Fabrication of deoxycholic acid-modified polymeric micelles and their transmembrane transport

作     者：Qi Liu Leqi Wang Xinping Hu Chuhang Zhou Yingwei Tang Yining Ma Xiaoxiao Wang Yan Liu 刘琦;王乐淇;胡新平;周楚杭;唐颖蔚;马翊宁;王骁潇;刘艳

作者机构：Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery SystemsSchool of Pharmaceutical SciencesPeking University Health Science CenterBeijing 100191China 

基　　金：The National Natural Science Foundation of China(Grant No.81673366) 

出 版 物：《Journal of Chinese Pharmaceutical Sciences》 (中国药学（英文版）)

年 卷 期：2021年第30卷第1期

页      码：17-26页

摘      要：Oral administration is the best way for the most patients due to the good compliance,and intestinal epithelium is the main barrier of oral drug *** order to overcome the small intestine epithelial barrier to orally deliver water-insoluble drugs,deoxycholic acid(DA),a substrate of the intestinal bile acid transporters,conjugated poly(2-ethyl-2-oxazoline)-poly(D,L-lactide)(DA-PEOz-PLA)was designed and synthesized,and deoxycholic acid-modified polymeric micelles composed of DA-PEOz-PLA and mPEG-PLA were fabricated to encapsulate model drug coumarin 6(C6)based on intestinal bile acid *** structure of DA-PEOz-PLA was confirmed using 1 H NMR and TLC,and the molecular weight measured by GPC was 10034 g/mol with a PDI of *** C6-loaded polymeric micelles with drug loading content of 0.085%were characterized to have 40.11 nm in diameter and uniform spherical morphology observed by ***,the deoxycholic acid-modified polymeric micelles were demonstrated to further enhance the transmembrane transport *** mechanic study evidenced that anchorage of deoxycholic acid onto the micelles surface enriched their transcellular transport ***,the designed deoxycholic acid-modified polymeric micelles might have a promising potential for oral delivery of water-insoluble drugs.

主 题 词：Deoxycholic acid Intestinal bile acid transporter Polymeric micelles Oral nano drug delivery system Transmembrane transport 

学科分类：100702[100702] 1007[医学-药学类] 1006[医学-中西医结合类] 100602[100602] 10[医学] 

核心收录：

D　O　I：10.5246/jcps.2021.01.002

馆 藏 号：203101974...