Abstract

Objectives: Caffeine has many functions including its use in the field of cosmetics. Nonetheless, the percutaneous absorption of caffeine is very low(9%), and the penetration of a substance such as caffeine in the skin is not desirable. Ethosomes and desmosomes are lipid vesicles created by themodification of liposomes containing phospholipids and ethanol or dimethyl sulfoxide (DMSO) as the penetration enhancer. The purpose of this studywas to compare the effectiveness of ethosomes and desmosomes as vesicles in increasing the penetration of caffeine.Methods: Ethosomes and desmosomes were prepared using phosphatidylcholine, ethanol/DMSO, and caffeine. Phosphatidylcholine was used in theform of phospholipon 90 g that was obtained from soybeans. Observations were done including the characteristic of ethosomes and desmosomes,organoleptic observation, homogeneity observation, and in vitro penetration test using Franz diffusion cell method.Results: The cumulative penetration of caffeine ethosome gel is 3316.46±218.51 μg/cm2, with flux 249.45±30.06 μg·cm−2·hr−1, and 62.35±4.52%. Thecumulative penetration of the desmosome gel is 2954.95±222.87 μg/cm2 with flux 381.68±34.91 μg·cm−2·hr−1 and 53.4±3.65%.Conclusions: It can be concluded that ethosome is more effective than desmosome in increasing the penetration of caffeine.

Highlights

  • Caffeine is an alkaloid derivate of methylxanthine and has nitrogen atoms with a two-ring or two-cycle structure [1]

  • Phosphatidylcholine was used in the form of phospholipon 90 g that was obtained from soybeans

  • It can be concluded that ethosome is more effective than desmosome in increasing the penetration of caffeine

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Summary

Introduction

Caffeine is an alkaloid derivate of methylxanthine and has nitrogen atoms with a two-ring or two-cycle structure [1]. Caffeine is mostly consumed in beverages and is used in medicines and cosmetics [2]. It is used as an active substance in anti-cellulite products because it can prevent fat accumulation [3]. According to the previous study, a less amount of caffeine is absorbed (only 9%) through the cutaneous layer [4]. The stratum corneum has a lamellar lipid layer and corneocytes that play a role in preventing the penetration of other substances, including drugs into the body [5]. It is not desirable that caffeine penetrates through the skin because it has a hydrophilic material with log p=−0.072. The objective of this study was to prepare caffeine ethosomes and desmosomes

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