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考察了氨基酸酯离子液体的体外经皮促渗活性,并评价其皮肤刺激性。以13种氨基酸酯离子液体为促渗剂,小鼠皮肤为药物模型,采用Franz扩散池法考察离子液体对模型药物睾酮的促渗作用;采用经皮水分散失速率仪,测定离子液体对皮肤通透性的影响;以荧光素钠为探针,采用荧光共聚焦显微镜,研究离子液体的皮肤促渗强度和促渗深度;最后以大鼠为模型动物,对离子液体的皮肤刺激性进行考察。结果表明,氨基酸离子液体能提高药物的溶解度,并改善皮肤的通透性,从而对睾酮产生促渗作用,促渗比最高可达10.96。经皮水分散失速率和荧光共聚焦显微镜考察结果表明,离子液体能够增强皮肤通透性,如小鼠皮肤经5%[SerC_1]Cl处理1 h,可使荧光渗透深度达到皮下500mm。皮肤刺激性试验中未观察到氨基酸酯离子液体对大鼠皮肤有刺激性,提示其安全性较高。
In vitro transdermal permeation activity of amino acid ester ionic liquids was investigated and their skin irritation was evaluated. Using 13 kinds of amino acid ester ionic liquids as the penetration enhancers and mouse skin as the drug model, the Franz diffusion cell method was used to investigate the effect of the ionic liquid on the testosterone promoting effect of the model drug. The transdermal aqueous dispersion rate meter Permeability of sodium dodecyl sulfate-polyacrylamide gel electrophoresis. Fluorescent confocal microscopy was used to investigate the skin penetration enhancement and penetration enhancement of ionic liquid with sodium fluorescein as probe. Finally, the skin irritation of ionic liquid was investigated using rat as a model animal. The results showed that the amino acid ionic liquid can improve the solubility of the drug and improve the permeability of the skin, thereby promoting the testosterone to promote penetration ratio up to 10.96. Transcutaneous water dispersion rate and fluorescence confocal microscopy results showed that ionic liquids can enhance skin permeability, such as mouse skin treated with 5% [SerC_1] Cl 1 h, the fluorescence penetration depth of subcutaneous 500mm. Amino-ester-based ionic liquids were not observed in skin irritation test irritating to the skin of rats, suggesting that their safety is high.