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.2024 Jun 19;16(6):830.
doi: 10.3390/pharmaceutics16060830.

The Assessment of Physicochemical and Antimicrobial Properties of Hydrophilic Gels Containing Tetracycline Hydrochloride and Various Concentrations of Ethanol

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The Assessment of Physicochemical and Antimicrobial Properties of Hydrophilic Gels Containing Tetracycline Hydrochloride and Various Concentrations of Ethanol

Agnieszka Kostrzębska et al. Pharmaceutics..

Abstract

The high prevalence of acne, which affects nearly 85% of adolescents and young adults, underscores the importance of exploring new therapeutic solutions. The aim of the present study was to design a stable hydrogel formulation containing tetracycline hydrochloride (TC) in the presence of ethanol at various concentration levels. The antibiotic stability was assessed over a period of 84 days using the HPLC method. The rheological properties of the formulations and their microbiological activity were also evaluated. Hydrogels without ethanol and those containing 5% and 25% alcohol showed similar rheological properties and high stability of the antibiotic throughout the observation period. The formulation with the highest ethanol content of 50% differed significantly from the others in terms of rheological properties. Although the flow and viscosity curves were like those of the other formulations, the viscosity values were significantly lower. The stability of tetracycline in this formulation was also significantly lower, and by the 84th day of observation, the concentration of the drug had decreased to almost 45% of its initial content. The formulations containing the highest concentration of ethanol displayed the highest activity against the biofilm of the acne-causing agent,Cutibacterium acnes. The study demonstrated the possibility of developing stable and antimicrobial effective hydrogel formulations with tetracycline and ethanol as a substance enhancing drug penetration into the hair follicles.

Keywords: C. acnes; HPLC; acne; ethanol; hydrogel; tetracycline hydrochloride.

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Conflict of interest statement

The authors declare no conflicts of interest.

Figures

Figure 1
Figure 1
Concentration of TC over 84 days, in formulations without ethanol (1) and containing 5% (2), 25% (3), and 50% (4) of ethanol.
Figure 2
Figure 2
Concentration of 4-ETC over 84 days, in formulations without ethanol (1) and containing 5% (2), 25% (3), and 50% (4) of ethanol.
Figure 3
Figure 3
Dynamic viscosity curves for formulations in formulations without ethanol (1) and containing 5% (2), 25% (3), and 50% (4) of ethanol, at 20 °C (a) and 37 °C (b).
Figure 4
Figure 4
Changes in viscosity values of preparations without ethanol (1) and containing 5% (2), 25% (3), and 50% (4) of ethanol, at varying temperatures increasing from 20 °C to 40 °C.
Figure 5
Figure 5
The comparison ofC. acnes biofilm biomass exposed to the formulations A1–4, B1–4. Images: the positive control (image C+) isC. acnes biofilm biomass that is not exposed to the presence of any formulation, while “OCT” is theC. acnes biofilm biomass exposed to the topical antimicrobial agent, referred to as octenidine dihydrochloride, applied herein in the role of the experiment’s usability control (image “OCT”). Images “A4” and “B4” show CV-dyed biofilm treated with A4 or B4 formulation, respectively. The asterisks are used to show the statistical significance between the differences in biofilm biomass. (“**” indicates a significance level of 0.01, “****” indicates a significance level of 0.0001). ANOVA with Tukey’ post hoc multiple comparison test.
Figure 6
Figure 6
Sub-panel (A): images (three repeats) of non-exposedC. acnes biofilm (control of growth). Sub-panel (B): images (three repeats) ofC. acnes exposed to formulation A4. Sub-panel (C): images (three repeats) ofC. acnes exposed to formulation B4. Red bar in the lower right corner of each image represents 20 µm.
Figure 7
Figure 7
The relative number of live (L, green dots) or dead (D, red dots) biofilm-formingC. acnes cells exposed to A4 or B4 formulations, compared to the non-exposedC. acnes biofilm (C+). [A.U.]—arbitrary units. (“*” indicates a significance level of 0.01, ANOVA test).
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References

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