Scalia Santo, Trotta Valentina, Bianchi Anna
Acta Pharm. 2014 Jun;64(2):257-65. doi: 10.2478/acph-2014-0017.
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.
本研究的目的是考察局部给药载体对抗氧化剂及皮肤光保护剂（-）-表没食子儿茶素-3-没食子酸酯（EGCG）在人体角质层的体内渗透作用。制备了含1%（m/m）EGCG的水包油（o/w）乳剂和凝胶制剂模型，并进行光降解研究，以选择能使EGCG光不稳定性降至最低的辅料。将优化后的乳剂和凝胶应用于人体志愿者，采用胶带剥离技术在体内评估EGCG的经皮渗透情况。在o/w乳剂（36.1±7.5%）和凝胶（35.5±8.1%）制剂之间，未观察到扩散进入角质层的EGCG给药剂量百分比有显著差异。然而，与凝胶相比，o/w乳剂渗透进入人体角质层较深区域的EGCG量显著更大。因此，乳剂是EGCG局部给药的合适载体。
