Objective: To investigate the stability and physicochemieal properties of the dispersed docetaxel lyophilized polymeric micelle formulations containing arginine as a stabilizing agent. Methods: Arginine containing (experimental group) and arginine free (control group) lyophilized formulations were respectively prepared using monomethoxy poly (ethylene glycol)-block-poly (D,L-lactide) (mPEG-PLA) as a carrier by evaporation and hot melt method. We explored the stability of the micelle solution by monitoring micelle size and content of docetaxel over time at room temperature. The entrapment efficiency and drug content were characterized by HPLC. The morphology, diameter, size distribution and zeta potential of the micelles were characterized by atomic force microscopy (AFM), dynamic light scattering (DIS) and zeta potential analyzer, respectively. The in vitro release behavior of docetaxel from polymeric micelles was investigated using dialysis method. Results: The dispersed docetaxel lyophilized polymeric micelle solution remained stable at room temperature over 12 hours. Conclusion: The incorporation of arginine improves the stability of docetaxel loaded polymeric micelle.%目的:考察以精氨酸作为稳定剂的多西他赛嵌段聚合物胶束冻干粉的复溶稳定性与理化性质.方法:以聚乙二醇单甲醚-聚乳酸嵌段共聚物(mPEG-PLA)为载体制备多西他赛胶束冻干粉对照组制剂与实验组制剂(含精氨酸).通过动态光散射法(DLS)与高效液相色谱法(HPLC)测定了制剂复溶后胶束粒径与多西他赛含量随时间的变化.分别使用(HPLC)、原子力显微镜、动态光散射法和Zeta电位分析仪对包封率、胶束形态、粒径与分布、Zeta电位和pH进行了表征;采用透析法考察了载药聚合物胶束的体外释放.结果:室温条件下实验组制剂复溶后胶束溶液在考察的12h内保持稳定.结论:精氨酸的加入使实验组制剂稳定得到极大提高.
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