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新型硫醇响应性可降解聚乳酸基嵌段共聚物胶束的设计。

New design of thiol-responsive degradable polylactide-based block copolymer micelles.

机构信息

Department of Chemistry and Biochemistry and Centre for Nanoscience Research (CENR), Concordia University, Montreal, Quebec, Canada.

出版信息

Macromol Rapid Commun. 2013 Jan 25;34(2):163-8. doi: 10.1002/marc.201200532. Epub 2012 Sep 28.

Abstract

A new design to synthesize thiol-responsive degradable polylactide (PLA)-based micelles having a disulfide linkage in the middle of triblock copolymers is reported. They were synthesized by a new method that centers on the use of a disulfide-labeled diol as an initiator for ring-opening polymerization, followed by controlled radical polymerization. These well-controlled copolymers with monomodal and narrow molecular weight distribution (M(w) /M(n) < 1.15) self-assembled to form aqueous micellar aggregates with disulfide-containing PLA cores, which is not toxic to cells. Central disulfide linkages were cleaved in response to thiols; such thiol-triggered degradation enhanced the release of encapsulated anticancer drugs.

摘要

报道了一种新的设计,用于合成具有二硫键的硫醇响应性可降解聚乳酸(PLA)基胶束,该胶束在三嵌段共聚物的中间具有二硫键。它们是通过一种新的方法合成的,该方法的核心是使用二硫键标记的二醇作为引发剂进行开环聚合,然后进行可控自由基聚合。这些具有单分散性和较窄分子量分布(M(w)/M(n) < 1.15)的良好控制的共聚物自组装形成含有含二硫键的 PLA 核的水性胶束聚集体,对细胞没有毒性。中心二硫键在硫醇的响应下被切断;这种硫醇触发的降解增强了封装的抗癌药物的释放。

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