Reduction-sensitive amphiphilic copolymers made via multi-component Passerini reaction for drug delivery
Reduction-sensitive amphiphilic copolymers made via multi-component Passerini reaction for drug delivery
复制标题
通过多组分帕塞里尼反应制备的还原敏感两亲共聚物用于药物递送
DOI：
10.1016/j.colsurfb.2014.12.030
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发表时间：
2015-02-01
影响因子：
5.8
通讯作者：
Xie, Zhigang
中科院分区：
文献类型：
--
作者：
Lin, Wenhai;Guan, Xingang;Xie, Zhigang
通过多组分Passerini反应，一步合成了疏水骨架中含有二硫键的两亲聚合物。所得聚合物在水溶液中自组装成胶束。姜黄素（CUR）是一种安全有效的抗癌药物，但由于其不溶于水，生物利用度低，因此被限制在胶束中作为模型药物。通过动态光散射（DLS）和透射电子显微镜（TEM）证实了纳米聚合物胶束。激光共聚焦扫描显微镜（CLSM）观察到更快的细胞内CUR释放与GSH预处理的HeLa细胞比未预处理的。胶束还负载有NH 2-BODIPY，其几乎是无荧光的，并且在酸性条件下给出强增强的荧光。在预处理的HeLa细胞中的较强的荧光增强现象进一步表明所获得的聚合物是还原敏感的。体外MTT实验表明，该胶束具有良好的生物相容性，与游离CUR相比，负载CUR的胶束对HeLa细胞具有更高的增殖抑制作用。这些结果突出了利用多组分Passerini反应制备功能共聚物作为药物递送的智能纳米载体的潜力。(C)2014爱思唯尔有限公司版权所有。
One-step synthesis of amphiphilic polymers containing disulfide bond within the hydrophobic backbone was demonstrated via multi-component Passerini reaction. The obtained polymer was self-assembled into micelles in aqueous solution. Curcumin (CUR), an effective and safe anticancer agent, which was limited by its water insolubility and poor bioavailability, was loaded into the micelles as a model drug. The nanoscale polymeric micelles were confirmed by dynamic light scattering (DLS) and transmission electron microscopy (TEM). Faster intracellular CUR release was observed by confocal laser scanning microscopy (CLSM) in the HeLa cells pretreated with GSH than in the unpretreated ones. Micelles also loaded with NH2-BODIPY which was almost non-fluorescent and gave strong enhanced fluorescence under acid conditions. The phenomenon of the stronger enhanced fluorescence in the pretreated HeLa cells showed further that the obtained polymer was reduction-sensitive. In vitro MTT assays showed that the micelles were biocompatible and CUR-loaded micelles had higher cellular proliferation inhibition in contrast to free CUR toward HeLa cells. These results highlight the potential of using multi-component Passerini reaction to make functional copolymers as smart nanocarriers for drug delivery. (C) 2014 Elsevier B.V. All rights reserved.