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以离体小鼠皮肤为屏障、人参皂苷Rg_1为指标,考察了11种咪唑类离子液体对促进三七总皂苷经皮渗透的影响。激光共聚焦显微镜(CLSM)考察结果表明,咪唑类离子液体能促进荧光素钠在小鼠皮肤中的渗透深度和渗透量。继而初步考察了咪唑类离子液体的构效关系。结果表明,离子液体的促渗作用受取代基链长、数目和类型的影响。双取代离子液体比单取代和三取代离子液体促渗作用强;在双取代离子液体结构引入羟基基团可增大促渗作用,而引入羧基基团则减弱促渗作用;双取代促渗剂与常用促渗剂(月桂氮酮、N-甲基-2-吡咯烷酮和1,2-丙二醇)的促渗作用相当,甚至更优。
In vitro mouse skin as a barrier, ginsenoside Rg_1 as an indicator to investigate the impact of 11 kinds of imidazole ionic liquids to promote Panax notoginseng transdermal penetration. Confocal laser scanning microscopy (CLSM) results showed that imidazole ionic liquids can promote sodium penetration in the mouse skin and penetration of sodium fluorescein. Then the structure-activity relationship of imidazole ionic liquids was first investigated. The results showed that the ionic liquid promoted the penetration by the substituent chain length, number and type. Disubstituted ionic liquid is more effective than monosubstituted and trisubstituted ionic liquids. The introduction of hydroxyl groups in the disubstituted ionic liquid can increase the permeation enhancement effect, while the introduction of carboxyl groups can reduce the effect of osmotic penetration. With the commonly used penetration enhancers (Azone, N-methyl-2-pyrrolidone and 1,2-propanediol) permeability effect is equivalent to, or even better.