改良-薄膜分散法优化栀子提取物类脂质体的制备工艺

Optimization of the gardenia extract liposome based on Modified-film dispersion method

目的优选栀子提取物类脂质体粉末的制备工艺并进行质量评价。方法采用改良-薄膜分散法制备栀子提取物类脂质体,结合单因素考察法和L_9(3~4)正交试验法,以包封率为考察指标,考察表面活性剂HLB值、载体与药物比值、表面活性剂与胆固醇摩尔比、水合介质pH、温度及时间等对类脂质体包封率的影响。采用喷雾干燥法制备类脂质体粉末,并对其性状、粒径、临界相对湿度、载药量进行质量评价。结果最佳制备工艺为以Span 60和Tween 80为表面活性剂,HLB值为8,载体与药物比值为1∶0. 75,表面活性剂与胆固醇的摩尔比为1∶1. 2,水合介质为p H7. 6;类脂质体喷雾干燥后为淡黄色至黄色粉末。结论所得类脂质体呈圆形或椭圆形,粒径较小、载药量高、工艺稳定。

OBJECTIVE To optimize the preparation process parameters of the gardenia extract liposome powder based on the modified-film dispersion method,and the quality is also evaluated.METHODS The gardenia extract liposome was prepared using Modified-film dispersion method.Combined with the single factor method and L9(34)orthogonal test method,the encapsulation efficiency was used to investigate the HLB value,carrier-to-drug ratio and surface activity.The effects of the molar ratio of the agent to cholesterol,the p H of the hydration medium,the temperature and the time on the encapsulation efficiency of the liposome were also tested.Lipid-like powders were prepared by spray drying method,and their properties,particle size,critical relative humidity and drug loading were evaluated.RESULTS The best preparation process is Span 60 and Tween 80 as surfactants,HLB value of 8,the ratio of carrier to drug as 1∶0.75,the molar ratio of surfactant to cholesterol is 1∶1.2 and the p H of hydration medium as 7.6.The plastid spray is dried to a pale yellow to yellow powder.CONCLUSION The obtained liposome is round or elliptical and has a small particle size,a high drug loading amount and a stable process.