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In vivo human skin penetration of (–)-epigallocatechin-3-gallate from topical formulations

机译:局部制剂对(–)-epigallocatechin-3-gallate的体内人类皮肤渗透

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摘要

The aim of the study was to examine the effect of topical vehicles on the in vivo human stratum corneum penetration of the antioxidant and skin photoprotective agent (–)-epigallocatechin-3-gallate (EGCG). Model oil-in-water (o/w) emulsion and gel formulations containing 1 % (m/m) EGCG were prepared and subjected to photodegradation studies in order to select excipients that minimize the light instability of EGCG. The optimized emulsion and gel were applied to human volunteers and the EGCG percutaneous permeation was evaluated in vivo by the tape-stripping technique. No significant differences in the percentage of the applied EGCG dose diffused into the stratum corneum were observed between the o/w emulsion (36.1 ± 7.5 %) and gel (35.5 ± 8.1 %) preparations. However, the amount of EGCG permeated into the deeper region of human stratum corneum was significantly larger for the o/w emulsion compared to the gel. Therefore, the emulsion represents a suitable vehicle for topical delivery of EGCG.
机译:该研究的目的是研究局部用载体对体内抗氧化剂和皮肤光保护剂(-)-epigallocatechin-3-gallate(EGCG)的角质层渗透的影响。制备了包含1%(m / m)EGCG的模型水包油(o / w)乳液和凝胶制剂,并对它们进行光降解研究,以选择能使EGCG的光不稳定性最小的赋形剂。将优化的乳剂和凝胶应用于人类志愿者,并通过胶带剥离技术在体内评估EGCG经皮渗透。在o / w乳剂(36.1±7.5%)和凝胶(35.5±8.1%)制剂之间未观察到扩散到角质层的EGCG剂量百分比的显着差异。然而,与凝胶相比,对于o / w乳液,渗透到人角质层较深区域的EGCG的量明显更大。因此,乳液代表了用于EGCG局部递送的合适载体。

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