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以磷酰胺键将聚乙二醇高分子MePEG2000-NH2与磷脂POPA连接在一起,合成聚乙二醇磷脂衍生物,以聚乙二醇磷脂衍生物为主要膜材构建酸敏脂质体。采用荧光分析法系统研究了聚乙二醇磷脂衍生物脂质体在酸性条件下对荧光染料的释药特性。以聚乙二醇磷脂衍生物构建的酸敏脂质体,在pH6.5～7.5时稳定,其稳定性与制备脂质体的磷脂种类及胆固醇含量密切相关,在pH5.0时发生显著的荧光泄漏,泄漏率与环境酸性的强度及处于酸性的时间呈正相关。聚乙二醇磷脂衍生物构建的脂质体具有开发成酸敏释药脂质体的前景。
Phosphamide bond polyethylene glycol polymer MePEG2000-NH2 and phospholipid POPA linked together to synthesize polyethylene glycol phospholipid derivatives, polyethylene glycol phospholipid derivatives as the main material to build acid-sensitive liposomes. Fluorescence analysis was used to systematically study the drug release characteristics of liposomes with polyethylene glycol phospholipid under acidic conditions. Acid-sensitive liposomes constructed with polyethylene glycol phospholipid derivatives are stable at pH 6.5-7.5 and their stability is closely related to the type of lipids and the cholesterol content, and significant at pH 5.0 Fluorescent leakage, leakage rate and environmental acidity and acidity in the time was positively correlated. Liposomes constructed with polyethylene glycol phospholipid derivatives have the potential of developing liposomes as acid sensitive drug-eluting liposomes.