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Review
.2020 Jun 27;25(13):2959.
doi: 10.3390/molecules25132959.

Phospholipid Vesicles for Dermal/Transdermal and Nasal Administration of Active Molecules: The Effect of Surfactants and Alcohols on the Fluidity of Their Lipid Bilayers and Penetration Enhancement Properties

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Review

Phospholipid Vesicles for Dermal/Transdermal and Nasal Administration of Active Molecules: The Effect of Surfactants and Alcohols on the Fluidity of Their Lipid Bilayers and Penetration Enhancement Properties

Hiba Natsheh et al. Molecules..

Abstract

This is a comprehensive review on the use of phospholipid nanovesicles for dermal/transdermal and nasal drug administration. Phospholipid-based vesicular carriers have been widely investigated for enhanced drug delivery via dermal/transdermal routes. Classic phospholipid vesicles, liposomes, do not penetrate the deep layers of the skin, but remain confined to the upper stratum corneum. The literature describes several approaches with the aim of altering the properties of these vesicles to improve their penetration properties. Transfersomes and ethosomes are the most investigated penetration-enhancing phospholipid nanovesicles, obtained by the incorporation of surfactant edge activators and high concentrations of ethanol, respectively. These two types of vesicles differ in terms of their structure, characteristics, mechanism of action and mode of application on the skin. Edge activators contribute to the deformability and elasticity of transfersomes, enabling them to penetrate through pores much smaller than their own size. The ethanol high concentration in ethosomes generates a soft vesicle by fluidizing the phospholipid bilayers, allowing the vesicle to penetrate deeper into the skin. Glycerosomes and transethosomes, phospholipid vesicles containing glycerol or a mixture of ethanol and edge activators, respectively, are also covered. This review discusses the effects of edge activators, ethanol and glycerol on the phospholipid vesicle, emphasizing the differences between a soft and an elastic nanovesicle, and presents their different preparation methods. To date, these differences have not been comparatively discussed. The review presents a large number of active molecules incorporated in these carriers and investigated in vitro, in vivo or in clinical human tests.

Keywords: dermal/transdermal; edge activator; ethanol; ethosomes; glycerosomes; nasal; penetration enhancement; phospholipid nanovesicle; skin; transethosomes; transfersomes.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Transmission electron (TE) micrographs of multilamellar to the core minoxidil ethosomes. Reproduced from Reference [24] with permission.
Figure 2
Figure 2
TE micrograph of transfersomes showing hollow nanovesicles. Reproduced from Reference [54] with permission.
Figure 3
Figure 3
TE micrographs of diclofenac sodium loaded in PL90H-based glycerosomes containing 20% glycerol, scale bar 200 nm. Reproduced from Reference [40] with permission.
Figure 4
Figure 4
Proposed model for the mechanism of skin delivery from ethosomal systems containing phospholipids, ethanol and the drug. Reproduced from Reference [4] with permission.
Figure 5
Figure 5
Proposed mechanism of skin penetration by transfersomes. Top: computer simulated distribution of more (red, e.g., a surfactant) or less (blue, e.g., a phospholipid) water soluble molecules with hydrophobic (yellow) chains arranged in a mixed amphipathic spherical bilayer as a function of predefined vesicle shape. Middle: a simulation of a highly deformable, infinitely permeable, non-destructible vesicle forced by a horizontal gradient into a pore with 0.5 smaller diameter. Bottom: an electromicrograph of elongated, deformable vesicles in an inter-corneocyte water-filled channel within the human stratum corneum after an application of a lipid preparation on its open surface. Reproduced from Reference [68] with permission.
Figure 6
Figure 6
Safety studies carried out with ethosomes. Reproduced from Reference [24] with permission.
Figure 7
Figure 7
TE micrographs showing the multilamellar structure of: (a) Soft vesicular nasal nanocarrier, ×110k, scale bar 200 nm. Reproduced from Reference [10] with permission. (b) Phospholipid magnesome ×135k, scale bar 100 nm. Reproduced from Reference [152] with permission.
Figure 8
Figure 8
Delivery of epidermal growth factor (EGF) to the brain; near infrared imaging (NIR) image of brain of mice treated with 1 mg/kg EGF IRDye® 800CW incorporated in phospholipid magnesome and in three control systems: water solution (WS), liposome (Lipo) and nonvesicular carrier (NV). Reproduced from Reference [152] with permission.
Figure 9
Figure 9
Transmission electron micrograph of chitosan composite transfersomes showing the outline and the core of spherical vesicles, ×20,000, scale bar 500 nm. Reproduced from Reference [156] with permission.
Figure 10
Figure 10
Mean clinical scores (mean ± SE) in EAE mice that received 6.7 mg/kg/days CBD alone or in combination with 6.7 mg/kg/day GA nasally from a nasal nanovesicular carrier (NDS) or subcutaneously, starting from the first day of the clinical manifestation of the disease. Reproduced from Reference [151] with permission.
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