Preparation and characterization of intestinal transporter-targeted polymeric micelles

作     者：Chuyu He Yao Jin Yunqiang Deng Yang Zou Shidi Han Chuhang Zhou Yuanhang Zhou Xinru Li Yanxia Zhou Yan Liu 何楚瑜;靳尧;邓运强;邹洋;韩诗迪;周楚杭;周远航;李馨儒;周艳霞;刘艳

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

基　　金：The 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：2018年第27卷第7期

页      码：490-497页

摘      要：The intestinal epithelium is the main barrier to the oral delivery of poorly water-soluble drugs. Based on the specific transporters expressed on the apical membrane of the intestinal epithelium, novel polymer micelles targeting to the organic cation transporter 2（OCTN2） were constructed by combining carnitine conjugated poly（2-ethyl-2-oxazoline）-poly（D,L-lactide）（Car-PEOz-PLA） with monomethoxy poly（ethylene glycol）-poly（D,L-lactide）（mP EG-PLA）. The structure of the synthesized Car-PEOz-PLA was confirmed by -1H NMR, TLC and ammonium reineckate precipitation reaction, and the number-average molecular weight determined by GPC was 7260 g/mol with a low PDI of 1.44. Coumarin 6-loaded carnitine modified polymeric micelles prepared by film hydration method were characterized to have a nano-scaled size of about 31 nm in diameter, uniform spherical morphology, high drug loading content of 0.098%±0.03% and encapsulation efficiency of 92.67%±2.80%. Moreover, the carnitine-modified micelles exhibited the similar in vitro release behavior in SGF and SIF, and evidently enhanced intestinal absorption of poorly water-soluble agent. Therefore, the designed OCTN2-targeted micelles might have a promising potential for oral delivery of poorly water-soluble drugs.

主 题 词：Carnitine Organic cation transporter 2 (OCTN2) Polymeric micelles In vitro release Intestinal absorption 

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.2018.07.050

馆 藏 号：203304987...