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目的:分别制备含豆甾醇和胆甾醇的染料木素脂质体,研究脂质体热致相变的热力学性质,比较不同甾醇对脂质体热稳定性的影响。方法:用薄膜分散法制备空白和含药脂质体,差示扫描量热法(DSC)确定不同脂质体主相变的相变温度、相变焓等热力学参数。结果:含药脂质体的相变温度、相变焓均低于空白脂质体。在组成相同的情况下,豆甾醇脂质体与胆甾醇脂质体的相变温度和相变焓无明显差别。结论:染料木素进入脂质体膜的疏水区与磷脂分子的疏水尾链发生疏水相互作用。豆甾醇代替胆甾醇后脂质体的热稳定性变化很小,提示可用豆甾醇代替胆甾醇作为染料木素脂质体的膜材。
OBJECTIVE: To prepare the genistein liposomes containing stigmasterol and cholesterol, respectively, and to study the thermodynamic properties of liposomes induced by thermal phase transition. The effects of different sterols on the thermostability of liposomes were compared. Methods: Blank and drug-containing liposomes were prepared by thin-film dispersion method. The thermodynamic parameters such as phase transition temperature and enthalpy of phase transition were determined by differential scanning calorimetry (DSC). Results: The phase transition temperature and phase transition enthalpy of drug-containing liposomes were lower than that of blank liposomes. In the case of the same composition, there is no significant difference between the phase transition temperature and the enthalpy of phase change of liposomal stigmatide and cholesterol liposome. Conclusion: The hydrophobic region of genistein entering the liposome membrane has a hydrophobic interaction with the hydrophobic tail of phospholipid molecule. The thermal stability of liposomes replaced by sterol instead of cholesterol changed little, suggesting that instead of cholesterol, stigmasterol could be used as the membrane of genistein liposomes.