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胸腺嘧啶修饰的两亲性可生物降解共聚物用于光交联胶束作为稳定的药物载体。

Thymine modified amphiphilic biodegradable copolymers for photo-cross-linked micelles as stable drug carriers.

机构信息

State Key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, 130022, China; Graduate School of Chinese Academy of Sciences, Beijing, 100049, China.

出版信息

Macromol Biosci. 2013 Nov;13(11):1593-600. doi: 10.1002/mabi.201300254. Epub 2013 Aug 21.

Abstract

A photo-cross-linked micelle is synthesized via photodimerization of thymine moieties fabricated from amphiphilic block copolymers (mPEG-b-P(LA-co-MPT). The crosslinking behavior is monitored by UV-Vis spectra and (1) H NMR. Dynamic light scattering (DLS) and transmission electron microscopy (TEM) showed that cross-linked micelles had smaller sizes than their uncross-linked precursors. In vitro studies reveal that cross-linking of the micelle cores results in a slow drug release and faster cellular uptake in comparison with uncross-linked ones in MCF-7 and Hela cells. Moreover, the paclitaxel (PTX)-loaded core-cross-linked micelles exhibit similar anticancer efficacy as free PTX. This work provides a convenient tool for designing a more stable structure in the blood circulation to realize a controlled drug delivery.

摘要

一种光交联胶束是通过由两亲嵌段共聚物(mPEG-b-P(LA-co-MPT))制备的胸腺嘧啶部分的光二聚化合成的。通过紫外可见光谱和(1)H NMR 监测交联行为。动态光散射(DLS)和透射电子显微镜(TEM)表明,与未交联的前体相比,交联胶束的粒径更小。体外研究表明,与未交联的胶束相比,胶束核的交联导致药物释放缓慢,细胞摄取更快,在 MCF-7 和 Hela 细胞中。此外,负载紫杉醇(PTX)的核交联胶束表现出与游离 PTX 相似的抗癌功效。这项工作为设计在血液循环中更稳定的结构以实现药物控制释放提供了一种方便的工具。

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