Abstract
采用本体开环聚合法, 以乙交酯(GA)和 DL -丙交酯(DLA)为原料, 肌醇为引发剂, 合成了一系列不同分子量的六臂星型聚乳酸聚乙醇酸(PLGA)(6-s-PLGA 50 , 6-s-PLGA 100 , 6-s-PLGA 200 , 其中50, 100, 200为原料与引发剂的摩尔比), 采用羧基化反应对其端基进行羧化处理. 以聚乙二醇4000(PEG4000)为原料用对甲苯磺酰化法得到sTO-PEG-OTs, 再进行氨解得到双端氨基PEG(H 2 N-PEG-NH 2 ). 末端羧基6-s-PLGA x 通过 N -环己基碳二亚胺(DCC)缩合反应与双端氨基PEG连接得到两亲性星型六臂结构的聚合物(6-s-PLGA x -PEG-NH 2 ). 分别用核磁共振氢谱法( 1 H NMR)、 凝胶排阻色谱法(GPC)及差示热量热分析法(DSC)等手段对6-s-PLGA x 和6-s-PLGA x -PEG-NH 2 进行了表征. 以6-s-PLGA 100 -PEG-NH 2 聚合物为例, 自组装得到空白的纳米粒子, 并用透射电子显微镜法(TEM)和动态光散射法(DLS)考察了粒子的表面形态以及粒径分布特征, 用 1 H NMR分析了胶束的核-壳结构. 用噻唑蓝四氮唑溴化物(MTT)比色法探讨了该两亲性材料的体外细胞毒性. 研究结果表明, 合成了不同分子量的两亲性六臂星型端氨基PEG-PLGA, 该两亲性聚合物可自组装形成纳米胶束, 粒径范围在40~60 nm, 与PLGA 相比体外细胞毒性无显著性差异.
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