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目的:制备去甲斑蝥素(NCTD)脂质体并探讨其药剂学性质。方法:采用逆向薄膜蒸发法制备NCTD-脂质体,并采用正交设计优化处方工艺,利用平衡透析法对含NCTD的载药脂质体进行体外释放的评价。结果:影响包封率和粒径的因素,依次为A>C>B,各因素组合以A2C1B2最佳,即磷脂-药物质量比为10∶1,磷脂-胆固醇质量比为5∶1,超声次数为10次;制得的NCTD-脂质体的粒径为(90.50±2.40)nm,包封率为(34.7±1.3)%,实验结果显示缓释效果明显。结论:逆向薄膜蒸发法制备的NCTD-脂质体,其性质稳定,具有显著的体外缓释特性。
OBJECTIVE: To prepare norcantharidin (NCTD) liposome and to investigate its pharmacological properties. Methods: NCTD-liposomes were prepared by reverse membrane evaporation method. Orthogonal design was used to optimize the formulation process. The release of NCTD loaded liposomes in vitro was evaluated by equilibrium dialysis. Results: The factors influencing the entrapment efficiency and particle size were A> C> B, the best combination of the two factors was A2C1B2, the phospholipid-drug mass ratio was 10:1, the mass ratio of phospholipid-cholesterol was 5:1, The number of NCTD-liposomes was (90.50 ± 2.40) nm, the entrapment efficiency was (34.7 ± 1.3)%. The experimental results showed that the sustained-release effect was obvious. CONCLUSION: NCTD-liposomes prepared by reverse-phase thin-film evaporation have stable properties and have significant sustained-release characteristics in vitro.