目的 制备紫杉醇/聚乙二醇-聚谷氨酸苄酯纳米胶束的冻干粉针剂。方法 以胶束粒径、有机溶剂残留量等为评价指标，采用膜透析法制备纳米胶束；以冻干成品的外观形态、体外释药曲线为评价指标，优选冻干粉针剂的制剂处方；研究粉针剂的冻干工艺及该粉针剂对HepG-2肝癌细胞的体外细胞毒性。结果 以3 %甘露醇为比例，制备获得紫杉醇纳米胶束冻干粉针剂外观良好，其体外释药曲线具有突释与缓释特性，且与新鲜透析所得载药纳米胶束溶液的释药曲线基本相同；当紫杉醇浓度≤10 μg·mL-1时，冻干粉针剂对HepG-2肝癌细胞的细胞毒性远低于市售紫杉醇注射剂(P < 0.01)。结论 采用膜透析结合冷冻干燥法制备紫杉醇纳米胶束冻干粉针剂，避免使用紫杉醇增溶剂(聚氧乙烯蓖麻油)带来的不良过敏反应，并降低对体外肝癌细胞的细胞毒性，具有较好的临床价值与应用前景。

Objective To prepare the paclitaxel-loaded polyethylene glycol-polybenzyl-L-glutamate(PEG-PBLG)lyophilized nano-micelles and to study the in vitro properties of the nano-micelles. Methods With the micelle particle diameter and organic solvent residual volume as the evaluation indexes，paclitaxel-loaded lyophilized nano-micelles with amphiphilic copolymer PEG-PBLG was prepared by the membrane dialysis method. The preparation formula of paclitaxel-loaded lyophilized nano-micelles was optimized with the lyophilized nano-micelles macroscopic appearance and in-vitro drug-release curve as the indexes. The in vitro effects of paclitaxel-loaded lyophilized nano-micelles and commercially available paclitaxel injection with Cremophor EL on the growth of tumor cells were observed. Results The paclitaxel-loaded lyophilized nano-micelles showed better macroscopic appearance when the proportion of manicol was 3 %. The in vitro paclitaxel release profile was characterized with a rapid release at the initial stage and then following by smooth and sustained-release from the lyophilized nano-micelles. At low concentration of paclitaxel(≤10 μg·mL-1)，the paclitaxel-loaded PEG-PBLG lyophilized nano-micelles displayed much less cell cytotoxicity than paclitaxel injection with Cremophor EL(P < 0.01). Conclusion The paclitaxel-loaded PEG-PBLG lyophilized nano-micelles have less cytotoxicity than the commercially available paclitaxel injections with Cremophor EL. Hence，paclitaxel-loaded PEG-PBLG micelles would be a novel paclitaxel preparation in clinic for the treatment of tumor.

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广东省科技计划项目(2009B030801081)；广东省自然科学基金(博士启动S2012040007298)；广东高校优秀青年创新人才培养计划(育苗工程2012LYM_0130)；佛山科学技术学院校级课题(2011101)。