Key Laboratory of Biomedical Polymers of Ministry of Education, and Department of Chemistry, Wuhan University, Luojia Hill, Wuhan 430072, China.
Macromol Biosci. 2012 May;12(5):703-11. doi: 10.1002/mabi.201100459. Epub 2012 Apr 11.
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.
本文报道了一种基于两亲嵌段共聚物聚[(PEG-MEMA)-共-(Boc-Cyst-MMAm)]-嵌段-PEG(记为 PEG-P-SS-HP)的温敏和还原敏感聚合物胶束的发展,用于抗癌药物的细胞内递送。PTX 作为模型药物,被包封到 PEG-P-SS-HP 胶束中,包封效率>90%,载药含量高(高达 35wt%)。负载 PTX 的 PEG-P-SS-HP 胶束在 PBS 中显示出缓慢的药物释放,而在与 DTT 孵育后则迅速释放。负载 PTX 的胶束显示出比游离药物更好的细胞毒性作用,而空胶束则被发现没有毒性。所描述的温敏和还原敏感聚合物胶束可用作细胞毒性药物的有前途的载体。