天麻素脂质体的制备及其结构表征

Preparation and structure characterization of gastrodine liposomes

目的研究天麻素脂质体的最佳制备工艺,并表征其结构。方法采用薄膜—超声法制备。以包封率为指标,卵磷脂与胆固醇之间的质量比、油水相的体积比和超声时间为考察因素,采用L9（3^4）正交试验法优化制备工艺;显微镜下观察脂质体的形态、粒径大小和分布,并测定其包封率和稳定性。结果回归方程式为Y=239.75X＋0.0207（n=5）,R^2=0.9996,在0.002-0.010 mg/m L范围内具有良好的线性关系。最佳工艺为：卵磷脂与胆固醇的质量比为4∶1、水油相的体积比为3∶1、超声时间控制为60 min;脂质体呈现类球形或椭圆形,形态规则、大小均匀;平均包封率为60.65%,平均粒径分布为327 nm,稳定性良好。结论优选后的制备工艺稳定,所需设备简单,包封率较高,粒径较均匀,可适用于包埋水溶性药物。

Objective To study the optimum preparation process of gastrodin liposome, characterization its structure.Methods Perpared gastrodin liposome with film-ultrasonic method.The entrapment efficiency as index, quality between lecithin and cholesterol ratio, oil-water phase volume ratio and ultrasonic time as factors by L9 （3^4 ） orthogonal test to optimize the preparation process.Observed the liposome morphology, particle size and distribution under the microscope, and determined the entrapment efficiency and stability.Results Regression equation was Y=239.75 ＋0.0207X（n=5）, R^2 =0.9996, 0.002 to 0.010 mg/mL had a good linear relationship.The optimum of preparation process： lecithin and cholesterol quality ratio was 4：1, water and oil phase volume ratio of 3：1, ultrasonic time control for 60 min;Liposomes showed spherical or oval shape, regular shape, uniform size.The average entrapment efficiency was 60.65%, the average particle size distribution at 327 nm, and it had good stability.Conclusion The preparation of gastrodine liposome has advantages of simple, higher entrapment efficiency and even particle size.The method can be used for embedded water-soluble medicine.