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-  2015 


DOI: 10.3866/PKU.WHXB201509141

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Abstract:

采用薄膜旋转蒸发-超声法分别制备了柠檬酸铁脂质体(FAC-Lip)和血红素铁脂质体(Heme-Lip).通过测定铁脂质体的体外释放,发现两种铁脂质体均具有缓释性,并且Heme-Lip的缓释性比FAC-Lip的好;采用平衡透析法测定了脂质体/水分配系数(P),并考察影响分配系数的因素,初步探讨了FAC和Heme与脂质体膜结合的吉布斯自由能(ΔG),结果发现随着胆固醇含量和药脂比例的增加, P先增大后减小,当P最大时,药物与磷脂膜的氢键及静电作用力最大;在透析平衡时,计算得到了FAC-Lip和Heme-Lip中药物与脂质体膜层之间的吉布斯自由能分别为-12.7和-18.2 kJ·mol-1.
Ferric citrate liposomes (FAC-Lip) and heme liposomes (Heme-Lip) were successfully prepared by a rotary-evaporated film-ultrasonication method. The release of iron liposomes were studied in vitro, and results showed that both iron liposomes had sustained-released properties, with Heme-Lip showing superior sustained-released over FAC-Lip. The liposome/water partition coefficients (P) were determined by equilibrium dialysis and the influences on P were evaluated, as well as the binding Gibbs free energy between FAC (Heme) and liposome. The results show that P initially increased and then decreased with increasing cholesterol content and the ratio of lipid to drug. The hydrogen and electrostatic interactions were largest when P was at its maximum. At the dialysis equilibrium, the binding Gibbs free energies (ΔG) of FAC-Lip and Heme-Lip were -12.7 and -18.2 kJ·mol-1, respectively

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