高乌甲素脂质体凝胶制备工艺筛选实验研究

Study on the experiment for screening preparation process of lappaconitine liposome gel

目的:研究乙醇注入法制备高乌甲素脂质体凝胶的工艺。方法:采用单因素实验分析药脂比、磷脂胆固醇比、水化液pH、水化温度筛选影响包封率及载药量的因素,再采用正交试验优选最佳处方;制备得到高乌甲素脂质体后,单因素实验筛选最佳卡波姆用量及pH,得到最适宜脂质体凝胶配方。结果:采用正交试验法确定高乌甲素脂质体最佳处方工艺组合为卵磷脂:胆固醇为6∶1、药脂比为1∶10、水化温度为55℃,水化液pH值为7.0,该处方制备的脂质体包封率高,粒径分布均匀;当卡波姆-940用量为1%、在pH 6~7时,所制备的高乌甲素脂质体凝胶易涂布、黏度适宜。结论:制备的高乌甲素脂质体凝胶工艺简单可行,包封率较高,可以进一步研究。

OBJECTIVE To study the preparation of lappaconitine liposome gel by ethanol injection.METHODS The factors affecting entrapment efficiency and drug loading were analyzed by single factor test,including the ratio of drug to lipid,the ratio of phospholipid to cholesterol,the pH of the hydration solution and the hydration temperature,and then orthogonal test was used to select the optimal prescription.After preparing the lappaconitine liposome,the optimal carbomer dosage and pH were screened by single factor test to obtain the most suitable liposome gel formula.RESULTS The best prescription process combination of lappaconitine liposome was determined by orthogonal test:lecithin:6∶1,the ratio of drug to lipid was 1∶10,the hydration temperature was 55℃,and the pH of hydration solution was 7.0.The liposome prepared by the prescription has high encapsulation efficiency and uniform particle size distribution.When the carbomer-940 dosage is 1%and the pH is 6-7,the prepared lappaconitine liposome gel was easy to apply and had a suitable viscosity.CONCLUSION The prepared lappaconitine liposome gel process is simple and feasible with a high encapsulation efficiency,which can be further studied.