双重敏感性两亲性聚己内酯混合胶束的合成

Dual-Sensitive Mixed Micelle Formed by Amphiphilic Poly(Epsilon-Caprolactone) Copolymers

合成了两亲性嵌段共聚物聚己内酯(ε-己内酯)-b-聚甲基丙烯酸二乙胺基乙酯和聚乙二醇-二硫键-聚己内酯,用核磁氢谱和凝胶渗透色谱对聚合物的结构及分子量进行了表征。用溶剂挥发法制备了聚合物胶束,用动态光散射以及扫描电镜对胶束结构及性质进行了表征。结果显示,两种聚合物自身可以形成胶束,也可以形成混合胶束;形成的混合胶束粒径在pH小于5.5或pH大于6.5时基本保持稳定,且前者稍大于后者,而在10mmol/L的二硫苏糖醇(DTT)的还原条件下,胶束发生破坏并产生团聚,体现了混合胶束的pH敏感性和还原敏感性,期望能够作为新的药物载体。

Amphiphilic copolymers poly （ epsilon-caprolactone）-b-poly （ 2-（diethylamino） ethyl methacrylate） and disulfide-linked of poly （epsilon-caprolactone）-poly （ethyl glycol） were synthesized. Molecular structure of the amphiphilic copolymers was confirmed by 1H-nuclear magnetic resonance and gelpermeation chromatography. Micelles were formed by solvent evaporation method and were characterized dynamic light scattering, scanning electron microscope. The results indicate that micelles could be formed by individual copolymers or cooperatively by these two copolymers. The size of the mixed micelle is stable when pH is lower than 5.5 or higher than 6.5, and the former size is larger than the latter one. When treated in 10mmol/L dithiothreitol （DTT）, the micelles are damaged and become to aggregate, indicating pH and reduction dual-responsivity of the mixed micelles, which suggests that the copolymers can be used as anticancer drug carriers.