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。
Nanoparticles with typical core-shell structure were prepared with a blend of methoxypoly（ethylene glycol）-poly（lactide） copolymer （MPEG-PLA） and poly （lactic acid） （PLA） along with paclitaxel by the O/W solvent evaporation method. An orthogonal experiment L9（3）3 was applied to get the best preparation conditions. The core-shell paclitaxel-loaded MPEG-PLA/PLA nanoparticles with the highest drug loading efficiency were obtained when amount of MPEG-PLA, time of ultrasonication and volume of deionized water were 300 mg, 10 rain and 30 mL, respectively. The release behavior of paclitaxel from the optimal MPEG-PLA/PLA nanoparticles showed that 22% ofpaclitaxel was released in 14 d. When incubating with human nasopharyngeal carcinoma ceils expressing LMP 1, these optimal nanoparticles showed a little lower tumor growth compared with free paclitaxel.
