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利用反胶束法调节分配系数以增强表没食子儿茶素没食子酸酯的皮肤渗透性。

Enhancing skin penetration of epigallocatechin gallate by modifying partition coefficient using reverse micelle method.

作者信息

Rosita Noorma, Meitasari Vinta Arnike, Rianti Mirna Candra, Hariyadi Dewi Melani, Miatmoko Andang

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, Universitas Airlangga, Kampus C Mulyorejo, Surabaya 60115, Indonesia.

出版信息

Ther Deliv. 2019 Jul;10(7):409-417. doi: 10.4155/tde-2019-0015. Epub 2019 Jul 19.

Abstract

(-)-Epigallocatechin gallate (EGCG) has been reported as inducing apoptosis in cervical cancer. However, EGCG demonstrates low skin permeability. In order to develop topical delivery of EGCG, the partition coefficient, log P, was modified using a reverse micelle method. During this study, Tween 80 and Span 80 were added to EGCG at hydrophilic-lipophilic balance (HLB) values of 4.3, 6 and 8. The results showed that lowering the HLB value increases the log P value of EGCG and results in higher IC values in Henrietta Lacks (HeLa) cancer cells than that of EGCG. Surfactant-modified EGCG-HLB 6 produced faster and deeper skin penetration than EGCG. Modification of log P value using a combination of Tween 80 and Span 80 improved cytotoxicity and topical delivery of EGCG.

摘要

(-)-表没食子儿茶素没食子酸酯(EGCG)已被报道可诱导子宫颈癌细胞凋亡。然而,EGCG的皮肤渗透性较低。为了开发EGCG的局部给药方法,采用反胶束法对分配系数log P进行了修饰。在本研究中,将吐温80和司盘80以亲水亲油平衡(HLB)值4.3、6和8添加到EGCG中。结果表明,降低HLB值会增加EGCG的log P值,并导致其在海拉(HeLa)癌细胞中的IC值高于EGCG本身。表面活性剂修饰的EGCG-HLB 6比EGCG具有更快、更深的皮肤渗透效果。使用吐温80和司盘80组合修饰log P值可提高EGCG的细胞毒性和局部给药效果。

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