去甲斑蝥素脂质体的制备及其体外释放特性的研究

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。

Studies on Preparation and Drug Release Characteristics of Norcantharidin Liposomes in Vitro

Objective： To Prepare the Norcantharidin（NCTD）liposome and to discuss its character. Methods： NCTD liposornes were obtained using reverse film evaporation technique and the best recipe was selected using orthogonal design optimizing recipe process. The In vitro release of NCTD from liposomes was evaluated using the balance dialysis method. Results： The results were as follows： Influence encapsulation efficiency and particle size factor, in turn, for A〉C〉B, the factors combination is phospholipid-drug quality ratio of 10：1, phosphatide-cholesterol mass ratio of 5： 1, ultrasonic frequency of 10 times. The encapsulation efficiency of NCTD-liopsomes was （90.50±2.40）nm and the encapsulation efficiency was （34.7± 1.3）%.The experimental results show that the slow release effect was obvious.Conclusion： NCTD liposomes obtained using reverse film evaporation method are stable and have significant in vitro slow release characteristics.