Synthesis of poly(ethylene glycol)-SS-poly(ε-caprolactone)-SS-poly(ethylene glycol) triblock copolymers via end-group conjugation and self-assembly for reductively responsive drug delivery

被引：0
作者：
Junbo Li
Junting Jiang
Biyu Zhou
Chaohuang Niu
Wendi Wang
Wenlan Wu
机构：
[1] Henan University of Science and Technology,School of Chemical Engineering and Pharmaceutics
[2] Henan University of Science and Technology,School of Medicine
来源：
Frontiers of Materials Science | 2019年 / 13卷
关键词：
poly-ε-caprolactone; poly(ethylene glycol); block copolymer; reductive responsiveness; drug; release;
D O I：
暂无
中图分类号：
学科分类号：
摘要：
In this study, we describe a simple synthesis route to prepare triblock copolymers with disulfide-linkers, poly(ethylene glycol)-SS-poly(ε-caprolactone)-SS-poly (ethylene glycol) (PEG-SS-PCL-SS-PEG) for application in the reductively responsive release of doxorubicin (DOX). To synthesize PEG-SS-PCL-SS-PEG, two end-groups of PCL-diol were first modified with cystamine to introduce disulfide bonds and subsequently conjugated with PEG-NHS via carbodiimide chemistry. PEG-SS-PCL-SSPEG fabricated into polymeric micelles with stable structure and different nanoscale sizes via adjusting the PCL chain length, showing obvious reductive responsiveness and fast drug release of encapsulated DOX in the presence of glutathione (GSH). Moreover, DOX-loaded PEG-SS-PCL-SS-PEG micelles exhibited higher therapeutic efficacy than reduction-insensitive PEG-b-PCL micelles in vitro. Thus, end-groups conjugation is a simple and straightforward strategy to introduce intelligent responsiveness in biocompatible block copolymers and improve their therapeutic efficacy.
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页码：410 / 419
页数：9
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