文献类型：期刊文献

英文题名：Acetal-Linked Paclitaxel Polymeric Prodrug Based on Functionalized mPEG-PCL Diblock Polymer for pH-Triggered Drug Delivery

作者：Zhai, Yinglei Zhou, Xing Jia, Lina Ma, Chao Song, Ronghua Deng, Yanhao Hu, Xueyao Sun, Wei

第一作者：Zhai, Yinglei

通信作者：Sun, W[1]

机构：[1]Shenyang Pharmaceut Univ, Sch Med Devices, Dept Biomed Engn, Shenyang 110016, Peoples R China;[2]Luoyang Ship Mat Res Inst LSMRI, State Key Lab Marine Corros & Protect, Qingdao 266101, Peoples R China;[3]Hainan Inst Mat Med, Haikou 570311, Hainan, Peoples R China;[4]Shenyang Pharmaceut Univ, Sch Life Sci & Biopharmaceut, Dept Pharmacol, Shenyang 110016, Peoples R China;[5]Guizhou Inst Technol, Coll Food & Pharmaceut Engn, Guiyang 550003, Guizhou, Peoples R China

第一机构：Shenyang Pharmaceut Univ, Sch Med Devices, Dept Biomed Engn, Shenyang 110016, Peoples R China

通信机构：corresponding author), Shenyang Pharmaceut Univ, Sch Med Devices, Dept Biomed Engn, Shenyang 110016, Peoples R China.

年份：2017

卷号：9

期号：12

外文期刊名：POLYMERS

收录：;EI(收录号：20175004545818);Scopus(收录号：2-s2.0-85037728516);WOS:【SCI-EXPANDED(收录号:WOS:000419239400064)】；

基金：This work is supported by the National Natural Science Foundation of China (81603053 and 81502927), Hainan S&T Project (KYYS-2015-38), and the Scientific Research General Project of Liaoning Provincial Department of Education (201610163L29).

语种：英文

外文关键词：prodrug; polymer micelles; pH-sensitive; acetal; paclitaxel

摘要：The differences in micro-environment between cancer cells and the normal ones offer the possibility to develop stimuli-responsive drug-delivery systems for overcoming the drawbacks in the clinical use of anticancer drugs, such as paclitaxel, doxorubicin, and etc. Hence, we developed a novel endosomal pH-sensitive paclitaxel (PTX) prodrug micelles based on functionalized poly(ethylene glycol)-poly(epsilon-caprolactone) (mPEG-PCL) diblock polymer with an acid-cleavable acetal (Ace) linkage (mPEG-PCL-Ace-PTX). The mPEG-PCL-Ace-PTX5 with a high drug content of 23.5 wt % was self-assembled in phosphate buffer (pH 7.4, 10 mM) into nanosized micelles with an average diameter of 68.5 nm. The in vitro release studies demonstrated that mPEG-PCL-Ace-PTX5 micelles was highly pH-sensitive, in which 16.8%, 32.8%, and 48.2% of parent free PTX was released from mPEG-PCL-Ace-PTX5 micelles in 48 h at pH 7.4, 6.0, and 5.0, respectively. Thiazolyl Blue Tetrazolium Bromide (MTT) assays suggested that the pH-sensitive PTX prodrug micelles displayed higher therapeutic efficacy against MCF-7 cells compared with free PTX. Therefore, the PTX prodrug micelles with acetal bond may offer a promising strategy for cancer therapy.