两种秋水仙碱醇质体的制备及评价

Preparation and Evaluation of Two Kinds of Colchicines Ethosomes

目的比较分别用不饱和磷脂和饱和磷脂为膜材,不同溶剂制得的秋水仙碱醇质体理化特性的差别。方法采用注入法制备秋水仙碱醇质体,正交设计法筛选处方。比较不饱和磷脂与饱和磷脂对其形态学、包封率、稳定性和经皮渗透的累积透过量的影响。结果制备的两种醇质体形状呈圆球形或类圆形,结构完整。含不饱和磷脂醇质体平均粒径为100 nm,粒径分布较窄,包封率达58%;含饱和磷脂醇质体平均粒径为50 nm,粒径分布较宽,包封率达63%;含饱和磷脂醇质体的稳定性受高温和光照的影响都要明显小于含不饱和磷脂醇质体。含饱和磷脂醇质体的药物单位面积累计透过量和药物在皮肤中的滞留量也明显高于含不饱和磷脂醇质体的透过量和滞留量。结论经初步评价,用氢化磷脂、乙醇和Tween 80所制备的秋水仙碱醇质体在包封率、稳定性和经皮渗透的累积透过量方面明显优于用大豆磷脂和异丙醇所制备的秋水仙碱醇质体。

OBJECTIVE To compare the difference of characteristics of colchicines ethosomes that made by soybean phospholipids or hydrogenated phosphatidylcholines.METHODS Colchicines ethosomes were prepared by injection method.The best prescription were screened out by an orthogonal design test.To compare the influence of soybean phospholipids and hydrogenated phosphatidylcholines at morphology、entrapment efficiency,stability,respectively.The difference of transdermal penetration rate were also studied.RESULTS The ethosomes with spherical or ellipsoidal shape.The particle size of colchicines ethosomes made by soybean phospholipids were 100 nm with a narrow range of size distribution.The entrapment efficiency were 58%.The particle size of colchicines ethosomes made by hydrogenated phosphatidylcholines were 50 nm with a wide range of size distribution.The entrapment efficiency were 63%.No obvious changes were found in all the indices in the stability test of the ethosomes made by hydrogenated phosphatidylcholines.Better than the ethosomes made by soybean phospholipids.So did in the transdermal penetration test.CONCLUSION By primary study,colchicines ethosomes made by hydrogenated phosphatidylcholines is better than colchicines ethosomes made by soybean phospholipids at entrapment efficiency、stability、 transdermal penetration test.