a matte finish to the skin; an evening of skin type; reduction in oily/greasy feel to skin and/or hair; reduction in the incidence of dandruff; reduction in the incidence of blocked/clogged pores; reduction in the incidence of comedones; reduction in the incidence of acne lesions; reduction in the area over expressing or over-producing lipids; reduction in thickness of skin affected by over-production of lipids; and/or combinations thereof.
Octrooi (aanvraag): 2037617 5
[00011] It is another aspect of the present disclosure to provide compositions, formulations and methods containing materials newly determined to be useful in the treatment of wrinkles, fine lines, folds, furrows and other signs of aging skin, in addition to treating, preventing or reducing hyperhidrosis. These materials exert their effectiveness according to this disclosure by working at the neuromuscular junctions (NMI), such as in the muscle and nerve cell or tissue layer of a site of application, e.g., skin of the face, neck, arms, feet, or hands, or in the dermal layer of the skin where sweat glands are located. More specifically, the extracts from the flower of one or more species of the lotus flower constituents block or inhibit the release of acetylcholine at the NMJ of skeletal muscle, which, in turn, results in the relaxation or decontraction of contracted muscles. Contracted muscles are associated with the formation of fine lines, wrinkling and the like.
[00012] It is another aspect of the present disclosure to provide compositions, formulations and methods utilizing materials that are newly determined to be useful in the reduction of sweating from the skin.
[00013] The physiological act of sweating serves as the body's natural coolant, protecting it from overheating. When subjected {a temperature InCreases, stress, or exercise, the body excretes sweat, a fluid comprising mostly water along with minerals, lactate and urea, to cool the body by evaporation of the water, {00014} Sweating can have adverse effects on the use of cosmetics, for example by adversely impacting the ability of foundation to maintain integrity on the skin, While occlusive agents have been oulized to decrease the amount of perspiration, such occlusive agents can also hinder the skin's ability to breathe and to release oils, which can result in skin trriation and comedogenic effects.
[00015] IL is an object of the present wvention to provide a cosmetic composition that does nat require the presence of an aluminum salt and/or an oceclosive agent to deliver a sweat management benefit.
[00016] It is to be understood that, as used herein, the terms treating and treatment include and encompass preventing, reducing, ameliorating, improving, alleviating, and/or eliminating the dermatological effects of aging and sun exposure, with particular regard to wrinkles, fine lines, folds. furrows, creases of the skin, and the like. The present disclosure further encompasses the treatment, as defined above, of “marionette” lines that run on either
Octrooi (aanvraag): 2037617 6 side of the mouth, as well as lines on the forehead, and the perpendicular lines between the brows. The present compositions and methods are also suitable for use in treating, as defined above, dermatological conditions of the skin in numerous areas of the body, including, without limitation, the face, forehead, neck, arms, hands, legs, knees, feet, chest, back, groin, buttocks, and the like.
DETAILED DESCRIPTION OF THE INVENTION[00017] Reference will now be made in detail to certain aspects of the disclosed subject matter. While the disclosed subject matter will be described in conjunction with the enumerated claims, 1t will be understood that the exemplified subject matter is not intended to limit the claims to the disclosed subject matter.
[00018] Throughout this document, values expressed in a range format should be interpreted in a flexible manner to include not only the numerical values explicitly recited as the limits of the range, but also to include all the individual numerical values or sub-ranges encompassed within that range as if each numerical value and sub-range is explicitly recited.
For example, a range of “about 0.1% to about 5%” or “about 0.1% to 5%” should be interpreted to include not just about 0.1% to about 5%, but also the individual values (e.g., 1%, 2%, 3%, and 4%) and the sub-ranges (e.g., 0.1% to 0.5%, 1.1% to 2.2%, 3.3% to 4.4%) within the indicated range. The statement “about X to Y” has the same meaning as “about X to about Y,” unless indicated otherwise. Likewise, the statement “about X, Y, or about Z” has the same meaning as “about X, about Y, or about Z,” unless indicated otherwise.
[00019] In this document, the terms “a,” “an,” or “the” are used to include one or more than one unless the context clearly dictates otherwise. The term “or” is used to refer to a nonexclusive “or” unless otherwise indicated. The statement “at least one of A and B” has the same meaning as “A, B, or A and B.” In addition, it is to be understood that the phraseology or terminology employed herein, and not otherwise defined, is for the purpose of description only and not of limitation. Any use of section headings is intended to aid reading of the document and is not to be interpreted as limiting; information that is relevant to a section heading may occur within or outside of that particular section.
[00020] As used herein, the term “composition” includes a composition intended for application to a body surface, such as for example, skin or hair. . The term “composition” may
Octrooi (aanvraag): 2037617 7 also include cleaning compositions, such as fabric care composition or home care compositions, including air care compositions (e.g., air fresheners), for use on clothing or other substrates such as hard surfaces (e.g., dishes, floors, countertops). Additional non-limiting examples of “composition” may also include facial or body powder, deodorant, foundation, body/facial oil, mousse, creams (e.g., cold creams), waxes, sunscreens and blocks, bath and shower gels, lip balms, self-tanning compositions, masks and patches.
[00021] As used herein, the term “consumer” means both the user of the composition and the observer nearby or around the user. {22} As used herein, the term “integument” means the set of organs forming the outennoest layer of an animals body, It comprises the skin and iis appendages, which act as a physical barrier between the external environment and the wiornal environment that it serves io protect and maintain the body,
[00023] As used herein, the term “intimate area” means the area near or between the thighs, including the crotch area of a human where body exudates, such as urine, feces, vaginal discharge, menstrual Thad, and the like, may be present. The intimate area shall also include the breasts.
[00024] As used herein, the term “sebum control” means Products/compositions designed to regulate oil production and reduce shine on the skin
[00025] As used herein, the term “longwear” means Cosmetics/compositions designed to have extended wear time, providing long-lasting coverage or color intensity.
[66928] As used herein, the term “sweating” means the excretion of perspiration from the pores of the skin, Sweating includes, but not limited to, 1) non-pathological sweating, such as thermally-induced, exercise-induced, or stress-induced sweating; and 2) pathological or excessive sweating such as hyperhidrosis. The invention is useful in any area of the body where sweating occurs such as the hands, feet, face, head, torso, or underarms (axilla).
[00027] It is understood that the test methods that are disclosed in the Test Methods
Section of the present application may be used to determine the respective values of the parameters of Applicants’ disclosures as described and claimed herein.
[00028] In all aspects of the present disclosure, all percentages are by weight of the total composition, as evident by the context, unless specifically stated otherwise. All ratios are
Octrooi (aanvraag): 2037617 8 weight ratios, unless specifically stated otherwise, and all measurements are made at 25 °C, unless otherwise designated.
[00029] A pH of the composition can be in a range of from about 4 to about 8, about 5 to about 7, less than, equal to, or greater than about 4, 5, 6, 7, or about 8. The ethanol concentration in any of the compositions described herein can be less than about 78 wt% ethanol, less than about 70 wt% ethanol, less than about 60 wt% ethanol, less than about 50 wt% ethanol, less than about 40 wt% ethanol, less than about 30 wt% ethanol, less than about 20 wt% ethanol, less than about 10 wt% ethanol, or free of ethanol.
[00039] Human skin comprises two major compartments: a superficial outer compartment, the epidermis, and a deeper compartment, the dermis. The outermost epidermal skin layers typically provide a certain degree of protection to the body, although fine lines and wrinkles can be readily visualized in this portion of the skin. The epidermis and dermis bear the brunt of harmful effects of photodamage. The natural human epidermis functions to provide the essential protectant role of the skin in the human body. The dermis, which provides a solid and nutritional support to the epidermis, comprises mainly fibroblasts and an extracellular matrix composed primarily of a substance that includes collagen, elastin and glycosaminoglycans (“GAGs”). In addition, the dermis contains leukocytes, mast cells, tissue macrophages, blood vessels, muscle cells and nerve fibers. The dermal muscles of the face are controlled by motor nerve afferences of the facial nerve. The interlobular septa of the hypoderm contain within them fibers that constitute a striated muscle tissue, i.e., the panniculus carnosus.
It is known that a subpopulation of dermal fibroblasts, called myofibroblasts, has contractile characteristics similar to those of muscle cells and tissue.
[00031] Glabellar facial lines arise from the activity of the corrugator and orbicularis oculi muscles. These muscles move the brow medially, and the procerus and depressor supercilii pull the brow inferiorly. This creates a frown or “furrowed brow”. The location, size, and use of the muscles vary markedly among individuals. Lines induced by facial expression occur perpendicular to the direction of action of contracting facial muscles. An effective dose for facial lines is determined by gross observation of the patient’s ability to activate the superficial muscles injected.
[00032] Lateral canthal lines arise largely from the activity of the orbicularis oculi muscles around the eye responsible for blinking and eyelid closure. Forceful contraction of the
Octrooi (aanvraag): 2037617 9 orbicularis oculi results in lateral and radially oriented folds (crow’s feet lines) which originate from the lateral canthus. The distribution of these radial lines differs among patients. Forehead lines arise largely from the activity of the frontalis muscles. This muscle moves the brow superiorly, interacting with the procerus, orbicularis, corrugator, and depressor supercilli.
Frontalis contraction causes brow elevation. The location, size, and use of the muscles vary markedly among individuals.
[00033] Sebum production by skin may lead to aesthetic problems, such as oily/shiny skin or hair, acne-prone skin, enlarged pores, thickened skin, or poorer hold of makeup.
Additionally, the excess sebum may act as a catalyst for acne by clogging pores leading to the formation of comedones (“blackheads” or “whiteheads™), which, when left untreated, may become inflamed and progress into acne vulgaris. The compositions described herein can provide a skin benefit in that they can prevent these undesirable effects caused by excess sebum production.
[00034] In a further aspect, the skin benefit may be selected from the group consisting of: reducing lipid production by sebaceous glands; reducing lipid synthesis in subcutaneous adipose tissue; reducing triglyceride synthesis; reducing fatty acid synthesis; preventing and/or improving conditions related to skin associated with inhibited lipolysis; preventing and/or improving conditions related to skin associated with nonselective tor partially selective PPAR- gamma. stimulators/up regulators; preventing and/or improving conditions related to skin associated with nonselective or partially selective up regulation of adipogeneic genes typically up regulated by PPAR-.gamma. activation; preventing and/or improving conditions related to skin associated with nonselective or partially selective FAS stimulators/up regulators; preventing and/or improving conditions related to skin associated with nonselective or partially selective SCD-1 receptor stimulators/up regulators; preventing, ameliorating or treating oily skin; preventing, ameliorating or treating oily hair; preventing, ameliorating or treating oily scalp; preventing, ameliorating or treating enlarged pores; preventing, ameliorating, or treating acne-prone skin; preventing, ameliorating or treating body odors associated with excess sebum production; preventing, ameliorating or treating cellulite in adults; preventing, ameliorating or treating excess accumulation or production of subcutaneous fat in adults; improving skin texture associated with cellulite; and/or combinations thereof.
Octrooi (aanvraag): 2037617 10
[00035] In certain aspects, the skin in need of the disclosed composition(s), may be skin having excess sebum. In a further aspect of a method for treating skin with excess sebum, the skin benefit may selected from the group consisting of: restoration of a matte finish to the skin; an evening of skin type; reduction in oily/greasy feel to skin and/or hair; reduction in the incidence of dandruff; reduction in the incidence of blocked/clogged pores; reduction in the incidence of comedones; reduction in the incidence of acne lesions; reduction in the area over expressing or over-producing lipids; reduction in thickness of skin affected by over-production of lipids; and/or combinations thereof.
[00036] According to various aspects of the present disclosure a cosmetic composition can include an active component.
Sweat Reduction
[00037] Eccrine, apocrine and apoeccrine glands all contribute to sweat excretion (see hitps www nebinimonih.gov/pme/aticles/PMUSTTI238/). Through iontophoresis, acetylcholine binds to the muscarinic receptors on the sweat gland, causing an immediate sweat response. Acetylcholine, which is released by sympathetic nerves, acts as a potent stimulator for sweat secretion, and cholinergic substances are those known to be capable of producing, altering or releasing acetylcholine.
[00038] Sebaceous glands are a separate type of gland from sweat glands. Sebaceous glands are holocrine glands, secreting a viscous, lipid-rich fluid consisting of triglycerides, wax esters, squalene, cholesterol, and cholesterol esters. The evidence for cholinergic signalling in sebaceous glands remains under study.
[00039] (rttpsiffwww.sciencediiectoomyscience/article/abs/pi/S0Y23 18 LL 13002183).
[00940] The neurotransmitter acetylcholine is secreted by neurons in many areas of the brain, but specifically by the large pyramidal cells of the motor cortex, by several different neurons 1n the basal ganglia, by the motor neurons that innervate the skeletal muscles, by the preganglionic neurons of the autonomic nervous system (both sympathetic and parasympathetic), by the bag 1 fibers of the muscle spindle fiber, by the postganglionic neurons of the parasympathetic nervous system, and by some of the postganglionic neurons of the sympathetic nervous system. Essentially, only the postganglionic sympathetic nerve fibers to the sweat glands, the piloerector muscles and a few blood vessels are cholinergic as most of
Octrooi (aanvraag): 2037617 11 the postganglionic neurons of the sympathetic nervous system secret the neurotransmitter norepinephine. In most instances acetylcholine has an excitatory effect. However, acetylcholine is known to have inhibitory effects at some of the peripheral parasympathetic nerve endings, such as inhibition of heart rate by the vagal nerve.
[00041] The efferent signals of the autonomic nervous system are transmitted to the body through either the sympathetic nervous system or the parasympathetic nervous system.
The preganglionic neurons of the sympathetic nervous system extend from preganglionic sympathetic neuron cell bodies located in the intermediolateral horn of the spinal cord. The preganglionic sympathetic nerve fibers, extending from the cell body, synapse with postganglionic neurons located in either a paravertebral sympathetic ganglion or in a prevertebral ganglion. Since, the preganglionic neurons of both the sympathetic and parasympathetic nervous system are cholinergic, application of acetylcholine to the ganglia will excite both sympathetic and parasympathetic postganglionic neurons.
[00042] Acetylcholine activates two types of receptors, muscarinic and nicotinic receptors. The muscarinic receptors are found in all effector cells stimulated by the postganglionic neurons of the parasympathetic nervous system as well as in those stimulated by the postganglionic cholinergic neurons of the sympathetic nervous system. The nicotinic receptors are found in the adrenal medulla, as well as within the autonomic ganglia, that is on the cell surface of the postganglionic neuron at the synapse between the preganglionic and postganglionic neurons of both the sympathetic and parasympathetic systems. Nicotinic receptors are also found in many nonautonomic nerve endings, for example in the membranes of skeletal muscle fibers at the neuromuscular junction.
[00043] Acetylcholine is released from cholinergic neurons when small, clear, intracellular vesicles fuse with the presynaptic neuronal cell membrane. A wide variety of non- neuronal secretory cells, such as, adrenal medulla (as well as the PC12 cell line) and pancreatic islet cells release catecholamines and parathyroid hormone, respectively, from large dense-core vesicles. The PC12 cell line is a clone of rat pheochromocytoma cells extensively used as a tissue culture model for studies of sympathoadrenal development.
[00044] A neuromuscular junction is formed in skeletal muscle by the proximity of axons to muscle cells. A signal transmitted through the nervous system results in an action potential at the terminal axon, with activation of ion channels and resulting release of the
Octrooi (aanvraag): 2037617 12 neurotransmitter acetylcholine from intraneuronal synaptic vesicles, for example at the motor endplate of the neuromuscular junction The acetylcholine crosses the extracellular space to bind with acetylcholine receptor proteins on the surface of the muscle end plate. Once sufficient binding has occurred, an action potential of the muscle cell causes specific membrane ion channel changes, resulting in muscle cell contraction. The acetylcholine is then released from the muscle cells and metabolized by cholinesterases in the extracellular space. The metabolites are recycled back into the terminal axon for reprocessing into further acetylcholine.
[00045] It has been found that the incorporation of an active ingredient capable of reducing integument sebum production may yield a cosmetic composition capable of remaining on the skin for extended periods of time. The present disclosure provides a cosmetic composition that includes an active component. The active component can include a material that inhibits integument sebum production. In one aspect, it has been proposed that the active ingredient downregulates integument sebum production via leptin receptor downregulation. In another aspect, the active ingredient downregulates integument sebum production via competitive inhibition of cell surface leptin receptor activity. In another aspect, the active ingredient inhibits acetylcholine release.
[00046] In one aspect, the active component is a leptin receptor downregulator and/or acetylcholine release inhibitor. In one aspect, the leptin receptor downregulator and/or acetylcholine release inhibitor is an extract solution that can include nymphaea coerulea flower extract and nelumbo nucifera flower extract. In one aspect, the solution is available as a product under the tradename NELUPURE (INCI: PROPANEDIOL (AND) GLYCERIN (AND)
NYMPHAEA CAERULEA FLOWER EXTRACT (AND) NELUMBO NUCIFERA
FLOWER EXTRACT). Without intending to be bound to any theory, it is thought that the extract solution 1s useful in a cosmetic composition in part because it reduces the expression of the leptin cellular receptor in sebocytes, thus preventing the triggering of sebum production and inflammatory processes that cause skin blemishes; and/or inhibits acetylcholine release at the neuromuscular junction, thus decreasing the amount of sweat produced in response to acetylcholine release. . The benefits of including the extract solution are at least somewhat unexpected because it may be an inhibitor of acetylcholine release and may be utilized at a concentration; bioavailability; duration; and/or frequency to inhibit acetylcholine release in the dermis. According to some aspects, the ability of the extract solution to function as a
Octrooi (aanvraag): 2037617 13 component of a cosmetic composition is determined by an assay for determining the levels of sebum; leptin cell surface receptors in sebocytes; and/or, acetylcholine release inhibition in a sample that has been contacted with the extract or a composition including the extract.
[00047] The ability of the extract solution of nymphaea coerulea flower extract and nelumbo nucifera flower extract to provide beneficial properties as an acetylcholine release inhibitor suggests that other natural extracts with acetylcholine release inhibition properties can also be used for the modalities described herein.
[00048] According to some aspects, the ability of the extract solution to function as a sebum and/or sweat reducing component of a cosmetic composition is determined by an assay for determining the levels of acetylcholine (e.g., an ELISA assay in a sample that has been contacted with the extract or a composition including the extract.
[00049] The present disclosure provides novel compositions and methods comprising components newly found to be effective to treat, including prevent, ameliorate, inhibit and/or reduce, hyperhidrosis (sweating or perspiration) and its associated effects, such as decreased cosmetic remanence.
[00050] More specifically, the components (also referred to as active agents, constituents, ingredients, reagents, substances, or compounds herein) of this disclosure are extracts from the flower of one or more species of the lotus flowers, obtained from plants and the like, preferably of the Nelumbo family. These plant materials have been newly determined to be effective constituents in compositions and methods for treating, preventing, reducing, inhibiting, improving and/or eliminating wrinkles, fine lines, creases, folds, furrows, and other signs of dermatological aging due to chronological and/or hormonal aging, or due to sunlight exposure of the skin, as well for use in the treatment of hyperhidrosis.
[00051] According to the present disclosure, yet without wishing to be bound by theory, the extracts from the flower of one or more species of the lotus flower constituents exert their effects by their ability to inhibit, block, reduce, or prevent the release of acetylcholine at the neuromuscular junction (NMJ) of skeletal muscle cells and tissue, thereby relaxing muscles, for example, muscles associated with facial movement or expressions. Both nerve and muscle cells (skeletal muscle cells) are electrically excitable and the junctions between these types of cells are known as NMJ. The stimulation of a motor nerve innervating a skeletal muscle also may cause the release of acetylcholine and that acetylcholine, in turn, stimulates the skeletal
Octrooi (aanvraag): 2037617 14 muscle to contract. Thus, acetylcholine has been identified as the neurotransmitter at the neuromuscular junction. (see, e.g., B. Alberts et al, 1989, Molecular Biology of the
Cell, 2" Ed., Chapter 19, The Nervous System, Garland Publishing, Inc., NY, pp. 1075 et seq.). Provided by the present disclosure from the flower of one or more species of the lotus flower constituents which are newly described herein to inhibit, reduce, block, or prevent the release of acetylcholine at the NMJ of the skeletal muscle and thus relax the muscles, preferably those associated with facial expression or movement, particularly when employed in the compositions and methods of the invention. By inhibiting acetylcholine release, compositions and methods comprising the extracts from the flower of one or more species of the lotus flower extract as described herein can reduce, treat, and/or prevent excessive sweating or perspiration.
[00052] The ability of the extracts from the flower of one or more species of the lotus flower constituents to inhibit acetylcholine release by muscle cells results in a modulation of motor contraction so as to relax the muscle fibers in cutaneous or subcutaneous muscle and/or nerve tissue, thereby attenuating wrinkles, as well as fine lines, folds, furrows, and the like. By relaxing or preventing the contraction or hypercontraction of the cutaneous or subcutaneous muscle cells of areas such as the face, or hands, feet, etc., the extracts from the flower of one or more species of the lotus flowers and compositions containing extracts from the flower of one or more species of the lotus flowers can effectively smooth out the landscape of the skin in those areas where muscle contraction is involved in the formation of wrinkles and the like.
Thus, if muscle cell contractility is associated with the formation of wrinkles, fine lines, etc, the relaxation or decontraction of the contractility of cutaneous or subcutaneous muscle tissue by the extracts from the flower of one or more species of the lotus flower actives in the compositions of this disclosure can serve to loosen or slacken the contracting muscle tissue and alleviate, reduce, ameliorate, inhibit, or eradicate the wrinkles, fine lines, etc. Contraction of cutaneous or subcutaneous muscle cells or tissue of skin can elicit wrinkling, fine lines, and the like, which constitute at least some of the visible dermatological effects of aging due to chronological and/or hormonal aging, and/or due to photoexposure, as described herein. {00053} Thus, in one of its aspects, the present disclosure encompasses compositions, formulations and methods containing components, preferably, extracts from the flower of one or more species of the lotus flower constituents, newly determined to be useful in the treatment of wrinkles, fine lines, folds, furrows and other signs of aging and/or photoexposure of skin, in
Octrooi (aanvraag): 2037617 15 addition to treating, preventing or reducing hyperhidrosis. Skin in a variety of areas of the body is amenable for treatment and/or receipt of the compositions of the present disclosure the face, forehead, neck, arms, legs, hands, feet, torso (chest), back, and the like.
[00054] In general, for the purposes of the present disclosure, a substance, such as extracts from the flower of one or more species of the lotus flower constituent of the described compositions, is recognized as being a muscle relaxant when it elicits a relaxation effect on contracted muscle cells or on tissue, such as cutaneous or subcutaneous muscle tissue, and/or exhibits an inhibitory effect on acetylcholine release at the NMJ. Contracted muscle cells or tissue is associated with formation of wrinkles, fine lines, etc. Relaxation or decontraction of contracted muscle, such as by the action of extracts from the flower of one or more species of the lotus flowers to inhibit or block acetylcholine release at the NMJ, serves to smooth out the landscape, or microrelief, of the skin, thereby effecting the prevention, amelioration, reduction, and/or eradication of wrinkling and fine line, etc. formation caused by contracted muscle tissue in skin.
[00055] For use in the compositions of this disclosure, the extracts from the flower of one or more species of the lotus flower extracts can be chemically synthesized. Alternatively, these plant alkaloids may be extracted from plants. When extracted, they may be in a pure form, a semi-purified form, or may be a component of an unpurified plant extract.
[00056] The extracts from the flower of one or more species of the lotus flower plant materials contained in the compositions of the present disclosure can be chemically synthesized at industrial scale in large amounts. Alternatively, the materials may be extracted from natural raw materials from plants. Any and all methods of preparation may be used, including the use of cultured plant seed cells, as disclosed in U.S. Ser. No. 10/040,242, which is hereby incorporated by reference herein. For example, unpurified plant extracts may be employed in the present disclosure on the solubility of the particular plant extract in water or in organic solvent, the extraction process may differ. Two methods for extracting the materials from raw plant materials include organic solvent extraction, and aqueous-organic solvent extraction, as described in U.S. Pat. No. 6,372,239 to Wu et al. The organic extraction method involves a step of continuous washing and extracting the plant material against a stream of organic solvent. Examples of organic solvents include, but are not limited to methanol, ethanol, dichloromethane, chloroform, xylene, and petroleum ether. Alternatively, the alkaloid can be
Octrooi (aanvraag): 2037617 16 partially purified or completely purified. Chemical synthesis of the alkaloid obviates the need for extraction and purification.
[00057] In accordance with this disclosure, the extracts from the flower of one or more species of the lotus flower constituents comprise compositions which include, without limitation, topically applied formulations, anti-oxidants, anti-inflammatories, sunscreens, cosmetics, including make-ups, anti-aging formulations, e.g., creams for fine lines and/or wrinkles, topicals, skin penetration enhancers, antiperspirants, deodorants, and the like. Also in accordance with this disclosure from the flower of one or more species of the lotus flower constituents and additional ingredients comprising such compositions can be formulated in a variety of product forms. Preferably, the compositions are prepared in targeted delivery systems, e.g., transdermal, such as patches, and the like, particularly for topical administration.
[00058] The present disclosure encompasses compositions comprising one or more extracts from the flower of one or more species of the lotus flower constituents, preferably in a pharmaceutically-acceptable cosmetic or dermatological formulation which is suitable for contact with living animal tissue, including human tissue, and for topical administration, with virtually no adverse physiological effect, e.g., irritation, to the user. Thus, the inventive compositions are especially suitable for sensitive skin.
[00059] Compositions embraced by this disclosure can be provided in any cosmetically and/or dermatologically suitable form, preferably as a lotion, gel, cream, or incorporated into a transdermal patch, and also in an ointment or oil base, as well as in a sprayable liquid form.
Other suitable cosmetic product forms for the compositions of this disclosure for example, an emulsion, a mousse, a lip balm, a lip gloss, a lotion, a mask, an ointment, a pomade, a solution, a serum, a spray, or a towelette. In addition, the compositions contemplated by this invention can include more compatible cosmetically acceptable adjuvants commonly used and known by the skilled practitioner, such as colorants, fragrances, emollients, humectants, preservatives, vitamins, chelators, thickeners, and the like, as well as other botanicals such as aloe, chamomile, and the like, and as further described below. The compositions are preferably applied topically once or twice daily. The daily application can be for periods of up to two weeks, four weeks, or more. In one embodiment, a composition is utilized that combines lotus flower extracts with one or more additional sweating modulation and / or sweat absorbing materials.
Octrooi (aanvraag): 2037617 17
[000680] In one aspect encompassing sunscreen formulations, the compositions comprising extracts from the flower of one or more species of the lotus flower constituents can further include, without limitation, ingredients such as avobenzone, cinnamic acid derivatives (e.g., octylmethoxycinnamate), octyl salicylate, oxybenzone, titanium oxide, zinc oxide and mixtures or combinations thereof. Such formulations can also preferably include an alpha hydroxy acid, an oxa acid, an oxa diacid, and mixtures or combinations thereof.
[00061] The compositions of this disclosure can also be formulated into liposomes which can comprise other additives or substances, and/or which can be modified to more specifically reach or remain at a site following administration. Alternatively, the extracts from tbe flower of one or more species of the lotus flower-containing compositions can be injected subcutaneously (s.c.) or intradermally (i.d.) (for example, via microneedling optionally associated with a transdermal patch) at a site in need of wrinkle, fine line, etc. reduction, improvement, prevention, and/or elimination, resulting from inhibition of acetylcholine release at the NMJ and concomitant relaxation of contracted muscle.
[00062] Pharmaceutical or physiologically acceptable compositions suitable for use in the present disclosure include compositions in which the active constituents, ingredients, or materials are contained in an amount effective to achieve the intended purpose. By way of example, in the present compositions, extracts from the flower of one or more species of the lotus flower constituent is present in an amount of from about 0.0001 wt % to about 10 wt %, based on the total weight of the composition. More preferably, the present compositions include one or more extracts from the flower of one or more species of the lotus flower constituents in an amount from about 0.0005 wt % to about 5 wt %. Most preferably, the present compositions include one or more extracts from the flower of one or more species of the lotus flower constituents in an amount from about 0.001 wt % to about 2 wt % of the total composition. 100063] The determination of an effective dose or amount is well within the capability of those skilled in the art. A therapeutically effective dose refers to that amount of active ingredient, for example, extracts from the flower of one or more species of the lotus flower constituent identified 1n accordance with the present disclosure, which, for instance, treats, prevents, ameliorates, reduces, or eliminates the condition, more specifically, wrinkles, fine lines, creases, and the like. The practitioner, who will consider the factors related to the
Individual requiring treatment, will determine the exact dosage. Dosage and administration are
Octrooi (aanvraag): 2037617 18 adjusted to provide sufficient levels of the active constituent or to maintain the desired effect.
Factors which are typically considered include the severity of the individual's particular need, general health of the patient, age, weight, and gender of the individual, diet, time and frequency of administration, drug combination(s), reaction sensitivities, and tolerance/response to treatment, As a general guide, long-acting pharmaceutical compositions can be administered once daily, every 2 to 4 days, every week, or once every two weeks, depending on half-life and clearance rate of the particular formulation. Variations in these dosage levels can be adjusted using standard empirical routines for optimization, as is well understood in the art. Guidance as to particular dosages and methods of delivery is provided in the literature and is generally available to practitioners in the art. Those skilled in the art will employ different formulations depending upon the nature, e.g., structure, composition, of the active extracts from the flower of one or more species of the lotus flower constituent.
[00064] The compositions of the present disclosure yield improvements to the aesthetic appearance of the skin by treating at least one of the following: signs of dermatological aging, especially chronological, actinic or hormonal aging, or signs of extrinsic aging, such as sun exposure. In particular, improvements to the aesthetic appearance of skin include at least one of the following: makes facial lines appear less noticeable, makes facial lines and/or wrinkles feel plumped, improves appearance of suborbital lines and/or periorbital lines, improves appearance of crow's feet, reduces and/or diminishes the appearance of wrinkles, particularly facial wrinkles on the cheeks, forehead (e.g., perpendicular wrinkles between eyes, horizontal wrinkles above the eyes), and/or around the mouth, (e.g., marionette lines), and particularly deep wrinkles, folds, or creases, improves skin suppleness, reduces and/or eliminates fine and/or deep lines, folds and creases, and smoothes skin, e.g., to the extent that it reduces wrinkling/lines.
[00065] Embraced by the present disclosure are transdermal modes of delivery, such as patches and the like, with or without a suitable skin penetration enhancer. The methods and compositions embodied by the disclosure include a means by which the one or more extracts from the flower of one or more species of the lotus flower constituents can be effectively administered in a transdermal system. Frequently, compounds having poor topical absorption, or which are required at high dosage levels, are delivered transdermally. Accordingly, a transdermal means of delivering a composition or formulation (often with a skin penetration
Octrooi (aanvraag): 2037617 19 enhancer composition) to the skin is that of the transdermal patch or a similar device as known and described in the art. Examples of such devices are disclosed in U.S. Pat. Nos. 5,146,846, 5,223,262, 4,820,724, 4,379,454 and 4,956,171; such descriptions are not meant to be limiting.
The transdermal mode of storing and delivering the compositions onto the skin and forming the active composition is convenient and well suited for the purposes of an aspect of the present disclosure a topical patch is used, the patch is applied to the desired area for extended period of time. Preferably. the extended period of time is greater than one hour; more preferably, the extended period of time is overnight, e.g., when the user is sleeping.
[00066] A particular aspect of the present disclosure is directed to the delivery of the described compositions by the use of targeted delivery systems, for example, liposomes, microspheres (see, e.g., U.S. Pat. No. 5,770,222 to Unger et al.), transdermal patches, and the like, so that the extracts from the flower of one or more species of the lotus flower actives can more readily reach and affect the muscle layer of the area of application, e.g., face or neck, or the dermis layer of the skin, where sweat glands are located, e.g., underarm, foot, hand, etc.
Compositions comprising extracts from the flower of one or more species of the lotus flower constituents, including liposome formulations, can also be administered by direct injection subcutaneously or intradermally to more precisely deposit the active agents at sites which require muscle relaxation or decontraction via acetylcholine release inhibition.
[00067] Liposomes and delivery systems and vehicles involving liposomes are well- known in the art. In brief, liposomes are unilamellar or multilamellar lipid vesicles which entrap a significant fraction of aqueous solution. The vesicular microreservoirs of liposomes can contain a variety of water-soluble materials, which are suspended within the emulsion (e.g, reviewed in G. Gregorius (Ed.), 1991, Liposome Technology, Vols. 1, 11, HI, CRC Press, Boca
Raton, Fla.; Davis S. S. and Walker I. M., 1987, Methods in Enzymology, 149:51-64; Mayhew
E. et al, 1987, Methods in Enzymology, 149:64-77; and Shafer-Korting M. et al., 1989, J. Am.
Acad. Dermatol., 21:1271-1275). The preparation of liposomes and the variety of uses of liposomes in biological systems have been described (e.g., in U.S. Pat. No. 4,708,861 to M. C.
Popescu et al., U.S. Pat. No. 4,224,179 to M. Schneider and U.S. Pat. No. 4,235,871 to D. P.
Papahadjopoulos et al.). Accordingly, such liposomes can be formulated into any of the dermatological or cosmetic compositions as described herein.
Octrooi (aanvraag): 2037617 20
[00068] In addition to the extracts from the flower of one or more species of the lotus flower constituents as active agents, as described herein, the physiologically acceptable and pharmaceutical compositions can contain suitable pharmaceutically acceptable carriers, diluents, or excipients comprising auxiliaries which facilitate processing of the active compounds into preparations which can be used pharmaceutically. Further details on techniques for formulation and administration are provided in the latest edition of Remington's
Pharmaceutical Sciences (Mack Publishing Co.; Easton, Pa.). Pharmaceutical compositions containing the extracts from the flower of one or more species of the lotus flower ingredients of the present disclosure can be manufactured in a manner that is known in the art, e.g., by means of conventional mixing, dissolving, granulating, dragee-making, levigating, emulsifying, encapsulating, entrapping, or lyophilizing processes.
[00069] If applicable, the pharmaceutical composition can be provided as a salt and can be formed with many acids, including but not limited to, hydrochloric, sulfuric, acetic, lactic, tartaric, malic, succinic, and the like. Salts tend to be more soluble in aqueous solvents, or other protonic solvents, than are the corresponding tree base forms. In other cases, the preparation can be a lyophilized powder.
[00070] A preferred aspect of the topical compositions of the present disclosure also includes at least one of the following: a surface smoother, a skin plumper, an optical diffuser, a sunscreen, an exfoliation promoter, or an antioxidant. 100071] A surface smoother provides the functional benefits of enhancing skin smoothness and reducing the appearance of fine lines and coarse wrinkles. Examples include, without limitation, isopropyl myristate, petrolatum, isopropyl lanolate, silicones (e.g, methicone, dimethicone), or any mixtures thereof. The surface smoother is preferably present from about 0.1 wt % to about 50 wt % of the total weight of the composition. 100972] A skin plumper serves as a collagen enhancer to the skin. An example of a suitable and preferred skin plumper is palmitoyl oligopeptide. Other nonlimiting examples of skin plumpers include collagen and/or glycosaminoglycan (GAG) enhancing agents. The skin plumper is preferably present from about 0.1 wt % to about 20 wt % of the total weight of the composition.
[00073] An optical diffuser is a particle that changes the surface optometrics of skin, resulting in a visual blurring and softening of, for example, lines and wrinkles. Examples of
Octrooi (aanvraag): 2037617 21 optical diffusers that can be used in the present disclosure include, but are not limited to, boron nitride, mica, nylon, polymethylmethacrylate (PMMA), polyurethane powder, sericite, silica, silicone powder, talc, Teflon, titanium dioxide, zinc oxide, or any mixtures thereof. The optical diffuser is preferably present from about 0.01 wt % to about 20 wt % of the total weight of the composition.
[00974] In another aspect, the present disclosure embraces a sunscreen that protects skin from damaging ultraviolet rays. Hlustratively, the sunscreen provides both UVA and UVB protection by using either a single sunscreen or a combination of sunscreens. Among the sunscreens that can be employed in the present compositions are avobenzone, cinnamic acid derivatives (such as octylmethoxy cinnamate), octyl salicylate, oxybenzone, titanium dioxide, zinc oxide, or any mixture or combination thereof. Preferably, the sunscreen is present from about 1 wt % to about 30 wt % of the total weight of the composition. In particular, the addition of a sunscreen is preferred to prevent/reduce the photodegradation of the composition and/or ingredients therein while in the package and/or on the skin after application,
[00075] It will be appreciated that the compositions of the present disclosure containing sunscreen bring about additional improvements to the aesthetic appearance of skin, including at least one of the following: minimizes sunburning, minimizes tanning, reduces redness, and reduces future wrinkle development. It will be appreciated that when the topical composition 1s intended to be applied prior to retiring for the evening, the addition of a sunscreen agent may not be preferred.
[00076] The present compositions may also have one or more exfoliation promoters.
Suitable examples of an exfoliation promoter that can be used in the present compositions include keratolytic agents, i.e., an active agent having desquamating, exfoliant, or scrubbing properties, or an active agent which can soften the horny layer of the skin; alpha (a) and/or beta (B) hydroxy acids; benzoyl peroxide; keto acids, such as pyruvic acid, 2-oxopropanoic acid, 2- oxobutanoic acid, and 2-oxopentanoic acid; oxa acids, as disclosed in U.S. Pat. Nos. 5,847,003 and 5,834,513, the disclosures of which are incorporated herein by reference; urea; retinoids, or any mixtures thereof. These anti-wrinkle or anti-fine line active agents can be formulated, for example, in amounts of from about 0.0001% to 5% by weight relative to the total weight of the composition.
Octrooi (aanvraag): 2037617 22
[00077] More specifically, examples of hydroxy acids include, but are not limited to, o- hydroxy acids or B-hydroxy acids, either linear, branched, cyclic, saturated or unsaturated. The hydrogen atoms in the carbon-based backbone of these materials can be substituted with halogens, halogen-containing alkyl, acyl, acyloxy, alkoxycarbonyl, or alkoxy radicals having from 2 to 18 carbon atoms. Suitable hydroxy acids include, for example, glycolic acid, lactic acid, malic acid, tartaric acid, citric acid, 2-hydroxyalkanoic acid, mandelic acid, salicylic acid and alkyl derivatives thereof, including 5-n-octanoylsalicylic acid, 5-n-dodecanoylsalicylic acid, 5-n-decanoylsalicylic acid, S-n-octylsalicylic acid, 5-n-heptyloxysalicylic acid, 4-n- heptyloxysalicylic acid and 2-hydroxy-3-methylbenzoic acid or alkoxy derivatives thereof, such as 2-hydroxy-3-methyoxybenzoic acid. Exemplary retinoids include, without limitation, retinoic acid (e.g., all-trans or 13-cis) and derivatives thereof, retinol (Vitamin A) and esters thereof, such as retinol palmitate, retinol acetate and retinol propionate, and salts thereof.
Preferred exfoliation promoters are 3,6,9-trioxaundecanedioic acid, glycolic acid, lactic acid, or any mixtures thereof. Other acids, such as oxa acid (e.g., U.S. Pat, No. 6,069,169) and an oxadiacid (e.g., U.S. Pat. No. 5,932,229) can be included in the compositions of this disclosure.
[00078] When the present disclosure includes an exfoliation promoter, the composition typically includes about 0.5 wt % to 30 wt Ze, preferably about 1 wt Ze to about 15 wt %, more preferably about 2 wt % to about 10 wt %, and most preferably about 4 wt %, of the exfoliation promoter based on the total weight of the composition.
[00079] An antioxidant functions, among other things, to scavenge free radicals from skin to protect the skin from environmental agressors. Examples of antioxidants that can be used in the present compositions include compounds having phenolic hydroxy functions, such as ascorbic acid and its derivatives/esters; beta-carotene; catechins; curcumin; ferulic acid derivatives (e.g., ethyl ferulate or sodium ferulate); gallic acid derivatives (e.g., propyl gallate); lycopene; reductic acid; rosmarinic acid; tannic acid; tetrahydrocurcumin; tocopherol and its derivatives; uric acid; or any mixtures thereof. Other suitable antioxidants are those having one or more thiol (—SH) functions, in either reduced or non-reduced form, such as glutathione, lipoic acid, thioglycolic acid, and other sulfhydryl compounds. The antioxidant may be inorganic, such as bisulfites, metabisulfites, sulfites, or other inorganic salts and acids containing sulfur. Compositions of the present disclosure can include an antioxidant preferably
Octrooi (aanvraag): 2037617 23 from about 0.001 wt % to about 10 wt %, and more preferably from about 0.001 wt % to about wt %, of the total weight of the composition.
[00080] The compositions of this disclosure can also include one or more of the following ingredients, additives, or adjuvants: anesthetics, anti-allergenics, anti-fungals, 5 antiseptics, chelating agents, colorants, dyestuffs, demulcents, emollients, emulsifiers, fragrances, fillers, humectants, lubricants, moisturizers, pH adjusters, pigment altering agents, preservatives, skin penetration enhancers, stabilizers, surfactants, thickeners, viscosity modifiers, hydrophilic or lipophilic gelling agents, vitamins, or any mixtures thereof. The amounts of these various ingredients, additives, adjuvants, or active agents are those that are conventionally used in the cosmetic or pharmaceutical fields, for example, they can constitute from about 0.01% to 20% of the total weight of the composition. In addition, the adjuvants, ingredients, additives, or active agents can be introduced into the fatty phase, into the liquid phase, and/or into lipid vesicles, depending on their nature.
[00081] The component(s) of the present disclosure are preferably contained in a cosmetically acceptable medium (i.e, vehicle, diluent or carrier). In an aspect embracing topical application, the compositions of this disclosure a medium that is compatible with human skin. The compositions can be formulated as aqueous, alcohol, or aqueous/alcohol-based solutions, ointments, lotions, gels, water-in-oil, oil-in-water, or water-oil-water triple emulsions having the appearance of a cream or gel, microemulsions, or aerosols. In addition, the compositions can be in the form of vesicular dispersions containing ionic and/or nonionic lipids, as described above. Dosage units suitable for such pharmaceutical compositions are formulated according to the conventional knowledge and techniques used 1n the art.
[00082] More particularly, the compositions for topical application can be in the form of a protective care composition for the skin, preferably for the face, the neck, the hands, the feet, or other areas of the body. Nonlimiting examples include day creams or lotions, night creams or lotions, sunscreen creams, lotions, or oils, body milks, makeup (a foundation), artificial tanning compositions and depilatories.
[00083] If the composition of the disclosure is an emulsion, the proportion of fatty substances comprised therein can range from about 5% to 80%, by weight, preferably from about 5% to 50% by weight, relative to the total weight of the composition. The fatty substances and emulsifiers used in the composition in emulsion form are one or more of those
Octrooi (aanvraag): 2037617 24 conventionally employed in the cosmetic or pharmaceutical field. Nonlimiting examples of fatty substances include mineral oils (e.g., petroleum jelly), plant oils and hydrogenated derivatives thereof, animal oils, synthetic oils (e.g.. perhydrosqualene), silicone oils (e.g., polydimethylsiloxane) and fluoro oils. Other exemplary fatty substances include fatty alcohols (eg. stearyl or cetyl alcohol), fatty acids (e.g., stearic acid) and waxes.
[00084] Emulsifiers are typically present in the compositions of the disclosure in an amount of about 0.3% to 30%, by weight and preferably from about 0.5% to 30% by weight relative to the total weight of the composition.
[00085] In one aspect, the present disclosure relates to the administration of an effective amount of at least one extracts from the flower of one or more species of the lotus flower constituent or composition comprised thereof to inhibit or block acetylcholine release by nerve cells at the NMJ to relax and/or decontract subcutaneous muscles, particularly facial expression muscles, thereby smoothing out or unwrinkling skin, wherein the inhibition of acetylcholine release by nerve cells at the NMJ corresponds to muscle, preferably facial expression muscle relaxation or decontraction.
[00086] In yet another aspect, the present disclosure encompasses a method of treating hyperhidrosis or perspiration, comprising applying to skin a composition containing extracts from the flower of one or more species of the lotus flower in a cosmetically and/or dermatologically acceptable medium, and in an amount effective to treat, reduce, prevent and/or ameliorate hyperhidrosis or perspiration. The application of the extracts from the flower of one or more species of the lotus flower containing composition is preferably topical.
[00087] Another aspect of the present disclosure relates to a method of improving the aesthetic appearance of skin and comprises applying to the skin, or introducing via a directed mode of delivery, a composition including one or more extracts from the flower of one or more species of the lotus flower constituents in an amount effective to improve the aesthetic appearance of the skin. According to this aspect in aesthetic appearance involves the treatment of at least one condition, such as signs of dermatological aging. Dermatological aging can include chronological aging, actinic aging, hormonal aging, or any combination thereof.
[00088] As will be appreciated by the practitioner, cosmetic treatments comprising compositions containing the extracts from the flower of one or more species of the lotus flower constituents of the disclosure can be carried out, for example, by topically applying the
Octrooi (aanvraag): 2037617 25 cosmetic composition as described herein according to the routine technique for administering such compositions. Routine and commonly practiced techniques encompass the application of creams, lotions, gels, sera, ointments, antiperspirants, or deodorants to the skin; spraying as a form of application is also envisioned.
[006089] In addition to the active ingredient, the disclosed cosmetic compositions can include sebeorgulator ingredients that can work in conjunction with the solution of the lotus flower extract blend and/or constituents thereof. Examples of seboregulating ingredients include a mixture of Glycerin and Aqua and Palmitoyl Pentapeptide-4 (tradename BB-BIONT) and is known to help reduce biofilm formation of c acnes and can help to reduce acne scars.
Additional seberegulators include zinc, zinc pea, zinc gluconate, zinc oxide, Lens esculenta (Lentil) Seed Extract, syringa vulgaris extract, a mixture of Glycerin and Water and Backhousia
Citriodora Leaf Extract, a mixture of Octyldodecanol and Leptospermum Scoparium
Branch/Leaf Oil and Piper Nigrum (Pepper) Seed Extract and Magnolia Officinalis Bark
Extract, salicylic acid, salix alba extract, Quillaja Saponaria Bark Extract, Cupressus
Sempervirens Fruit Extract, Mimosa Tenuiflora Bark Extract, a mixture of Butylene Glycol and 10-Hydroxydecanoic Acid and Sebacic Acid, niacinamide, a mixture of Aqua and
Niacinamide and Faex and Aesculus Hippocastanum (Horse Chestnut) Seed Extract and
Ammonium Glycyrrhizate and Panthenol and Propylene Glycol and Zinc Gluconate and
Caffeine and Biotin, a mixture of eucalyptus globulus and pimpinella anisum seed extract, rosa centifolia flower extract, paeonia lactiflora root extract, bombax malabaricum flower extract, a mixture of Pistacia Lentiscus Gum / Pistacia Lentiscus (Mastic) Gum and Lecithin and
Glycerin and Alcohol and Aqua / Water, laminaria, a mixture of Isopentyldiol and Trifolium
Pratense (Clover) Flower Extract, cucurbita pepo, a mixture of Cinnamomum cassia bark extract and Zingiber officinale (ginger) root extract and Sanguisorba officinalis root extract,
Salvia Officinalis (Sage) Extract, retinol, a retinoid, a retinyl derivate, a mixture of Plantago
Lanceolata Leaf and Berberis Aquifolium, hypericum perforatum, a mixture of Serenoa
Serrulata Fruit Extract and Sesamum Indicum (Sesame) Seed Oil and Argania Spinosa Kernel
Oil and Beta-Sitosterol and Tocopherol, spiraea ulmaria extract, a mixture of Crambe
Abyssinica Seed Oil and vitis vinifera and iris fiorentina extract, a mixture of Propylene Glycol and Humulus Lupulus (Hops) Extract, a mixture of Hamamelis Virginiana (Witch Hazel) and
Water, a mixture of qua and Pyridoxine HC! and Niacinamide and Glycerin and Panthenol and
Octrooi (aanvraag): 2037617 26
Hydrolyzed Yeast Protein and Threonine and Allantoin and Biotin, green tea which is a mixture of Camellia Sinensts Leaf Extract and Hedera Helix (Ivy) LeafiStem Extract and hydrolyzed soy protein and Esteromorpha Compressa Extract and Boty] Avocadats and Tocopherol and
Potassium Azeloyl Diglycinate, a mixture of Moringa Pterygosperma Seed Extract and
Sarcosine and Cinnamomum Zeylanicum Bark Extract and houttuynia cordata and crithmum maritimum extract and cananga odorata flower extract and linum usitatissinum and verbena officinalis, lactobacillus ferment, a mixture of Magnesium Aluminum Silicate and
Hydroxyethylcellulose and Nigella Sativa Seed Oil and Curcubita Pepo (Pumpkin) Seed Oil and Phospholipids, a mixture of butylene Glycol and Barosma Betulina Leaf Extract and Citrie
Acid, a mixtore of cedrus atlantica bark extract and hatylene Glycol and Barosma Betglina
Leaf Extract and Citric Acid, a mixture of ORTHOSIPHON STAMINEUS LEAF EXTRACT and water and maltodextrin and wanthan gum, a mixture of Butylene Glycol and Enantia
Chlorantha Bark Extract and Oleanolic Acid, a miture of melia azadirachta leaf and arctium lappa root, a mixture of Sarcosine and Cinnamomum Zeylanicum Bark Extract and kojic acid,
Bambusa Arundinacea Siem Extract, a mixture of Farnesyl Acetate and Panthenyl Triacetate and Tocopheryl Acetate and salicylic acid and salix alba bark and leptospermum scoparium, a mixture of cassia italica and saponaria officinalis and santalum album and lamium album and plantago major and myrtus communis and origanum marjorana and lysine carboxymethyl cysteinate and lysine thiazolidine and alchemilla vulgaris extract and harpagophytum procubens root extract and dioic acid and glycolic acid and lactic acid and mandelic acid and gluconolactone and lactobionic acid and algae extract and laminaria saccharina extract and acetyl glucosamine and hinokitiol and acacia senegal gom and melaleuca altemiola leaf oil,
Caprviovl Salicghe Acid, s mixture of Chlorhexidine Digluconate and Proctone Olamine and carnosine and azelaic acid and sulfur and calamine and witch hazel extract and silymarin and ferulic acid, a mixture of L ascorbic acid and benzoyl peroxide and tartaric acid and citric acid, charcoal, kaolin, or a mixture thereof.
[00090] In addition to the active ingredient, the disclosed cosmetic compositions may comprise any number of additional ingredients, such as, but not limited to: additional active ingredients (e.g., cosmetic, dermatological, and/or pharmaceutical), alcohols, allergy inhibitors, amino acids, anti-acne agents (e.g., salicylic acid), anti-aging agents, antiseptics,
Octrooi (aanvraag): 2037617 27 antifungal agents, analgesics, anti-hair loss agents, anti-wrinkle agents, antibacterial agents, anti-microbial agents, anti-oxidants, anti-inflammatory agents, burn healing agents, colorants (e.g., lakes, pigments, and the like), de-pigmentation agents, deodorants, dyes, emollient (e.g., glycerin, butylene glycol), excipients, fatty substances, fillers, film formers e.g., dimethicone acrylate copolymer, ethylhexyl acrylate copolymer), fragrances, free radical scavengers, glycerin, glycerin monostearate, glycerin distearate, hair growth agents, hair conditioners, hair softeners, hair moisturizers, herbal extracts, humectants (e.g., hyaluronic acid, orotic acid, lipoprotein), insect repelants, medication, moisturizers, non-active carrier oils (e.g, triglycerides, silicone oils, mineral oils), oils, peptides, polypeptides, proteins, perfumes, pigments, preservatives, plasticizers, reflectants, sebum absorbers, skin lightening agents, sunscreens, surfactants, tanning agents, thickening agents hydroxyethylcellulose, xanthan gum, carbomer), Vaseline, vasoconstrictors, vasodilators, vitamins (e.g.. Vitamin A, Vitamin E), water, waxes, and/or combinations thereof.
[00091] In addition to the active ingredient, the disclosed cosmetic compositions may comprise any number of additional ingredients, such as, but not limited to: additional active ingredients (e.g., cosmetic, dermatological, and/or pharmaceutical), alcohols, allergy inhibitors, amino acids, anti-acne agents (e.g., salicylic acid), anti-aging agents, antiseptics, antifungal agents, s, analgesics, anti-hair loss agents, anti-wrinkle agents, antibacterial agents, anti-microbial agents, anti-oxidants, anti-inflammatory agents, burn healing agents, colorants (e.g. lakes, pigments, and the like), de-pigmentation agents, deodorants, dyes, emollient (e.g., glycerin, butylene glycol), excipients, fatty substances, fillers, film formers e.g., dimethicone acrylate copolymer, ethylhexyl acrylate copolymer), fragrances, free radical scavengers, glycerin, glycerin monostearate. glycerin distearate, hair growth agents, hair conditioners, hair softeners, hair moisturizers, herbal extracts, humectants (e.g., hyaluronic acid, orotic acid, lipoprotein), insect repelants, medication, moisturizers, non-active carrier oils (e.g., triglycerides, silicone oils, mineral oils), oils, peptides, polypeptides, proteins, perfumes, pigments, preservatives, plasticizers, reflectants, sebum absorbers, skin lightening agents, sunscreens, surfactants, tanning agents, thickening agents hydroxyethylcellulose, xanthan gum, carbomer), Vaseline, vasoconstrictors, vasodilators, vitamins (e.g., Vitamin A, Vitamin E), water, waxes, and/or combinations thereof.
Octrooi (aanvraag): 2037617 28
[00092] Sunscreens components can include zinc oxide, titanium dioxide, octinoxate, ensulizole, ethylhexyl triazone, octyl salicylate, butyl methoxydibenzoylmethane, bisethylhexyloxyphenol methoxyphenyl triazine, isoamyl-p-methoxycinnamate, diethylhexyl butamido triazone, or a mixture thereof. In some aspects, the sunscreen components can be free of octocrylene. Additionally, according to some aspects, the sunscreen formulations described herein are eco-compatible compositions. For example, the sunscreen formulations are compatible with organism life and not harmful to marine ecosystems (in particular for tropical environments with coral reefs). Specifically, the sunscreen formulations are free of components that inhibit cell growth or cell replication in a marine environment. In some examples, this can be accomplished by the sunscreen formulations being free of bis ethylhexyloxyphenol methoxyphenyl triazine (BEMT), cinnamates, benzophenones, camphor derivatives, titanium oxide, melaleuca essential oil, ylang ylang flower extracts, Bambousa
Arundinacea extracts, Karite, animal-derived fats, argan oil, ocopheryl acetate, tocopherol, retinol, polyphenolic compounds extracted from green tea or mixtures thereof.
[00093] The composition of the present disclosure may also include other cosmetic ingredients such as, but not limited to, humectants emollients, moisturizers, anti-wrinkle ingredients, concealers, matte finishing agents, pigments, colorants, proteins, anti-oxidants, bronzers, chelating agents, emulsifiers, ultraviolet (UV) absorbing agents, oil absorbing agents, anti-foam agents, anti-tack agents, thickeners, fragrances, preservatives, anti-microbials, fungistats, neutralizing agents, vitamins, plasticizers, cohesion agents, basifying and acidifying agents, fillers, solvents, and mixtures thereof.
[00094] The compositions may contain additional ingredients such as alkalinizing agents, emulsifying agents, emollients, plasticizers, preservatives, humectants, moisturizing agents, solvents, and tonicity agents or active ingredients suitable to provide anti-aging benefits. Examples of preferred additional ingredients include glycerin.
[00095] Additional ingredients may optionally be added to the disclosed compositions as detailed below.
[00096] Colorants or pigments: The compositions may comprise one or more cosmetic powders, for example, calcium aluminum borosilicate, PMMA, polyethylene, polystyrene, methyl methacrylate crosspolymer, nylon-12, ethylene/acrylic acid copolymer, boron nitride,
Teflon, silica, or the like. Typically the compositions will include colorants or pigments to
Octrooi (aanvraag): 2037617 29 impart a desired color or effect, examples are inorganic pigments, organic pigments, and/or lakes. Exemplary inorganic pigments include, but are not limited to, metal oxides and metal hydroxides such as magnesium oxide, magnesium hydroxide, calcium oxide, calcium hydroxides, aluminum oxide, aluminum hydroxide, iron oxides (a-Fe;Os, y-Fe203, Fe304,
FeO), red iron oxide, yellow iron oxide, black iron oxide, iron hydroxides, titanium dioxide, titanium lower oxides, zirconium oxides, chromium oxides, chromium hydroxides, manganese oxides, cobalt oxides, cerium oxides, nickel oxides and zinc oxides and composite oxides and composite hydroxides such as iron titanate, cobalt titanate and cobalt aluminate. Non-metal oxides such as alumina and silica, ultramarine blue (i.e., sodium aluminum silicate containing sulfur), Prussian blue, manganese violet, bismuth oxychloride, talc, mica, sericite, magnesium carbonate, calcium carbonate, magnesium silicate, aluminum magnesium silicate, silica, titanated mica, iron oxide titanated mica, bismuth oxychloride, and the like, are also contemplated to be suitable inorganic pigments. Organic pigments can include, but are not limited to, at least one of carbon black, carmine, phthalocyanine blue and green pigment, diarylide yellow and orange pigments, and azo-type red and yellow pigments such as toluidine red, litho red, naphthol red and brown pigments, and combinations thereof.
[00097] Lakes generally refer to a colorant prepared from a water-soluble organic dye, (e.g., D&C or FD&C) which has been precipitated onto an insoluble reactive or adsorptive substratum or diluent. The term “D&C” as used herein means drug and cosmetic colorants that are approved for use in drugs and cosmetics by the FDA. The term “FD&C” as used herein means food, drug, and cosmetic colorants which are approved for use in foods, drugs, and cosmetics by the FDA. Certified D&C and FD&C colorants are listed in 21 CFR. § 74.101 et seq. and include the FD&C colors Blue 1, Blue 2, Green 3, Orange B, Citrus Red 2, Red 3, Red 4, Red 40, Yellow 5, Yellow 6, Blue 1, Blue 2, Orange B, Citrus Red 2, and the D&C colors
Blue 4, Blue 9, Green 5, Green 6, Green 8, Orange 4, Orange 5. Orange 10, Orange 11, Red 6,
Red 7, Red 17, Red 21, Red 22, Red 27, Red 28, Red 30, Red 31, Red 33, Red 34, Red 36, Red 39, Violet 2, Yellow 7, Yellow 8, Yellow 10, Yellow 11, Blue 4, Blue 6, Green 5, Green 6,
Green 8, Orange 4, Orange 5, Orange 10, Orange 11, and so on. Substrates suitable for forming lakes include, without limitation, mica, bismuth oxychloride, sericite, alumina, aluminum, copper, bronze, silver, calcium, zirconium, barium, and strontium, titanated mica, filmed silica, spherical silica, polymethylmethacrylate (PMMA), micronized teflon, boron nitride, acrylate
Octrooi (aanvraag): 2037617 30 copolymers, aluminum silicate, aluminum starch octenylsuccinate, bentonite, calcium silicate, cellulose, chalk, corn starch, diatomaceous earth, fuller's earth, glyceryl starch, hectorite, hydrated silica, kaolin, magnesium aluminum silicate, magnesium trisilicate, maltodextrin, montmorilionite, microcrystalline cellulose, rice starch, silica, talc, mica, titanium dioxide, zinc laurate, zinc myristate, zinc rosinate, alumina, ahapulgite, calcium carbonate, calcium silicate, dextran, nylon, silica silylate, silk powder, sericite, soy flour, tin oxide, titanium hydroxide, trimagnesium phosphate, walnut shell powder, and mixtures thereof. Suitable lakes include, without limitation, those of red dyes from the monoazo, disazo, Norm, xanthene, or indigoid families, such as Red 4, 6, 7, 17, 21, 22, 27, 28, 30, 31, 33, 34, 36, and Red 40; lakes of yellow pyrazole, monoazo, fhioran, xanthene, quinoline, dyes or salt thereof, such as Yellow 5,6, 7, 8, 10, and 11; lakes of violet dyes including those from the anthroquinone family, such as
Violet 2, as well as lakes of orange dyes, including Orange 4, 5, 10, 11, and the like. Suitable lakes of D&C and FD&C dyes are defined in 21 CFR. § 82.51.
[00098] The coloring agents may be optionally surface treated, for example, to make the particles more hydrophobic or more dispersible in a vehicle. The surface of the particles may, for example, be covalently or ionically bound to an organic molecule or silicon-based molecule or may be adsorbed thereto, or the particle may be physically coated with a layer of material.
The surface treatment compound may be attached to the particle through any suitable coupling agent, linker group, or functional group (e.g., silane, ester, ether, etc). The compound may comprise a hydrophobic portion which may be selected from, for example, alkyl, aryl, ailyl, vinyl, alkyl-aryl, aryl-alkyl, organosilicone, di-organosilicone, dimethicones, methicones, polyurethanes, silicone-polyurethanes, and fluoro- or perfluoro-derivatives thereof. Other hydrophobic modifiers include lauroyl lysine, isopropyl Titanium Triisostearate (ITT), ITT and
Dimethicone (ITT/Dimethicone) cross-polymers, ITT and Amino Acid,
ITT/Triethoxycaprytylsilarte Crosspolymer, waxes (e.g., carnauba), fatty acids (e.g., stearates),
HDVTrimethylol Hexylactone Crosspolymer, PEG-8 Methyl. Ether Triethoxysilane, aloe, jojoba ester, lecithin, perfluoroalcohol phosphate, and Magnesium Myristate (MM), to name a few.
[00099] An optional pigment component includes and alkyl silane surface-treated colorant consisting essentially of or comprising an alumina substrate (e.g., platelet shaped) and a pigment, dye, or lake bonded to the alumina substrate by an alkyl silane surface treatment,
Octrooi (aanvraag): 2037617 31
Typically, the alkyl slime will be octylsilane, and may be formed by treatment with triethoxy caprylylsilane. Non-limiting examples of such colorants include, but are not limited to,
Alumina/Titanium Dioxide/Triethoxycaprylylsilane 1% (COVALUMINE Atlas White AS),
Alumina/D&C Red Aluminum Lake CTD/Triethoxycaprylylsilane 1% (COVALUMINE Red
Rose AS), Alumina/D&C Red Aluminum Lake CTD/Triethoxycaprylylsilane 1% (COVALUMINE Sonoma Red AS), Alumina/Black Iron Oxide CTD/Triethoxycaprylylsilane 1% (COVALUMINE Sonoma Black AS), Alumina/D&C Red #6 Aluminum Lake
CTD/Triethoxycaprylylsilane 1% (COVALUMINE Fire Red AS), Alumina/Yellow Iron
Oxide CTD/Triethoxycaprylylsilane 1% (COVALUMINE Sonoma Yellow AS),
Alumina/D&C Blue #1 Aluminum Lake CTD/Triethoxycaprylylsilane 1% (COVALUMINE
Astral Blue AS), Alumina/Carmine CTD/Triethoxycaprylylsilane 1% (COVALUMINE
Campari AS), Alumina/Yellow #5 CTD/Triethoxycaprylylsilane 1% (COVALUMINE
Sunburst AS), Alumina/Triethoxycaprylylsilane 1%, and combinations thereof, each of which is available from SENSIENT Cosmetic Technologies LCW.
[000100] Interference or pearl pigments may also be included. These are typically comprised of micas layered with about 50 to 300 nm films of TiO», Fe203, or Cr20:3 or the like.
These include white nacreous materials, such as mica covered with titanium oxide or covered with bismuth oxychloride; and colored nacreous materials, such as titanium mica with iron oxides, titanium mica with ferric blue or chromium oxide, titanium mica with an organic pigment of the aforementioned type. If these materials are used, it is preferred that these materials are used collectively in an amount of less than 1.0 wt %. Preferably, the pearlescent component has a bismuth oxychloride based pearlescent ingredient or reflectance pearls.
Bismuth oxychloride matches the skin's natural pearlescence more than compounds such as titanium oxide, which provide for a more artificial look. Bismuth oxychloride better mimics the skin's natural reflectance. However, other pearlescent ingredients may be used. A preferred pearlescent component is called CHROMA-LITE, which is a combination of colored pigment bonded to BI-LITE 20 (bismuth oxychloride and mica} using calcium stearate, The CHROMA-
LITE component is available in various shades/colors from Englehard Corporation (Iselin,
NJ).
[000101] Cosmetically acceptable vehicles: The disclosed compositions will typically comprise a cosmetically acceptable vehicle. “Cosmetically acceptable” as used herein means
Octrooi (aanvraag): 2037617 32 that it is safe for contact with a human integument. The vehicle may comprise a liquid, comprising a single phase, a dual-phase system, or an emulsion. Emulsions include oil-in- water, silicone-in-water, water-in-oil, water-in-silicone, and the like. When formulated as an emulsion, an emulsifier is typically included. Special mention may be made of volatile silicones (e.g. cyclopentasiloxane), hydrocarbons, ester oils, lower alcohols (e.g., ethanol, isopropyl alcohol, etc.), and water.
[000102] Emollients: Emollients may be used in the disclosure, and include, but are not limited to, ester oils, which will typically be the etherification product of an acid of the form
R4(COOH)1.2 with an alcohol of the form Rs(OH);.3 where R4 and Rs are each independently linear, branched, or cyclic hydrocarbon groups, optionally containing unsaturated bonds, and having from 1 to 30 carbon atoms, preferably from 2 to 30 carbon atoms, and more preferably, from 3 to 30 carbon atoms, optionally substituted with one or more functionalities including hydroxyl, oxa, oxo, and the like. Preferably, at least one of R4 and Rs comprises at least one fatty chain. The esters defined above will include, without limitation, the esters of mono-acids with mono-alcohols, mono-acids with diols and triols, di-acids with mono-alcohols, and tri- acids with mono-alcohols. Other emollients include dimethicone. Humectants, such as glycerin and other C1-10 polyols or diols may also be included.
[000103] Absorbent Powders: Absorbent powders capable of absorbing oils for increased comfort can be added. Examples of suitable absorbent powders can include silica, mica, elastomers, kaolin, starch, or mixtures thereof.
[000104] Fillers: Fillers can also optionally be added, in an amount from about 1% to about 20%, preferably from about 1% to about 10% by weight of the final composition.
Examples of fillers include, but are not limited to, silica, PMMA, nylon, alumina, barium sulfate, or any other filler typically used in such compositions. 1000105] Film formers: Polymeric film formers include cellulosics, polyolefins, polyvinyls, polacrylates, polyurethanes, silicones, silicone acrylates, polyamides, polyesters, fluoropolymers, polyethers, polyacetates, polycarbonates, polyimides, rubbers, epoxies, formaldehyde resins, and homopolymers and copolymers of any of the foregoing. In particular,
When present, the film former can be in a range of from about 2 wt% to about 20 wt% of the active component, about 7 wt% to about 13 wi% of the active component, less than, equal to, or greater than about 2 wt%, 3,4, 5,6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, or about
Octrooi (aanvraag): 2037617 33 20 wt%. As described herein above, the film former can be used to help produce a homogenous mixture of the extract solution as well as help to evenly distribute the composition about a user’s skin. According to various aspects, the film former can include Acrylates Copolymer,
Acrylates Copolymer (and) Acrylates/Polytrimethylsiloxymethaerylate Copolymer,
ACRYLATES/ OCTYLACRYLAMIDE COPOLYMER, Acrylates/C1-2
Succinates/Hydroxyacrylates Copolymer, Acrylates/C12-22 Alkyl Methacrylate Copolymer,
Acrylates/Dimethicone ~~ Copolymer, Acrylates/Ethylhexyl ~~ Acrylate Copolymer,
Acrylates/Hydroxyesters Acrylates Copolymer, Acrylates/Lauryl Acrylate/Stearyl
Acrylate/Ethylamine Oxide Methacrylate Copolymer, Acrylates/Octylacrylamide Copolymer
Acrylates/Polytrimethylsiloxymethacrylate Copolymer,
Acrylates/Polytrimethylsiloxymethacrylate Copolymer (and) Laureth-1 Phosphate,
Acrylates/t-Butylacrylamide Copolymer, Adipic Acid/Diglycol Crosspolymer, Adipic
Acid/Neopentyl Glycol/Trimellitic Anhydride Copolymer, Algin Aluminum Starch
OctenylsuccinateAMP-Acrylates Copolymer, Behenyl Methacrylate/t-Butyl Methacrylate
Copolymer, Brassica Campestris/Aleurites Fordi Ol Copolymer, Butyl
Acrylate/Hydroxypropyl Dimethicone Acrylate Copolymer, Butyl Ester of PVM/MA
Copolymer, C24-28 Alkyldimethylsdoxy Trimethylsiloxysilicate, Capryloyl Glycerin/Sebacic
Acid Copolymer, Diisostearoyl Polyglyceryl-3 Dimer Dilinoleate, Ethyl Ester of PVM/MA
Copolymer, Isobutylene/Ethylmaleimide/Hydroxyethylmaleimide Copolymer, Isopropyl Ester of PVM/MA Copolymer, Methacryloyl Ethyl Betaine/Acrylates Copolymer,
Octylacrylamide/Acrylates/Butylaminoethyl Methacrylate Copolymer,
Phenylpropyldimethylsiloxysilicate, Polyamide-3, Polyamide-8, Polyester-10, Polyester-7,
Polyethylene, Polymethylsilsesquioxane, Polyurethane-1, Polyurethane-14 (and) AMP-
Acrylates Copolymer, Polyurethane-18, Polyurethane-34, Polyurethane-35, Polyurethane-48,
Polyurethane-64, Polyurethane-93, Polyvinyl Stearyl Ether, PPG-17/IPDVDMPA Copolymer,
PPG-26/Dimer Dilinoleate Copolymer, Pullulan, PVP, PVP CROSSPOLYMER, Sodium
Polyacrylate, Sodium Polystyrene Sulfonate, Styrene/Acrylates Copolymer, Styrene/VP
Copolymer, Triacontanyl PVP, Trifluoropropyldimethylsiloxy/Trimethylsiloxy
Silsesquioxane, Trimethylpentanediol/Adipic Acid/Glycerin Crosspolymer,
Trimethylsiloxysilicate, VA/Butyl, Maleate/Isobornyl Acrylate Copolymer, VA/Crotonates
Copolymer, VA/Crotonates/Vinyl Neodecanoate Copolymer, Vinyl
Octrooi (aanvraag): 2037617 34
Caprolactam/VP/Dimethylaminoethyl Methacrylate Copolymer, VP/ HEXADECENE
COPOLYMER, VP/Acrylates/Lauryl Methacrylate Copolymer,
VP/Dimethylaminoethylmethacrylate Copolymer, VP/DMAPA Acrylates Copolymer,
VP/Eicosene Copolymer, VP/Hexadecene Copolymer, VP/Methacrylamide/Vinyl Imidazole
Copolymer, VP/VA Copolymer, VP/Vinyl Caprolactam/DMAPA Acrylates Copolymer, copolymers thereof, or mixtures thereof. In specific aspects, the film former can include sodium polyacrylate.
[000106] Oils: Suitable non-limiting examples of oils for the oil phase (for example, in an emulsion) include natural and synthetic oils, including animal, vegetable, and petroleum oils; fatty acid triglycerides; fatty acid esters such as octyl palmitate, isopropyl myristate and isopropyl palmitate; ethers such as dicapryl ether; fatty alcohols such as cetyl alcohol, stearyl alcohol and behenyl alcohol; sterols; hydrocarbons such as isooctane, isododecane, isohexadecane, decane, dodecane, tetradecane, tridecane, Cs20 isoparaffins, mineral oil, petrolatum, isoeicosane and polyisobutene; Cio.30 cholesterol/lanosterol esters; lanolin; and the like. Representative hydrocarbons include paraffinic hydrocarbons available from Exxon under the ISOPARS trademark. and from the Permethyl Corporation. In addition, Cs.20 paraffinic hydrocarbons such as Cj; isoparaffin (isododecane) manufactured by the Permethyl
Corporation having the tradename PERMETHYL 99ATM. are also contemplated to be suitable. Various commercially available Cis 1soparaffins, such as isohexadecane (having the tradename PERMETHYL.RTM.) are also suitable. Silicone oils such as dimethicones, cyclic silicones, and polysiloxanes may also be included in the oil phase. In one aspect, silicone oils are present in an amount less than about 5% by weight of the oil phase.
[000107] Solvents: The cosmetically acceptable vehicle may comprise a volatile solvent.
Typically, a volatile solvent may have a vapor pressure of above about 0.01 mmHg at 20.degree. C. Volatile solvents may include volatile Cs.12 hydrocarbons (e.g., isododecane), aromatic hydrocarbons (e.g., xylenes, toluene, etc.), ketones acetone, methylethyl ketone, etc.), ethers (e.g., diethyl ether, methylethyl ether, etc.), perfluorohydrocarbons, hydrofluoroethers,
Freons, esters of acetic acid (e.g., ethylacetate, butylacetate, etc.) and the like. Preferred volatile solvents will be cosmetically acceptable. The solvent can be an organic solvent. Where present, the solvent is in a range of from about 10 wt% to about 50 wt% of the active component, about 30 wt% to about 40 wt% of the active component, less than, equal to, or greater than about 30
Octrooi (aanvraag): 2037617 35 wit%, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, or about 50 wt% of the composition. Examples of organic solvents can include an isododecane component, an alkyl benzoate component, and a neopentyl glycol diheptanoate component. Isododecane (an example of which is represented by CAS 31807-55-3) is generally understood to be a clear, colorless and odorless, volatile liquid, which makes it suitable for use in color cosmetics like mascara, eyeliner, lip products, or any product where improved wear properties and no residues are wanted. It does not leave an oily residue. Isododecane is a volatile, lipophilic component for deodorant sprays and hair care applications. It is a hydrocarbon ingredient used as a solvent.
The alkyl benzoate component can be C12-15 alkyl benzoate (an example of which is represented by CAS 68411-27-8), which is generally understood to be a low-molecular weight ester of benzoic acid and C12-15 alcohols. C12-15 alkyl benzoate is a clear liquid that is practically odorless. In some examples, the alkyl benzoate component includes a C12 alkyl benzoate, a C13 alkyl benzoate, a C14 alkyl benzoate, a C15 alkyl benzoate, or a mixture thereof, Neopentyl glycol diheptanoate (an example of which is represented by CAS 68855- 18-5) is generally understood to be a mixture of texture-enhancing ingredient neopentyl glycol and grape-derived fatty acid heptanoic acid.
[000108] According to various aspects of the present disclosure, the composition is substantially free of cyclopentasiloxane. For example, the composition can include less than about 10 wt% cyclopentasiloxane, less than about 9 wt%, less than about 8 wt%, less than about 7 wt%, less than about 6 wt%, less than about 5 wt%, less than about 4 wt%, less than about 3 wt%, less than about 2 wt%, less than about 1 wt%, less than about 0.5 wt%, less than about 0.1 wt%, less than about 0.01 wt%, or less than about 0.001 wt%. in some aspects, the composition is completely free (e.g., includes O wt?) of cyclopentasiloxane. The disclosed isododecane component, alkyl benzoate component, and neopentyl glycol diheptanoate component, together, function to effectively replace cyclopentasiloxane in an while having similar, equal, or superior performance. Replacing cyclopentasiloxane can be desirable because, despite its performance in compositions, regulatory schemes seek to limit cyclopentasiloxane’s use in cosmetic products. Therefore, it 1s important to find an effective substitute for cyclopentasiloxane. Suitable substitutes can include an oleochemical component such as dicaprylyl carbonate, dicaprylyl ether, or a mixture thereof.
Octrooi (aanvraag): 2037617 36
[000109] The surface of all or a portion of the individual pigments of the pigment components can be at least partially coated. Examples of suitable coatings include a lauroyl lysine coating, a silane coating, a methicone coating, a dimethicone coating, a stearoyl glutamic acid, or a combination thereof. As generally understood, a lauroyl lysine is an amino acid derivative, derived from natural product lysine a protein and lauric acid another natural coconut fatty acid. lauroyl lysine treatment creates hydrophobic system with enhanced dispersion, increased wear properties and make up with a wet feel on the skin. Pigment surfaces are smooth, flat and less fluffy than with silane treatment, thus easier to press. Lauroyl lysine coatings are lubricious, giving the substrate a smooth, moist feel. As generally understood, a silane coating is a deposition of coatings through the reaction of silanols with the pigment. By hydrolysis of “Si— OR” groups to silanol (Si - OH), alkyl silane can self-associate or hydrogen bond to the pigment surface, so stable bonds are formed between the pigment and the treating compound following curing. Silicone treated pigments disperse well in cyclomethicones. They have very low surface tension, so they have excellent hydrophobicity and better lipophilicity due to which they easily disperse in mineral oils, esters and silicone fluids. Pigments treated with alkyl silane are more hydrophobic than methicone treated pigments, wet better in commonly utilized cosmetic oils and have lower oil absorption. In hydrous compact formulations, the excellent wetting imparted by alkyl silane treatment allows incorporation of high pigment loads to achieve a “powdery” sensation upon application to the skin while maintaining a low melt viscosity for hot filling. As generally understood, a methicone coating is a polymethylhydrogen siloxane, which absorb traces of water from pigment surface and converts Si - H bond to Si - OH with liberation of small amount of hydrogen gas and upon curing form covalent Si - 0 pigment chemical bonds. The coating formed is highly hydrophobic and not solubilized by common solvents. The pigments wet well in oils particularly silicone oils. Skin feel is somewhat dry with enhanced slip and spreadability. As generally understood, a dimethicone coating (also called polymethylsiloxane) is a coating bonded to a pigment or filler surface via the mechanism of hydrolysis, condensation and curing to a Si — O pigment linkage. Surface treated with dimethicone are quite hydrophobic and have good slip and more lubricious feel. It is useful in oil based systems, which may be used for anhydrous products.
[000116] On individual pigments, the coating can substantially coat 100% of the total surface area of the individual pigment. In some further aspects, the coating can coat about 5%
Octrooi (aanvraag): 2037617 37 to about 95% of the total surface area of the individual pigment about 10% of the total surface area to about 90% of the total surface area, about 15% of the total surface area to about % of the total surface area, about 20% of the total surface area to about 80% of the total surface area, about 25% of the total surface area to about 75% of the total surface area, about 30% of the total surface area to about 70% of the total surface area, about 35% of the total surface area to about 65% of the total surface area, about 40% of the total surface area to about 60% of the total surface area, about 45% of the total surface area to about 50% of the total surface area, less than, equal to, or greater than about, 5% of the total surface area, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39,40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 715, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89,90, 91, 92, 93, 94, or about 95% of the total surface area. In some aspects, at least a portion of the total number of pigments present may be substantially free of any coating. For example, when less than 100% of the total number of pigments include a coating about 5% to about 95% of the total number of pigments can include a coating, about 10% to about 90% of the total number of pigments can include a coating, about 15% to about % of the total number of pigments can include a coating, about 20% to about 80% of the total number of pigments can include a coating, about 25% to about 75% of the total number of pigments can include a coating, about 30% to about 70% of the total number of pigments can include a coating, about 35% to about 65% of the total number of pigments can include a coating, about 40% to about 60% of the total number of pigments can include a coating, about 45% to about 50% of the total number of pigments can include a coating, less than, equal to, or greater than about, 5% of the total number of pigments can include a coating, 6. 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43,44, 45,46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58. 59, 60, 61, 62, 63, 64, 65, 66, 67, 68,69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, or about 95%. Each pigment can be coated with the same material or a different portions of the pigments can be at least partially coated with different coatings. An example of a suitable coating is stearoyl glutamic acid.
[000111] In some examples in which the coating is stearoyl glutamic acid, the composition includes Triglycerol diisosterarate, glyceryl stearate, or a combination thereof.
Octrooi (aanvraag): 2037617 38
[000112] Thickeners: Suspending and thickening agents typically include silica gels, gums, clays, fumed silica, fatty acid soaps, and various hydrocarbon gels, and other ingredients that when incorporated into the formulation remain on the surface of keratinous tissues as disclosed in the International Cosmetic Dictionary and Handbook (12th Ed.), which is hereby incorporated by reference. Viscosifying agents such as gellants may also be used. Examples include bentone, triglycerides, aluminum stearate, C18-C36 acid glycol esters, glyceryl tribehenate, glycerol monostearate, alginates, carbomers, celluloses, gums; carageenans, starches or silicates.
[000113] Waxes: Waxes which may be used in the disclosure include, but are not limited to, linear polyethylene, microcrystalline petroleum wax, carnauba wax, lignite wax, ouricouri wax, rice bran wax, castor wax, mortar wax, stearone, acrawax, bayberry wax, castor wax,
Japan wax, ozokerite, beeswax, candelilla wax, petrolatum, ceresin wax, cocoa butter, illipe butter, esparto wax, shellac wax, ethylene glycol diesters or triesters of C18-C36 fatty acids, cetyl palmitate, paraffin wax, hard tallow. lanolin, lanolin alcohol, cetyl alcohol, glyceryl monostearate, sugarcane wax, jojoba wax, stearyl alcohol, silicone waxes, and combinations thereof.
[000114] In some aspects of the present disclosure, the composition can include a preservative. Where present, the preservative can be a range of from about 0.0001 wt% to about 0.5 wt% of the composition, about 0.0003 wt% to about 0.1 wt%, less than, equal to, or greater than about 0.0001 wt%, 0.0003, 0.0005, 0.001, 0.005, 0.01, 0.05, 0.1, or about 0.5.
[000115] When included, the preservative is included in an amount sufficient to prevent spoilage or prevent growth of inadvertently added microorganisms for a specific period of time, but not sufficient enough to contribute to the odor neutralizing performance of the composition.
In other words, the preservative 1s not being used as the antimicrobial compound to kill microorganisms on the surface onto which the composition is deposited in order to eliminate odors produced by microorganisms. Instead, it is being used to prevent spoilage of the composition in order to increase shelf-life. {000116} The preservative can be any organic preservative material which will not cause damage to fabric appearance, e.g., discoloration, coloration, bleaching. Suitable water-soluble preservatives include organic sulfur compounds, halogenated compounds, cyclic organic nitrogen compounds, low molecular weight aldehydes, parabens, propane diol materials,
Octrooi (aanvraag): 2037617 39 isothiazolinones, quaternary compounds, benzoates, low molecular weight alcohols, dehydroacetic acid, phenyl and phenoxy compounds, or mixtures thereof,
[000117] Non-limiting examples of commercially available water-soluble preservatives include a mixture of about 77% S5-chloro-2-methyl-4-isothiazolin-3-one and about 23% 2- methyl-4-isothiazolin-3-one, a broad spectrum preservative available as a 1.5% aqueous solution under the trade name Kathon® CG by Rohm and Haas Co.; 5-bromo-5-nitro-1,3- dioxane, available under the tradename Bronidox L® from Henkel; 2-bromo-2-nitropropane- 1,3-diol, available under the trade name Bronopol® from Inolex; 1,1'-hexamethylene bis(5-(p- chlorophenyl)biguanide), commonly known as chlorhexidine, and its salts, e.g., with acetic and digluconic acids; a 95:5 mixture of 1,3-bisthydroxymethyl)-5,5-dimethyl-2,4- imidazolidinedione and 3-butyl-2-iodopropynyl carbamate, available under the trade name
Glydant Plus® from Lonza; N-[1,3-bisthydroxymethyl)2.5-dioxo-4-imidazolidinyl]-N,N'- bisthydroxy-methyl) urea, commonly known as diazolidinyl urea, available under the trade name Germall® IH from Sutton Laboratories, Inc; N,‚N”-methylenebis {N'-{1- (hydroxymethyl)-2,5-dioxo-4-imidazolidinyljurea}, commonly known as imidazolidinyl urea, available, e.g., under the trade name Abiol® from 3V-Sigma, Unicide U-13® from Induchem,
Germall 115® from Sutton Laboratories, Inc.; polymethoxy bicyclic oxazolidine, available under the trade name Nuosept® C from Hills America; formaldehyde; glutaraldehyde; polyaminopropyl biguanide, available under the trade name Cosmocil CQ® from ICI
Americas, Inc., or under the trade name MikrokilI® from Brooks, Inc; dehydroacetic acid; and benzsiothiazolinone available under the trade name Koralone™ B-119 from Rohm and Hass
Corporation.
[000118] The composition can further include an inactive component, The inactive component can be in a range of from about 50 wt% to about 90 wt% of the composition, about 75 wt% to about 85 wt% of the composition, less than, equal to, or greater than about 50 wt%, 51,52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, or about 90 wtb. when the inactive component is present, the active component is in a range of from about 10 wt% to about 50 wt% of the composition, about 15 wt% to about 25 wt% of the composition, less than, equal to, or greater than about 10 wt%, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26,
Octrooi (aanvraag): 2037617 40 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, or about 50 wt% of the composition.
[000119] In one aspect, the composition is a pretreatment composition which consists of a nonpigmented formulation containing an active component for application to the integument for the purpose of sebum reduction prior to application of a colored cosmetic composition. Any portion of the aforementioned constituents can be combined in any desirable manner to produce many different types of cosmetic compositions. The cosmetic compositions can be applied to the epithelial layer of a user’s skin. For example the cosmetic composition can be a pretreatment formulation, make-up formulation, a foundation, a sunscreen, or any other cosmetic applied to a user’s epithelial tissue. Additionally, any portion of the aforementioned constituents can be combined to create a cosmetic formulation that can be applied to a keratinous tissue of a user. For example, the cosmetic formulation can be a mascara, hair dye, nail polish, lip gloss, lipstick or other pigmented/colored cosmetic formulation intended to be a long-wear composition.
[000120] In one aspect, the lotus plant denved constituents {(g.g..the lotus flower extract blend and/or constituents thereof } may be formulated and/or utilized in products and/or regimens that reduces perspiration in a subject. In some examples, perspiration reduction is accomplished primarily without clogging pores.
[000121] In one aspect, the lotus plant denved constituents may be formulated and/or unlized in the form of a primer for creating a substantially flawless canvas for longer lasting makeup following application. In another embodiment, the lotus plant derived constituents may be formulated and/or utilized in the form of a foundation composition. Suitable foundation formulations are those that are capable of evening ont skin tone, concealing imperfections and/or providing a flawless matte finish.
[000122] in another aspect, the lotus plant derived constituents may be formulated and/or abilized in the for of a cosmetic concealer that substantially conceals small imperfections, dark spots and circles.
[000123] In another aspect, the lotus plant derived constituents may be formulated and/or utilized in the form of combination cosmetic foundation/concealer product. In another aspect, the lotus plan derived constituents may be Tormulated and/or utilized in the form of a setting spray that may be sprayed over make-up to substantially lock wo a look (following make-
Octrooi (aanvraag): 2037617 41 up application) and protect the skin, The lotus plant derived constiuents may be oulized to help reduce breakouts caused by make-up and sweat.
[000124] In one aspect, the composition may be used to help treat rosacea. Patients with rosacea have symptoms including persistent erythema and flushing, which are secondary manifestations due to neurovascular alteration. Reducing these undesirable manifestations has been studied by administering acetylcholine release. It is thought that the lotus flower extract blend and/or constituents thereof can also have an action on persistent erythema, on rosacea and on redness in general. Therefore, a method of treating rosacea, may include administering a composition includingthe lotus flower extract blend and/or constituents thereof . The composition may be administered topically.
[000125] In one aspect, the lotus flower extract blend and/or constituents thereof decreases sweat production via superficial deposition and potential acetylcholine release inhibition rather than as a clogging or inflammation producing agent. In another aspect, wherein application of a cosmetic formula containing the lotus flower extract blend and/or constituents thereof to skin results in a decreased quantity of face sweat at day 0; day 4; day 14; and/or day 28 after initiation of at least once daily application at a concentration of at least 4% and as compared to application of a formula not containing the lotus flower extract blend and/or constituents thereof
[000126] In another aspect, wherein application of a cosmetic formula containing the lotus flower extract blend and/or constituents thereof to skin on an at least once daily basis for at least 28 days results in improved longwear remanence as assessed by photographic evaluation of wear and as compared to equivalent use of a formula lacking the lotus flower extract blend and/or constituents thereof,
[000127] In another aspect, wherein application of a cosmetic formula containing the lotus flower extract blend and/or constituents thereof to skin on an at least once daily basis for at least 28 days results in decreased generation of porphyrins in the skin as compared to equivalent use of a formula lacking the lotus flower extract blend and/or constituents thereof .
[000128] In another embodiment, the. use of the lotus flower extract blend and/or constituents thereof as an antioxidant component of a cosmetic formula, wherein the proof of concept of the lotus flower extract blend and/or constituents thereof as an antioxidant has been established via screening.
Octrooi (aanvraag): 2037617 42
[000129] Examples
[000130] The following examples are provided as prophetic examples of potential use and results from testing of formulas that utilize a sebum / sweat reducing agent such as
NELUPURE (INCI: PROPANEDIOL (AND) GLYCERIN (AND) NYMPHAEA
CAERULEA FLOWER EXTRACT (AND) NELUMBO NUCIFERA FLOWER EXTRACT) as compared to control formulas that do not utilize such as sebum / sweat reducing agent.
Various aspects of the present disclosure can be better understood by reference to the following
Examples which are offered by way of illustration. The present disclosure is not limited to the
Examples given herein. {000131} Example 1: Consumer Comparison of Long Wear Foundation Compositions
[000132] In a consumer test survey, consumers will be asked to compare a foundation composition comprising the NELUPURE (INCL: PROPANEDIOL (AND) GLYCERIN (AND) NYMPHAEA CAERULEA FLOWER EXTRACT (AND) NELUMBO NUCIFERA
FLOWER EXTRACT) extract solution to a commercialized transfer resistant, foundation composition (Standard) which does not contain the NELUPURE (INCI: PROPANEDIOL (AND) GLYCERIN (AND) NYMPHAEA CAERULEA FLOWER EXTRACT (AND)
NELUMBO NUCIFERA FLOWER EXTRACT) extract solution.
[000133] Each of the consumer testers will apply a layer of each foundation composition onto different clean (i.e. without wearing any face products) halves of their faces (e.g., left side vs. right side) in a double blind test. The consumers will be asked to compare the feel, comfort, appearance/coverage, and ease of removal of each at different times: initially after application, at 8 hours, and up to 9.9 hours after application and answer questions in a questionnaire comparing the two foundation compositions. Data will be tabulated using the
Compusense5 program and analyzed using standard statistical processing programs.
[000134] The comments from the consumer tests described above are expected to indicate that overall, the foundation composition comprising NELUPURE (INCI: PROPANEDIOL (AND) GLYCERIN (AND) NYMPHAEA CAERULEA FLOWER EXTRACT (AND)
NELUMBO NUCIFERA FLOWER EXTRACT) extract solution will provide a significantly more natural look after $ hours of wear compared to the other Standard foundation. The consumers are expected to find that the feel of the novel foundation is significantly more lightweight and comfortable at 8 hours after application when compared to the standard. The
Octrooi (aanvraag): 2037617 43 consumers are expected to think that the disclosed foundation was breathable and comfortable.
As for the appearance or coverage, the consumers are expected to agree that the disclosed foundation evened out skin tone, reduced the appearance of lines and wrinkles, reduced redness, and reduced the appearance of age or sun spots. Overall, it is expected that the disclosed foundation provided a natural and flawless appearance.
[000135] The technical evaluator who oversees the consumer testing is expected to determine that the novel foundation was more visible and provided more coverage at hours after application than the Standard foundation. On average, the novel foundation is expected to last at least 8 hours. The technical evaluator is expected to deem the novel foundation composition to be "long wearing."
[000136] Example 2: Consumer Testing of Long Wear Foundation Composition
[000137] In a consumer test survey, consumer testers will be asked to evaluate the inventive foundation composition comprising the NELUPURE (INCI: PROPANEDIOL (AND) GLYCERIN (AND) NYMPHAEA CAERULEA FLOWER EXTRACT (AND)
NELUMBO NUCIFERA FLOWER EXTRACT) extract solution. Each of the consumer testers will apply a layer of the foundation composition onto their clean faces (i.e., without wearing any face products). The consumers will be asked to evaluate the feel, comfort, application, appearance, and coverage at different times: initially at application and after 8 hours of application and answer questions. The questionnaire will be comprised of a series of questions about the aesthetics and performance of the foundation based on a seven point attribute scale.
An Expert Evaluator will also rate the appearance and wear properties at the initial time point and after 8 hours of wear compared to a Standard.
[000138] Overall, results along the following general description are expected: the consumers will like the composition initially and after 8 hours of wear. They will find that the foundation was easy to apply and blend, providing even coverage and a smooth feel upon application. They will find that the composition was initially lightweight; evened out skin tone; reduced: the appearance of fine lines and wrinkles, appearance of redness, dark under eye circles, age/sun spots, and shine; improved the appearance of skin texture; and provided a flawless and natural look. While after 8 hours of wear, the foundation is expected to be found to be breathable and comfortable. The finish, coverage, and color were expected to be maintained after 8 hours of wear. The foundation composition is expected to still control shine
Octrooi (aanvraag): 2037617 44 and oil breakthrough, while appearing freshly applied. After 8 hours the consumers are expected to find that the foundation did not settle in lines, wrinkles or pores, nor look cakey or masky. Even though it is expected that the foundation did not transfer after 8 hours, it is expected that the significant majority of the consumers will find that the foundation composition is easy to remove.
[000139] Example 3: Inhibition of Acetylcholine Release at the neuromuscular junction
[000140] The aim of the study will be to assess the effect of Nelupure (INCI: Propanediol (and) Glycerin (and) Nymphaea Caerulea Flower Extract (and) Nelumbo Nucifera Flower
Extract) at 0.2%. on the inhibition of Acetylcholine release. The study will be performed with a specific neuromuscular co-culture model. In this model, human fibroblasts will be reprogrammed into pluripotent cells and then differentiated into Motor Neurons. These Motor
Neurons will be cocultured with human muscle cells, creating a functional neuro-muscular junctions. After incubation with Nelupure (INCI: Propanediol (and) Glycerin (and) Nymphaea
Caerulea Flower Extract (and) Nelumbo Nucifera Flower Extract) @ 0.2%., cultures will be activated by glutamate, to induce Acethylcholine release by motor neurons. After activation,
Acetylcholine release will be quantified in the cell culture medium by appropriate ELISA test.
Under these experimental conditions, it is expected to be observed that Nelupure (INCL
Propanediol (and) Glycerin (and) Nymphaea Caerulea Flower Extract (and) Nelumbo Nucifera
Flower Extract) @ 0.2%. highly significantly inhibited (p< 0.0001) Acetylcholine release.
[000141] Example 4: Primer composition
[000142] A primer composition including Nelupure can include the components shown in Table 1.
[000143] Table 1 3-O-Ethyl Ascorbic Acid 0.050-0.150
Octrooi (aanvraag): 2037617 45
Arginine 0.035-0.090 1.500-5.500 5.000-9.000 1 SR Adime au Fo A -2 : a
Ammon Acryloyldimethyltaurate/Beheneth-25 ~~ Methacrylate 1.000-1. 500
Crosspolymer 1,2-Hexanediol AND Caprylyl Glycol 0.500-1.500
Propanediol AND Glycerin AND Nelumbo Nucifera Flower Extract 1.000-3.000
AND Nymphaea Caerulea Flower Extract } °
Water and Blue 1 0.100-0.300
Polysilicone-11 AND Water AND Laureth-12 AND Ethylhexylglycerin | 8.000-12.000 100000
[000144] Example 4: Primer composition
[000145] A primer composition including Nelupure can include the components shown in Table 2.
[000146] Table 2
INCI Mass (%) 65.000-
Sodium Hyaluronate 0.0500-0.1500 10.000-18.000
Ammonium Acryloyldimethyltaurate/Beheneth-25 Methacrylate | 0.150-0.250
Crosspolymer
Cetearyl Alcohol AND Cetearyl Glucoside 1.000-1,250
Octyldodecyl Neopentanoate 1.000-2.000
Pentaerythrity! 'Tetraethylhexanoate 1.000-3.000
Butylene Glycol 2.000-7.000
Sodium Polyacrylate Starch 0.050-0.110 0.250-0.750
Propanediol AND Glycerin AND Nelumbo Nucifera Flower Extract 1.000-3.000
AND Nymphaea Caerulea Flower Extract
Bisabolol 0.050-0.150
Water AND Vaccinium Macrocarpon (Cranberry) Fruit Extract AND | 0.050-0.150 1,2-Hexanediol AND Caprylyl Glycol 1,2-Hexanediol AND Capryivl Glycol 0.050-1.500
Polysorbate 80 50-1.500
[000147] Example 5: Primer composition
Octrooi (aanvraag): 2037617 46
[000148] A primer composition including Nelupure can include the components shown in Table 3.
[000149] Table 3
INCI (where available) Mass (%)
Titanium Dioxide AND Triethoxycaprylylsilane 1-000-3.000
Tocopheryl Acetate 0.300-0.700 10.000-15.000
Dicaprylyl Carbonate AND Tocopherol 2.000-5.000
Dicaprylyl Ether AND Tocopherol 2.000-5.000
Chromium Oxide Greens 0.500-1.000 0.020-0.060
Triethyl Citrate 0.700-1.100
Water 0.050-0.200
Chlorphenesin 0.100-0.300
Stearalkonium Bentonite 1.000-3.000
Mixture of Table 4 40.000-50.000
Mixture of Table 5 10.000-15.000 2,3-Butanediol AND Water 1.000-2.000
Aluminum Starch Octenylsuccinate 1.000-5.000 4.000-8.000
Propanediol AND Glycerin AND Nelumbo Nucifera Flower Extract AND 1.000-3.000
Nymphaea Caerulea Flower Extract
Saccharomyces Ferment AND Lauroyl Lysine 0.400-1.000
Glycerin AND Water AND Centella Asiatica Leaf Extract 0.030-0.:50
[000150] Table 4
INCI Mass (%) 65.000-75.000
SODIUM CHLORIDE 3.500-6.500
Sodium Benzoate 0.200-0.600
Dicaprylyl Carbonate AND Tocopherol 3.000-8.000
Dicaprylyl Ether AND Tocopherol 3.000-8.000
Tri(Polyglyceryl-3/1auryl) Hydrogenated Trilinoleate 1.000-5.000
Cetyl PEG/PPG-10/1 Dimethicone AND Pentaerythrityl Tetra-di-t-butyl | 0.500-2.000
Hydroxyhydrocinnamate
[000151] Table 5
INCI Mass (%)
Octrooi (aanvraag): 2037617 47
Dicaprylyl Carbonate AND Tocopherol 3.000-8.000
Tri(Polyglyceryl-3/Lauryl) Hydrogenated Trilinoleate 2.000-6.000
Dicaprylyl Ether AND Tocopherol 3.500-6.500 6.000-9.000
Cetyl PEG/PPG-10/1 Dimethicone AND Pentaerythrityl Tetra-di-t-butyl | 1.000-5.000
Hydroxyhydrocinnamate
Trimethylsiloxysilicate 13.000-19.000 2.000-6.000
Silica Dimethyl Silylate 1.000-4.000 30.000-39.000 8.000-12.000
SODIUM CHLORIDE 2.000-6.000 0.200-0.600
[000152] Example 6: Primer composition
[000153] A primer composition including Nelupure can include the components shown in Table 6.
[000154] Table 6
INCI Name Mass (%)
Dicaprylyl Carbonate AND Tocopherol 2.000-6.000
Dicaprylyl Ether AND Tocopherol 2.000-6.000
Cetyl PEG/PPG-10/ I Dimethicone AND Phentaerythrityl Tetra-di-t-butyl 0.500-4.0000
Hydroxyhydrocinnamate
Iron Oxides AND Dicaprylyl Carbonate AND Dicaprylyl Ether AND 0.500-2.300
Tri(Polyglyceryl-3/Lauryl) Hydrogenated Trilinoleate AND Cetyl PEG/PPG | ”
Iron Oxides AND Dicaprylyl Carbonate AND Dicaprylyl Ether AND 0.300-0.900
Tri(Polyglyceryl-3/Lauryl) Hydrogenated Trilinoleate AND Cetyl PEG/PPG | ’
Iron Oxides AND Dicaprylyl Carbonate AND Dicaprylyl Ether AND 0.100-0.600
Tri(Polyglyceryl-3/Lauryl) Hydrogenated Trilinoleate AND Cetyl PEG/PPG | °
Titanium Dioxide AND Triethoxycaprylylsilane 6.000-10.000
Zinc Oxide [nano] AND Triethoxycaprylylsilane 2.000-8.000 2.000-6.000
Octrooi (aanvraag): 2037617 48
Isododecane 2.000-6.000
Aluminum Starch Octenylsuccinate 2.00-6.000
Stearalkonium Bentonite 0.500-2.000
Mixture of Table 7 0.500-1.500
Mixture of Table 5 10.000-15.000
Mixture of Table 4 32.000-39.00 2,3-Butanediol AND Water 0.500-3.500 0.100-0.400
Glycerin 1.000-3.500
Alpha-Glucan Oligosaccharide 0.150-0.350
Sodium Hyaluronate 0.050-0.200
Dimethylmethoxy Chromanol 0.002-0.008
Vitamin E Acetate 0.300-0.800
Caprylic/Capric Triglyceride AND Rosa Damascena Flower Extract 0.300-0.800 0.500-3.000
Propanediol AND Glycerin AND Nelumbo Nucifera Flower Extract AND 0.500-3.000
Nymphaea Caerulea Flower Extract
[000155] Table 7
INCI Name
Propylene Carbonate 60-75
CHLORPHENESIN 15-25
Water Purified, USP, PhEur, JP, JSCI
Example 7: Setting Spay Formulation including Nelupre
[000156] A setting spray formulation including Nelupure can include the components shown in Table 8.
[000157] Table 8:
INCI Name Mass (%)
Alcohol Denat. and water 10-30
Octrooi (aanvraag): 2037617 49
Polysorbate 20 0.20-0.70
Polyurethane-14 and AMP-Acrylates | 5-9
Propanediol and glycerin and nymphaea | 1-4 carulea flower extract and nelumbo nucifera flower extract
Glycerine and water and sodium PCA and | 0.5-1.5 urea and treahalose and hexylene glycol and polyquaternium-51 and triacetin and caprylyl glycol
Hamamelis virginiana (witch hazel) water | 0.5-1.5 re
Glycerin and backhousta citriodora leaf | 0.20-0.50 eme Cm
[000158] Example 8: Testing for sebum control and heat response of cosmetic compositions including Nelupure
[000159] Various properties of a cosmetic composition including Nelupure as a component can be evaluated according to the following 28 day protocol. Any composition mentioned in this disclosure can be evaluated using the following protocol or any composition include 2 wt% or 4 wt% Nelupure can be analyzed using the following protocol.
[000160] According to the aforementioned protocol a participant will wash their face the evening before the protocol is begun. On the first day of the protocol, the participant will not wash their face. Baseline measurements using any one of more of a sebumeter, sebufix,
Octrooi (aanvraag): 2037617 50 colorface skin quality analysis, and porophyrins are established. The product is applied and measurements using any one of more of a sebumeter, sebufix, colorface skin quality analysis, and porophyrins may be taken at 1 hour, 4 hours, and 6 hours. The participant then applies a foundation product and takes a picture of their face with the foundation product applied before going to the sauna for 15-30 minutes at an elevated (relative to room temperature) temperature.
After sauna exposure the participant takes another picture of their face (with foundation product still applied). Over days 1-3 the product is applied twice daily.
[000161] On day 4, the participant will not wash their face the night before. Baseline measurements using any one of more of a sebumeter, sebufix, colorface skin quality analysis, and porophyrins are established. The product is applied and measurements using any one of more of a sebumeter, sebufix, colorface skin quality analysis, and porophyrins may be taken at 1 hour, 4 hours, and 6 hours. The participant then applies a foundation product and takes a picture of their face with the foundation product applied before going to the sauna for 15-30 minutes at an elevated (relative to room temperature) temperature. After sauna exposure the participant takes another picture of their face (with foundation product still applied).
[000162] On day 14, the participant will not wash their face the night before. Baseline measurements using any one of more of a sebumeter, sebufix, colorface skin quality analysis, and porophyrins are established. The product is applied and measurements using any one of more of a sebumeter, sebufix, colorface skin quality analysis, and porophyrins may be taken at 1 hour, 4 hours, and 6 hours. The participant then applies a foundation product and takes a picture of their face with the foundation product applied before going to the sauna for 15- 30minutes at an elevated (relative to room temperature) temperature. After sauna exposure the participant takes another picture of their face (with foundation product still applied).
[000163] On day 21, the participant will not wash their face the night before. Baseline measurements using any one of more of a sebumeter, sebufix, colorface skin quality analysis, and porophyrins are established. The product is applied and measurements using any one of more of a sebumeter, sebufix, colorface skin quality analysis, and porophyrins may betaken at 1 hour, 4 hours, and 6 hours. The participant then applies a foundation product and takes a picture of their face with the foundation product applied before going to the sauna for 15- 30minutes at an elevated (relative to room temperature) temperature. After sauna exposure the participant takes another picture of their face (with foundation product still applied).
Octrooi (aanvraag): 2037617 51
[000164] On day 28, the participant will not wash their face the night before. Baseline measurements using any one of more of a sebumeter, sebufix, colorface skin quality analysis, and porophyrins are established. The product is applied and measurements using any one of more of a sebumeter, sebufix, colorface skin quality analysis, and porophyrins are taken at 1 hour, 4 hours, and 6 hours. The participant then goes to the sauna for 30 minutes.
[009165] The terms and expressions that have been employed are used as terms of description and not of limitation, and there is no intention in the use of such terms and expressions of excluding any equivalents of the features shown and described or portions thereof, but it is recognized that various modifications are possible within the scope of the aspects of the present disclosure. Thus, it should be understood that although the present disclosure specifically disclosed by specific features, modification and variation of the concepts herein disclosed may be resorted to by those of ordinary skill in the art, and that such modifications and variations are considered to be within the scope of embodiments of the description.
[000166] Exemplary Aspects.
[000167] The following exemplary aspects are provided, the numbering of which is not to be construed as designating levels of importance:
[000168] In one aspect, a method of increasing the duration of use of a topical cosmetic composition, the method comprising applying the cosmetic composition to a user followed by applying the topical cosmetic composition to the cosmetic composition.
[000169] In one aspect, the extract solution is assessed for effectiveness as an acetylcholine inhibitor {000170} In one aspect, silica particles pre-loaded with the extract solution are used to absorb sebum and release the extract solution on sebum absorption
[000171] In one aspect, utilization of a nymphaea coerulea flower extract and nelumbo nucifera flower extract in combination with a clinically -effective amount of quercetin present to yield both antimicrobial and acetylcholine inhibitory effects.
[000172] In one aspect, increased color stability is seen as compared to a composition with an equivalent colorant load lacking the extract.
[000173] In one aspect composition has good color stability even when wetted with sweat and sebum. Color stability is suitable quantitatively measured by lack of shade change, which
Octrooi (aanvraag): 2037617 52 can be measured by color computer (SpectraFlash 600 Plus; Datacolor International Company) as delta E value of the colorimetric data before and after silicone oil was applied to the composition and wetted until max point of oil absorption. Hunter L-a-b color system 1s used for such colorimetric measurement.
[000174] In one aspect, the extract is utilized in a color cosmetic or skincare setting spray.
[000175] In one aspect, the use of the extract for a time and at a concentration sufficient to yield an anti-inflammatory effect when applied repeatedly to the skin.
[000176] In one aspect, the use of the extract in a topical composition that reduces pore size when applied for a time and at a concentration sufficient.
[000177] In one aspect, the use of the extract in a topical composition that yields better subsequent adherence of cosmetic formulations via decreasing skin sebum presence pre- cosmetic formula application.
[000178] In one aspect, the extract is incorporated into a powder form.
[000179] In one aspect, a cosmetic primer composition comprising a effective amount of an acetylcholine release inhibitor for reducing skin inflammation and / or pore size prior to applying a color cosmetic composition.
[000180] In one embodiment, a method of treating skin with an extract solution comprising: nymphaea coerulea flower extract; and nelumbo nucifera flower extract, wherein the effectiveness of the component is determined by an assay for determining the levels of sebum production, sebocyte leptin cell surface downregulation and/or acetylcholine release inhibition in a sample that has been contacted with the extract or a composition including the extract.
[000181] In one embodiment, A method comprising: (1) applying a sebum reducing composition comprising a topically acceptable vehicle and a sufficient amount of a sebum reducing agent to skin, followed by;(2) applying a cosmetic colorant composition comprising a colorant to the same skin, where the sequential application of the sebum reducing composition and the cosmetic colorant composition results in increased wear of the cosmetic colorant composition on the skin.
[000182] In one embodiment, The method .wherein the sebum reducing agent is an extract solution comprising nymphaea coerulea flower extract; and nelumbo nucifera flower extract.
Octrooi (aanvraag): 2037617 53
[000183] In one embodiment, A composition comprising silica particles loaded with extract solution comprising nymphaea coerulea flower extract; and nelumbo nucifera flower extract; wherein, upon application of the silica particles to a substrate containing sebum, the silica particles are capable of releasing the extract and preferentially absorbing the sebum.
[000184] In one embodiment, wherein the released extract decreased the amount of sebum produced by the substrate by at least 10% after 8 hours compared to an identical substrate that has not come into contact with the extract.
[000185] In one embodiment, The composition of any of the preceding embodiments further comprising quercetin or another suitable antimicrobial material.
[000186] In one embodiment, A color cosmetic composition comprising an extract solution comprising nymphaea coerulea flower extract; and nelumbo nucifera flower extract;wherein the color cosmetic composition exhibits improved color stability on contact with a sebum solution as compared to an otherwise identical color cosmetic composition lacking the extract solution.
[000187] In one embodiment, A method, wherein the sebum reducing composition is in the form of a spray.
[000188] In one embodiment, A method, wherein the skin is treated for a duration; frequency and/or with sufficient concentration of the extract to yield a decrease in expression of inflammatory biomarkers by the treated skin.
[006189] In one embodiment, A method, wherein the skin is treated for a duration; frequency and/or with sufficient concentration of the extract to yield a decrease in median pore size of the treated skin.
[000190] In one embodiment, A method, wherein the composition comprising the extract 18 in powder form.
[000191] In one embodiment, A cosmetic composition comprising:
[000192] Water in a range of about 55-65 wt%;
[000193] Aloe Barbadensis Leaf Juicein a range of about 0.050-0.150 wt%;
[000194] Sodium Hyaluronate in a range of about 0.050-0.150 wt%:
[000195] Glycerin in a range of about 3.000-10.000 wi;
[000196] Butylene Glycol in a range of about 2.000-7.000 wt%;
[000197] Chlorphenesin in a range of about 0.0100-0.350 wt%;
Octrooi (aanvraag): 2037617 54
[000198] 3-O-Ethyl Ascorbic Acid in a range of about 0.050-0.150 wt%:;
[000199] Arginine in a range of about 0.035-0.090 wt%:
[000200] PVP in a range of about 1.500-5.500 wt%:
[000201] Glycerin in a range of about 5.000-9.000 wt%;
[000202] Ammonium Acryloyldimethyltaurate/Beheneth-25 Methacrylate Crosspolymer in a range of about 1.000-1. 500 wt%;
[000203] 1,2-Hexanediol and Caprylyl Glycol in a range of about 0.500-1.500 wt%:;
[000204] Propanediol and Glycerin and Nelumbo Nucifera Flower Extract and
Nymphaea Caerulea Flower Extract in a range of about 1.000-3.000 wt;
[000205] Water and Blue 1 in a range of about 0.100-0.300 wt%; and
[000206] Polysilicone-11 and Water AND Laureth-12 and Ethylhexylglycerin in a range of about 8.000-12.000.
[000207] A cosmetic composition comprising:
[000208] Water in a range of about 65.000-75.000 wt%; 1000209] Sodium Hyaluronate in a range of about 0.0500-0.1500 wt%;
[000210] Glycerin in a range of about 10.000-18.000 wt%;
[000211] Ammonium Acryloyldimethyltaurate/Beheneth-25 Methacrylate Crosspolymer in a range of about 0.150-0.250 wt%; 1000212] Cetearyl Alcohol AND Cetearyl Glucoside in a range of about 1.000-1.250 wt%;
[000213] Octyldodecyl Neopentanoate in a range of about 1.000-2.000 wt%:
[000214] Pentaerythrityl Tetraethylhexanoate in a range of about 1.000-3.000 wt%:;
[000215] Butylene Glycol in a range of about 2.000-7.000 wt%:;
[000216] Sodium Polyacrylate Starch 1 a range of about 0.050-0.110 wt%;
[000217] Dimethicone in a range of about 0.250-0.750 wt%:
[000218] Propanediol AND Glycerin AND Nelumbo Nucifera Flower Extract and
Nymphaea Caerulea Flower Extract in a range of about 1.000-3.000 wt;
[000219] Bisabolol in a range of about 0.050-0.150 wt%:
[000220] Water and Vaccinium Macrocarpon (Cranberry) Fruit Extract and 1,2-
Hexanediol and Caprylyl Glycol in a range of about 0.050-0.150 wt%;
[000221] 1,2-Hexanediol and Caprylyl Glycol in a range of about 0.050-1.500 wt; and
Octrooi (aanvraag): 2037617 55
[000222] Polysorbate 8 in a range of about 0.050-1.500 wt%.
[000223] A cosmetic composition comprising:
[000224] Titanium Dioxide AND Triethoxycaprylylsilane in a range of about 1.000-3.000 wit%;
[000225] Tocopheryl Acetate in a range of about 0.300-0.700 wig;
[000226] Isododecane in a range of about 10.000-15.000 wt%;
[000227] Dicaprylyl Carbonate AND Tocopherol in a range of about 2.000-5.000 wt®%;
[000228] Chromium Oxide Greens in a range of about 0.500-1.000 wt%:Iron Oxides in a range of about 0.020-0.060 wt%;
[000229] Triethyl Citrate in a range of about 0.700-1.100 wt%;
[0002386] Water in a range of about 0.050-0.200 wie; Chlorphenesin in a range of about 6.100-0.300 wt%;
[000231] Stearalkonium Bentonite in a range of about 1.000-3.000 wt%;
[000232] In one embodiment, A method of treating skin with a component effective for functioning in a cosmetic composition , wherein the effectiveness of the component is determined by an assay for determining the levels of sebum production, sebocyte leptin cell surface downregulation, and/or acetylcholine release inhibition in a sample that has been contacted with the extract or a composition including the extract. 1000233] In one embodiment, A method of inhibiting acetylcholine release, the method comprising contacting the cosmetic composition with a keratinous tissue.
[000234] In one embodiment, A method of treating wrinkles and/or fine lines of the skin, comprising administering to a subject in need of treatment a composition comprising one or more acetylcholine release inhibitors derived from a combination of the nymphaea coerulea and nelumbo nucifera flower extracts in an amount effective to prevent, ameliorate, reduce, and/or eliminate wrinkles or fine lines.
[000235] In one embodiment, The method wherein the composition is applied to the face and the acetylcholine release inhibitor inhibits acetylcholine release at a neuromuscular junction of a facial expression muscle, thereby relaxing the muscle associated with marionette lines, wrinkles on the forehead, or wrinkles between the brows.
[000236] In one embodiment, A method of treating, preventing, reducing, ameliorating, and/or eliminating, wrinkles, fine lines, or deep frown lines in the skin, comprising: providing
Octrooi (aanvraag): 2037617 56 a composition comprising acetylcholine release inhibitor to an Individual in need thereof, in an amount effective to block or reduce acetylcholine release at a neuromuscular junction (NMJ), wherein said inhibition or reduction of acetylcholine release at the neuromuscular junction (NMJ) concomitantly inhibits or reduces contraction of muscle tissue, thereby treating, preventing, reducing, ameliorating, and/or eliminating wrinkling, fine lines, or deep frown lines in the skin.
[000237] In one embodiment, A method of reducing the likelihood of allergy elicitation in a subject comprising applying the extract solution as a pretreatement prior to use of a fragrance oil so as to decrease the likeliohood and/or severity ofallergy elicitation.
[000238] In one embodiment, A method of reducing shaving related irritation comprising applying a sufficient amount of the active agent to the skin to appreciably reduce pore size before shaving.
[000239] In one embodiment, A sunscreen formulation comprising a combination of lotus flower extracts where the sunscreen formulation demonstrates decreased sebum- associated loss of remanence.
[000240] In one embodiment, A composition comprising a liposome encapsulated combination of lotus flower extracts.
[000241] In one embodiment, A method of treatment comprising applying a composition comprising a lotus flower extract mixture to the skin so as to reduce skin sebum production prior to applying a color cosmetic to the skin.
[000242] In one embodiment, A method of treatment comprising utilization of an effective amount lotus flower extract in combination with an effective amount of quercetin to yield both anti-microbial and acetylcholine release inhibition effects.
[000243] In one embodiment, A method of treatment comprising utilization of a nymphaea coerulea flower extract and nelumbo nucifera flower extract to reduce the severity and/or duration of erythema.
[000244] In one embodiment, A method of treatment comprising in one embodiment, use of the extract for treating hot flashes and excessive sweating (hyperhidrosis) related to perimenopausal and menopausal symptoms.
Octrooi (aanvraag): 2037617 57 1000245] In one embodiment, A method of treatment comprising in one embodiment, the extract is utilized for a duration and at a concentration sufficient to provide a skin firming benefit.
[000246] In one embodiment, A method of treatment comprising in one embodiment, the extract is utilized in a color cosmetic or skincare setting spray.
[000247] In one embodiment, A method of treatment comprising in one embodiment, the extract is utilized in a composition that when incorporating the extract at a sufficient concentration / used for a suitable duration of time yields a decrease in foot odor.
[000248] In one embodiment, A method of treatment comprising applying a sufficient amount of the extract blend to treat, prevent, or ameliorate the effects of the presence of
Malassezia yeasts on the scalp.
[000249] In one embodiment, A method of treatment comprising in one embodiment, the use of a sufficient amount of the extract to inhibit upregulation of sebum gland lipid synthesis and thereby decrease the incidence and severity of acne.