王继波,金景玉,刘继民,刘兆刚,姜晓丽.脂膜修饰对阿糖胞苷脂质体物理稳定性的影响[J].,2017,17(35):6842-6846 |
脂膜修饰对阿糖胞苷脂质体物理稳定性的影响 |
Effect of Membrane Modification on Physical Stability of Cytarabine Liposome |
投稿时间:2017-02-28 修订日期:2017-03-24 |
DOI:10.13241/j.cnki.pmb.2017.35.010 |
中文关键词: 脂膜修饰 阿糖胞苷 脂质体 物理稳定性 |
英文关键词: Membrane modification Cytarabine Liposome Physical stability |
基金项目:山东省自然科学基金项目(ZR2011CM041) |
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中文摘要: |
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/mL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。 |
英文摘要: |
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/mL. Conclusion: Physical stability of Ara-C liposome coated with PEG was enhanced. |
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