Abstract

Objective: Capsaicin is a bioactive compound with poor solubility in water. Transfersomes can increase the solubility and thus the penetration ofcapsaicin into the epidermis. Transfersomes also offer the advantage of being ultradeformable vesicles that are made using the thin layer hydrationmethod. The aim of this study is to determine the effect of the hydrophilicity of surfactants on the characterization and in vitro penetrative ability ofcapsaicin transfersomes in gels using non-ionic surfactants with different hydrophile-lipophile balances, namely, Span 80, Tween 80, and a mixtureof Span 80, and Tween 80.Methods: The best characterization result for transfersomes is the formula using Tween 80. The total cumulative amount of capsaicin penetratedfrom the transfersome gel using Tween 80 is 1663.89±1.58 mg/cm2, the percentage is 57.96±0.05%, and the flux is 166.38±0.15 μg/cm2.hr−1.Results: In terms of the transfersome gel using a mixture of Span 80 and Tween 80, the cumulative amount of capsaicin penetrated is1539.8±21.23 μg/cm2, the percentage is 54.47±0.75%, and the flux is 153.98±2.12 μg/cm2.hr−1. Finally, from the transfersome gel using Span 80, thecumulative amount of capsaicin penetrated is 1395.10±7.23 mg/cm2, the percentage is 50.80±0.26%, and the flux is 139.51±0.72 mg/cm2.hr−1.Conclusions: The best characteristics resulted from the transfersome formulation using Tween 80, which demonstrated the highest entrapmentefficiency calculation result, the smallest particle size, the best deformability index, and the highest penetration when compared to the other twoformulations.

Highlights

  • Transfersomes are artificial vesicles that are designed to mimic cell vesicles, and they are used as medicines or to courier genetic materials to cells [1]

  • The total cumulative amount of capsaicin penetrated from the transfersome gel using Tween 80 is 1663.89±1.58 mg/cm2, the percentage is 57.96±0.05%, and the flux is 166.38±0.15 μg/cm2.hr−1

  • In terms of the transfersome gel using a mixture of Span 80 and Tween 80, the cumulative amount of capsaicin penetrated is 1539.8±21.23 μg/cm2, the percentage is 54.47±0.75%, and the flux is 153.98±2.12 μg/cm2.hr−1

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Summary

Introduction

Transfersomes are artificial vesicles that are designed to mimic cell vesicles, and they are used as medicines or to courier genetic materials to cells [1]. Transfersomes are composed of a surfactant and a phospholipid. The surfactant, for example, Tween 80 and Span 80, provides flexibility to the transfersome [2]. Such flexibility will serve to minimize the risk of vesicle rupture on the skin as well as enabling the transfersome to penetrate into the epidermis [3]. The phospholipid could interact with the stratum corneum, improve the hydration of tissue, merge with lipids from the stratum corneum, and enhance penetration [4]. Tween and Span are both types of non-ionic surfactant that can penetrate quickly and reach deeper than the stratum corneum layer [5]

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