State Key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, China.
Macromol Biosci. 2009 Nov 10;9(11):1059-68. doi: 10.1002/mabi.200900134.
A folate-conjugated copolymer PEG-PLA-PLL/folate was synthesized and mixed with pure PEG-PLA-PLL and a fluorescent model drug mFITC to prepare folate-conjugated micelles. The distribution of micelles was studied on cancer-cell-bearing mice via frozen slicing. The results show that mFITC is successfully encapsulated into folate(+) and folate(-)micelles; PEG-PLA-PLL micelles the latter can be internalized by both HeLa and CHO cells without selectivity due to their cationic surface charges, while folate(+)micelles exhibit more preferential endocytosis by HeLa cells than by CHO cells. The folate(-)micelles showed retention in both organs and tumors. The folate(+)micelles are a promising active targeting drug delivery system for FR over-expressing cells and they accumulate in tumor beds.
叶酸偶联共聚物 PEG-PLA-PLL/叶酸被合成，并与纯 PEG-PLA-PLL 和荧光模型药物 mFITC 混合，以制备叶酸偶联胶束。通过冷冻切片研究胶束在荷瘤小鼠中的分布。结果表明，mFITC 成功地包封在叶酸（+）和叶酸（-）胶束中；PEG-PLA-PLL 胶束后者由于其阳离子表面电荷，可以被 HeLa 和 CHO 细胞同时内吞，而没有选择性，而叶酸（+）胶束表现出对 HeLa 细胞的优先内吞作用，而不是 CHO 细胞。叶酸（-）胶束在器官和肿瘤中都有保留。叶酸（+）胶束是 FR 过表达细胞的一种有前途的主动靶向药物传递系统，它们在肿瘤床中积累。
