桂皮醛脂质体制备工艺研究

Preparation technology of Cinnamaldehyde liposomes

[目的]建立桂皮醛脂质体包封率的测定方法,以包封率与载药量为指标,研究桂皮醛脂质体的制备工艺及最优处方。[方法]采用超滤法分离桂皮醛脂质体中游离的药物,高效液相色谱法测定药物含量,计算桂皮醛脂质体包封率;采用薄膜-超声分散法制备桂皮醛脂质体;以胆固醇与卵磷脂质量的比例、桂皮醛与辅料质量的比例、水化温度、磷酸缓冲盐p H值为影响因素,采用正交法进行处方筛选。[结果]桂皮醛脂质体优化后的处方为:胆固醇与卵磷脂质量比为1∶8,桂皮醛与胆固醇卵磷脂总量比为1∶12,pH为7.0,水化温度为55℃,在此条件下制备的桂皮醛脂质体包封率为82.71%,载药量为5.32%。[结论]实验制备的桂皮醛脂质体方法简单可行,包封率较高,对桂皮醛改善皮肤光老化提供一定的指导意义。

[Objective]To establish a method for the determination of the encapsulation rate of cinnamaldehyde liposomes,and to study the preparation technology and optimal prescription of Cinnamaldehyde liposome using encapsulation rate and loading dose as index.[Methods]The ultrafiltration was employed to isolate free cinnamaldehyde and the content of cinnamaldehyde was determined by HPLC to calculate the encapsulation rate of cinnamaldehyde liposomes.The cinnamicaldehyde liposomes were prepared by thin film-ultrasonic dispersion method.The ratio of cholesterol to lecithin,the proportion of total cinnamicaldehyde and cholesterol lecithin,the hydration temperature,and the pH value of phosphoric acid buffer salt were selected as influence factors,the prescription was screened by orthogonal method.[Results]The optimized formula Cinnamaldehyde Liposome was as follows:the quality ratio of cholesterol and lecithin was 1∶8,the total ratio of cinnamaldehyde and cholesterol lecithin was 1∶12,pH 7.0,the hydration temperature was 55℃,the encapsulation rate of Cinnamaldehyde Liposome was 82.71%and the dose was 5.32%.[Conclusion]The preparation of cinnamaldehyde liposome is simple and feasible,and with a high encapsulation rate,which can provide further guidance for improving the skin aging of cinnamaldehyde.