注射用多西他赛脂质体的制备及其体内外评价

 目的：制备多西他赛脂质体，对其体内外性质进行评价。方法：采用改良薄膜分散法结合冷冻干燥工艺制备多西他赛脂质体冻干粉；用激光粒度仪考察了脂质体的粒径分布和Zeta电位；超滤法测定了包封率；以市售多西他赛注射液为对照，比较体外释放、大鼠骨髓抑制和裸鼠体内肿瘤抑制情况。结果：多西他赛脂质体平均粒径为92 nm，Zeta电位为-52.3 mV，包封率＞95%，24 h累积释放率为84.1%；相同剂量下，多西他赛脂质体比多西他赛注射液的骨髓抑制作用降低，但二者对HT-29移植瘤的抑制作用相同。结论：本实验所制备的多西他赛脂质体包封率较高、稳定性较好；与多西他赛注射液相比，毒性较低，同时具有相同的抗肿瘤效力。 

Preparation and in vivo-in vitro evaluation of docetaxel liposome for injection

Objective:To prepare docetaxel liposomes and characterize its in vitro and in vivo properties.Methods: Docetaxel liposomes were prepared by modified film dispersion-high pressure homogenization and lyophilization.Vesicle size and Zeta potential were determined by the Zetasizer Nano ZS.Encapsulation efficiency was evaluated by ultrafiltration method.The in vitro release,bone marrow toxicity and tumor inhibition of liposomal docetaxel were investigated in comparation with docetaxel injection.Results: The mean...