香豆素-6传递体的变形性与体外透皮性质的相关性研究

Study on the Relationship Between the Deformability of Transfersome Containing Coumarin-6 and Transdermal Permeation Properties in Vitro

目的研究香豆素-6传递体的变形性与体外透皮性质的相关性。方法制备4种不同处方的香豆素-6传递体,采用变形指数D,校正的变形指数Dcor,挤出前后粒径变化RD 3种指标,评价传递体的变形性;以大鼠皮肤作为模型,比较4种处方的药物累积透皮量。结果评价指数D和Dcor显示的变形性顺序为脱氧胆酸钠(TF-SDC)>胆酸钠(TF-SC)>空白(Liposome)>司盘-80(TF-SP80),评价指数RD显示的变形性顺序为TF-SP80>TF-SDC>TF-SC>Liposome;12h累积透皮量的顺序为TF-SDC>TF-SC>Liposome>TF-SP80。结论香豆素-6传递体的3种变形性评价指标中与其体外累积透皮量之间以评价指数D和Dcor的相关性为最佳。

OBJECTIVE To study the relationship between the indexs of the deformability of the different prescription of transfersomes containing coumarin-6 and transdermal permeation properties in vitro. METHODS Four kinds of different pre scription of transfersomes containing eoumarin-6 were prepared by using film dispersion method. The formulation was evalua ted through vesicle size, vesicle size distribution, drug entrapment efficiency, deformability and rat skin permeation amount in vitro. The deformability of vesicles was measured with extrusion method and evaluated by such three different indexes as the deformation index D, the corrected deformation index Door and the index RD. RESULTS The evaluation index D and Door shows that the order of the deformability of four different prescription of transfersomes containing coumarin-6 is sodium deoxycholate （TF-SDC）〉sodium cholate（TF-SC）〉the blank （Liposome）〉span 80（TF-SP80） and the evaluation index RD shows that the deformability order is TF SP80：〉TF-SDC〉TF-SC〉Liposome; the order of cumulative penetration amount of coumarin-6 in 12 h is TF-SDC〉TF-SC〉LiposomC〉TF-SP80. CONCLUSION The evaluation index D and Doorhave the best correlation with the cumulative penetration amount of coumarin-6 in vitro among 3 kinds of deformability index.