Facile fabrication of thermo-responsive and reduction-sensitive polymeric micelles for anticancer drug delivery.
Facile fabrication of thermo-responsive and reduction-sensitive polymeric micelles for anticancer drug delivery.
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DOI：
10.1002/mabi.201100459
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发表时间：
2012-05
影响因子：
4.6
通讯作者：
Xulin Jiang;Lihua Li;Jia Liu;W. Hennink;R. Zhuo
中科院分区：
文献类型：
--
作者：
Xulin Jiang;Lihua Li;Jia Liu;W. Hennink;R. Zhuo
本文报道了一种基于两亲性嵌段共聚物聚[（PEG-MEMA）-co-（Boc-Cyst-MMAm）]-block-PEG（简称PEG-P-SS-HP）的温度响应性和还原敏感性聚合物胶束的研究进展。以PTX为模型药物，以> 90%的包封率将PTX负载到PEG-P-SS-HP胶束中，导致高载药量（高达35wt%）。载PTX的PEG-P-SS-HP胶束在PBS中显示缓慢的药物释放，并且在与DTT孵育后显示快速释放。载PTX的胶束显示出比游离药物更好的细胞毒性作用，而空胶束被发现是无毒的。所描述的温度响应性和还原敏感性聚合物胶束可作为细胞抑制药物的有前途的载体。
The development of thermo-responsive and reduction-sensitive polymeric micelles based on an amphiphilic block copolymer poly[(PEG-MEMA)-co-(Boc-Cyst-MMAm)]-block-PEG (denoted PEG-P-SS-HP) for the intracellular delivery of anticancer drugs is reported. PTX, as model drug, was loaded into the PEG-P-SS-HP micelles with an encapsulation efficiency >90%, resulting in a high drug loading content (up to 35 wt%). The PTX-loaded PEG-P-SS-HP micelles show slow drug release in PBS and rapid release after incubation with DTT. The PTX-loaded micelles display a better cytotoxic effect than the free drug, whereas empty micelles are found to be non-toxic. The thermo-responsive and reduction-sensitive polymeric micelles described may serve as promising carriers for cytostatic drugs.