星状pH响应聚合物及其自组装胶束研究

研究了一种星状聚合物——金刚烷基聚己内酯-b-聚甲基丙烯酸二乙氨基乙酯-b-聚甲基丙烯酸单甲氧基聚乙二醇酯（Ad-（PCL-b-PDEAEMA-b-PPEGMA）₄）及其自组装胶束以用于阿霉素（DOX）递送.采用ROP和ARGET ATRP方法合成该聚合物，其自组装胶束具有良好的稳定性（CMC=3.4 mg/L）；DOX负载胶束在pH=5.0下的释放速率明显快于pH=7.4和pH=6.8.结果表明，pH响应Ad-（PCL-b-PDEAEMA-b-PPEGMA）₄胶束可作为抗癌药物靶向递送的潜在载体.

A Study of Star pH-Responsive Polymer and Its Self-Assembled Micelles

A star-shaped polymer adamantane-poly(ε-caprolactone)-b-poly(2-(diethylamino)ethyl methacrylate)-b-poly(poly(ethylene glycol) methyl ether methacrylate)]₄ (Ad-(PCL-b-PDEAEMA-b-PPEGMA)₄) and its pH-responsive self-assembled polymeric micelles were developed for adriamycin (DOX) delivery. This star-shaped polymer was synthesized via ring-opening polymerization (ROP) and activators regenerated by electron transfer atom transfer radical polymerization (ARGET ATRP), and characterized by ¹H NMR spectroscopy, gel permeation chromatograph (GPC), fluorescence spectra and dynamic light scattering (DLS). The resulting polymer had a definite structure with a narrow molecular weight distribution (PDI<1.3); the critical micelle concentration (CMC) of the polymer was very low (3.4 mg/L), which indicated that the polymeric micelles would keep stable in blood circulation system; resulting from the protonation of the tertiary amine group of PDEAEMA, the release performance of micelles at pH=5.0 were rapider than that at pH=7.4 and pH=6.8. The results shows that pH-responsive Ad-(PCL-b-PDEAEMA-b-PPEGMA)₄ micelles could be a potential carrier for targeted delivery of anti-cancer drugs with controlled and sustained release behavior.