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通过酯键将末端羧基化的聚乙二醇-聚乳酸(PEG-PLA)与紫杉醇连接,合成了前体化合物PEG-PLA-PTX(1),总收率约56%。芘荧光探针法测得1水溶液的临界胶束浓度为3.98×10-4 g/L,1在p H 7.4磷酸盐缓冲液中能缓慢释放出紫杉醇。体外抗肿瘤试验表明,1具有抑制鼻咽癌LMP1细胞增殖的作用。
PEG-PLA-PTX (1) was synthesized by the conjugation of terminal carboxylated polyethylene glycol-polylactic acid (PEG-PLA) with paclitaxel. The total yield was about 56%. Pyrene fluorescence probe method measured the critical micelle concentration of 1 aqueous solution of 3.98 × 10-4 g / L, 1 in p H 7.4 phosphate buffer can be slowly released paclitaxel. In vitro anti-tumor test showed that 1 has the effect of inhibiting the proliferation of nasopharyngeal carcinoma LMP1 cells.