[关键词]
[摘要]
目的 考察咪唑类离子液体([BMIM][Cl])对人参皂苷Rh1(Rh1)的体外经皮促渗作用及促渗机制。方法 以小鼠皮和猪皮为皮肤模型,以油酸、薄荷脑、肉豆蔻酸异丙酯和离子液体 [BMIM][Cl] 为促渗剂,采用摇瓶法测定Rh1在各促渗剂-水溶液中的溶解度;采用Franz扩散池进行体外经皮渗透实验;采用傅里叶转换红外线光谱(FTIR)法测定研究离子液体的经皮促渗机制。结果 与其他促渗剂相比,5%的 [BMIM][Cl] 能够显著增加Rh1在水中的饱和溶解度;同时对Rh1的体外经皮渗透有显著的促进作用。FTIR的研究结果表明,[BMIM][Cl] 能够改变小鼠皮肤角质层结构。结论 [BMIM][Cl] 作为一种新型的经皮吸收促渗剂,在外用制剂领域有潜在的使用价值。
[Key word]
[Abstract]
Objective To evaluate the in vitro percutaneous absorption profiles of ginsenoside Rh1 using ionic liquids [BMIM][Cl] as a novel permeation enhancer and to investigate the mechanism. Methods Mice skin and porcine skin were used as skin model. Oil acid, isopropyl myristate, and menthol were used as comparing skin enhancers. The solubility of Rh1 (with or without enhancer) in water was measured by shake-flask method. Skin permeation experiment was performed using Franz diffusion cells. Skin structure change after treatment of [BMIM][Cl] was measured by FTIR. Results By comparing with commonly used enhancers, 5% [BMIM][Cl] significantly increased the solubility of Rh1 and gave an excellent improvement on the skin penetrability of Rh1. The FTIR results suggested that [BMIM][Cl] accelerated the drug skin permeation by disrupting the lipid bilayer of skin stratum corneum. Conclusion [BMIM][Cl] can serve as a novel skin permeation enhancer, and show a broad application prospect in transdermal drug delivery system.
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[基金项目]
云南省科技厅人才培养项目(kksy201326118)