Construction and characterization of intestinal oligopeptide transporter PepT1-targeted polymeric micelles for enhanced intestinal absorption of poorly water-soluble agents

作     者：Yao Jin Qi Liu Chuhang Zhou Shidi Han Yuanhang Zhou Xinping Hu Leqi Wang Yan Liu 靳尧;刘琦;周楚杭;韩诗迪;周远航;胡新平;王乐淇;刘艳

作者机构：Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery Systems School of Pharmaceutical Sciences Peking University Health Science Center Beijing 100191 China 

基　　金：National Natural Science Foundation of China(Grant No.81673366) the National Key Science Research Program of China(973 Program,Grant No.2015CB932100) 

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

年 卷 期：2019年第28卷第8期

页      码：561-570页

摘      要：To overcome the main barrier of intestinal epithelium for the oral absorption of poorly water-soluble drugs and further improve their oral absorption, Gly-Sar, the substrate of the oligopeptide transporter PepT1 widely distributed in the small intestine,conjugated poly(ethylene glycol)-block-poly(D,L-lactide)(Gly-Sar-PEG-b-PLA) was designed and synthesized, and Pep T1-targeted polymeric micelles were prepared and characterized. The structure of the synthesized Gly-Sar-PEG-b-PLA was confirmed by use of TLC and 1 H-NMR. The average molecular weight measured by GPC was 5954 g/mol with PDI of 1.34. The DiI-loaded polymeric micelles from Gly-Sar-PEG-b-PLA with drug loading content of 0.076% were characterized to exhibit 40.36 nm in diameter with PDI of 0.294, and well-defined spherical shape observed by TEM. Furthermore, the PepT1-targeted polymeric micelles profoundly enhanced intestinal absorption of poorly water-soluble drug. Therefore, the designed PepT1-targeted polymeric micelles might have a promising potential for oral delivery of water-insoluble drugs.

主 题 词：Intestinal transporter Oligopeptide transporter PepT1 Gly-Sar Polymeric micelles Oral administration 

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.2019.08.054

馆 藏 号：203742955...