巯基-烯点击化学法制备还原响应两亲性聚合物

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.

Synthesis of Reduction responsive Amphiphilic Copolymer by Thiolene Click Chemistry

Amphiphilic triblock copolymer mPEG b P1 b mPEG,with disulfide bond in the main chain of the hydrophobic block,was prepared from cystamine dihydrochloride,allyl chloroformate,1,6 hexanedithiol and monomethoxy poly (ethylene glycol) with a thiol end group through thiolene click chemistry method. Self assembly of the obtained mPEG b P1 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 micelles in the presence of DTT,indicating the reduction responsiveness of the obtained amphiphilic copolymer. Therefore,these findings suggested the potentials of the amphiphilic copolymers as smart intracellular drug delivery systems.