首页 | 本学科首页   官方微博 | 高级检索  
   检索      


Carboxylated phytosterol derivative-introduced liposomes for skin environment-responsive transdermal drug delivery system
Authors:Naoko Yamazaki  Satoshi Yamakawa  Takumi Sugimoto  Yuta Yoshizaki  Ryoma Teranishi  Takaaki Hayashi
Institution:1. Research Institute, Fancl Corporation, Yokohama, Kanagawa, Japan;2. Department of Applied Chemistry, Graduate School of Engineering, Osaka Prefecture University, Osaka, Japan;3. Cosmetic Ingredients Laboratory, Nippon Fine Chemical Corporation, Takasago, Hyogo, Japan;4. Department of Applied Chemistry, Graduate School of Engineering, Osaka Prefecture University, Osaka, Japan
Abstract:Abstract

Transdermal drug delivery systems are a key technology for skin-related diseases and for cosmetics development. The delivery of active ingredients to an appropriate site or target cells can greatly improve the efficacy of medical and cosmetic agents. For this study, liposome-based transdermal delivery systems were developed using pH-responsive phytosterol derivatives as liposome components. Succinylated phytosterol (Suc-PS) and 2-carboxy-cyclohexane-1-carboxylated phytosterol (CHex-PS) were synthesized by esterification of hydroxy groups of phytosterol. Modification of phytosterol derivatives on 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC) liposomes was confirmed by negatively zeta potentials at alkaline pH and the change of zeta potentials with decreasing pH. In response to acidic pH and temperatures higher than body temperature, Suc-PS-containing and CHex-PS-containing liposomes exhibited content release at intracellular acidic compartments of the melanocytes at the basement membrane of the skin. Phytosterol-derivative-containing liposomes were taken up by murine melanoma-derived B16-F10 cells. These liposomes delivered their contents into endosomes and cytosol of B16-F10 cells. Furthermore, phytosterol-derivative-containing liposomes penetrated the 3?D skin models and reached the basement membrane. Results show that pH-responsive phytosterol-derivative-containing DMPC liposomes are promising for use in transdermal medical or cosmetic agent delivery to melanocytes.
Keywords:Liposome  phytosterol  pH-sensitive  transdermal delivery  cosmetics
设为首页 | 免责声明 | 关于勤云 | 加入收藏

Copyright©北京勤云科技发展有限公司  京ICP备09084417号