文献类型：期刊文章

作　　者：屈小又[1] 邹洋[1] 靳尧[1] 周远航[1] 王子琪[1] 何楚瑜[1] 邓运强[1] 李馨儒[1] 周艳霞[1] 刘艳[1]

机构地区：[1]北京大学医学部药学院分子药剂学与新释药系统北京市重点实验室,北京100191

出　　处：《Journal of Chinese Pharmaceutical Sciences》

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

年　　份：2017

卷　　号：26

期　　号：8

起止页码：582-588

语　　种：中文

收录情况：CAB、CAS、CSCD、CSCD2017_2018、DOAJ、EMBASE、IC、JST、SCOPUS、ZGKJHX、普通刊

摘　　要：To ensure the delivery of antitumor drugs to tumor site and quick release in tumor cells, we designed and prepared pH-sensitive polymeric micelles by combining cationic ring-opening polymerization of 2-ethyl-2-oxazoline （EOz） with vitamin E succinate （VES）, and then encapsulating paclitaxel （PTX） into the micelles self-assembled by poly（2-ethyl-2-oxazoline）-vitamin E succinate （PEOz-VES）. The structure of the synthesized PEOz-VES was confirmed by ^1H NMR spectrum, and the molecular weight measured by GPC was 1212 g/mol. The pKa of PEOz-VES with a low critical micelle concentration of （5.84±0.02） mg/L was determined to be 6.01. The PTX-loaded PEOz-VES polymeric micelles prepared by film hydration method were characterized to have a nanoscaled size of about 30 nm in diameter, a positive Zeta potential of 4.86 mV and uniform spherical morphology by TEM observation. The drug loading content and encapsulation efficiency were （2.63±0.16）% and （84.1±3.38）%, respectively. The in vitro release behavior of PTX from PEOz-VES micelles in PBS displayed pH-dependent pattern and was gradually accelerated with decrease of pH value, implying that the micelles could distinguish endo/lysosomal pH and tumor extracellular pH from physiological pH by accelerating drug release. Therefore, the designed PEOz-VES micelles might have significant promise for anti-cancer drug delivery.

关 键 词：Polymeric micelles  pH-Responsibility  Poly（2-ethyl-2-oxazoline）  PACLITAXEL In vitro release  

分 类 号：R943]