巯基-烯点击化学法制备还原响应两亲性聚合物

Synthesis of Reduction-responsive Amphiphilic Copolymer by Thiolene Click Chemistry

以胱胺二盐酸盐、氯甲酸烯丙酯、1,6-己二硫醇及端巯基聚乙二醇单甲醚等为原料,通过巯基-烯点击化学反应,合成了疏水段含二硫键的两亲性三嵌段共聚物mPEG-bP1-b-mPEG.对mPEG-b-P1-b-mPEG在水溶液中的自组装行为进行了深入的研究.结果表明,mPEG-b-P1-b-mPEG的临界胶束浓度为0.032 mg/mL,形成胶束的平均粒径为61.3nm.包载模拟药物尼罗红的释放行为研究表明,在D,L-二硫苏糖醇(DTT)存在的条件下,包裹在胶束中的尼罗红可以被释放出来,显示出快速的还原响应性能,表明合成的两亲性三嵌段共聚物mPEG-b-P1-b-mPEG有望作为疏水性药物载体,应用于药物控释领域.

Amphiphilic triblock copolymer mPEG-b-Pl-b-mPEG,with disulfide bond in the main chain of the hydrophobic block, was prepared from cystamine dihydrochloride, allyl chloroformate, 1,6-hexanedi- thiol and monomethoxy poly （ethylene glycol） with a thiol end group through thiolene click chemistry method. Self-assembly of the obtained mPEG-b-PI-b-mPEG was further investigated. The results showed that the critical micelle concentration of the amphiphilic block polymer was 0.032 mg/mL,and the average diameter of the micelle was about 61.3 nm. The loaded model drug Nile Red could be released from the mi- celles in the presence of DTT, indicating the reduction responsiveness of the obtained amphiphilic copoly- mer. Therefore, these findings suggested the potentials of the amphiphilic copolymers as smart intracellular drug delivery systems.