【摘要】 目的:探讨经聚乙二醇包覆后阿糖胞苷脂质体的物理稳定性。方法:以阿糖胞苷为装载药物,用经纯化的天然卵磷脂和胆固醇为包封材料,卵磷脂与胆固醇的摩尔比为1:1,用反相蒸发法制备阿糖胞苷脂质体。不同浓度的聚乙二醇对脂质体包覆进行表面修饰,通过显微形态鉴定,装载药物的渗漏量及经37~℃、48 h温育前后平均粒径的变化,对聚乙二醇包覆后阿糖胞苷脂质体的物理稳定性进行评价。结果:修饰后的阿糖胞苷脂质体具有较大的平均粒径和较低的药物渗漏量。当聚乙二醇浓度为2.0 mg/m L时,脂质体形态良好,药物的渗漏量比未修饰的脂质体低77.8%。温育后,脂质体平均粒径的增加值最低为151 nm。结论:阿糖胞苷脂质体经聚乙二醇的包覆提高了物理稳定性。更多还原

【Abstract】 Objective: To probe the effect of polyethylene glycol(PEG) on physical stability of cytarabine(Ara-C) liposome.Methods: Natural phosphatidyl choline and cholesterol(1 1, molar ratio) was used to prepare Ara-C liposome by reverse evaporating method, then Ara-C liposome was coated by different concentrations of PEG. The morphological characteristics, leaking amount of drug(LA) and the variation of mean particle size(MPS) of liposome after incubated at 37 ~℃ for 48 h were measured to assess the effect of membrane encapsulation by PEG on physical stability of Ara-C liposome. Results: PEG modified Ara-C liposome had bigger MPS and lower LA. PEG liposome had good appearance, its LA was 77.8 % lower than that of unmodified liposome and the MPS increase 151 nm was the smallest at ρ(PEG)=2.0 mg/m L. Conclusion: Physical stability of Ara-C liposome coated with PEG was enhanced.更多还原