PEG2000-DSPE含量不同的酒石酸长春瑞滨脂质体的制备和评价

Preparation and Evaluation of Vinorelbine Tartrate Liposomes with Different PEG2000-DSPE Contents

采用蔗糖八硫酸酯三乙胺梯度法制备聚乙二醇2000-二硬脂酰磷脂酰乙醇胺(PEG2000-DSPE)摩尔比分别为6%、3%和1%的酒石酸长春瑞滨(1)脂质体。考察了3种处方脂质体的药物粒径、ζ电位、包封率、体外释放度和稳定性。以1注射液为对照,比较3种脂质体对裸鼠SW620移植瘤的生长抑制作用。结果表明,3种处方脂质体的体外特性基本一致,且4℃条件下放置6个月,各样品的主要质量指标均未发生显著变化。药效学研究结果表明,PEG2000-DSPE含量由高至低的各脂质体组抑瘤率分别为52.8%、72.1%和61.8%,而1注射液组抑瘤率仅47%。

The vinorelbine tartrate （1） liposomes with 6％,3％ and 1％ molar ratios of polyethylene glycol 2000-distearoyl phosphatidyl ethanolamine （PEG2000-DSPE） were prepared by sucrose octasulfate gradient method.The particle size,ξ potential,entrapment efficiency,in vitro release and stability of the three types of liposomes were detected.The growth inhibition effects of three types of liposomes on SW620 cells transplanted into nude mice were investigated with 1 injection as the contrast.The results showed that the in vitro characteristics of the three types of liposomes were similar.Moreover,the main quality indicators of the three types of liposomes stored at 4 ℃ for 6 months had no significant changes.The tumor growth inhibition effects of the liposomes with 6 ％,3 ％ and 1％ of PEG2000-DSPE were 52.8 ％,72.1％ and 61.8 ％,respectively.Meanwhile,the tumor inhibition of 1 injection was only 47 ％.