水杨酸甲酯六角相液晶的处方筛选与体外透皮研究

Preparation and in vitro transdermal delivery of methyl salicylate-loaded hexagonal liquid crystal

目的优选出水杨酸甲酯六角相液晶的最优处方,并考察所制备的水杨酸甲酯六角相液晶的体外透皮性能。方法以植烷三醇为基质,采用自乳化法制备水杨酸甲酯六角相液晶;以累积渗透量为指标,采用单因素考察法优化处方;通过偏光显微镜和小角度X射线散射仪对制备的水杨酸甲酯六角相液晶进行表征;并采用改良Franz扩散池考察水杨酸甲酯六角相液晶的透皮性能。结果水杨酸甲酯六角相液晶最佳处方为植烷三醇66%,水22%,水杨酸甲酯12%;所制得的水杨酸甲酯六角相液晶为六角相;体外透皮实验显示,水杨酸甲酯六角相液晶的累积渗透量是市售复方水杨酸甲酯软膏的2.76倍。结论优选的水杨酸甲酯六角相液晶可显著提高水杨酸甲酯的透皮性能,为水杨酸甲酯六角相液晶的进一步研究提供参考依据。

Objective To optimize the formulation of methyl salicylate-loaded hexagonal liquid crystal and investigate the in vitro trans-dermal delivery properties of the optimal formulation. Methods The methyl salicylate-loaded hexagonal liquid crystal was formulated via self-emulsifying based on phytantriol. Drug-loading rate and penetration enhancers were investigated while accumulative permeation amount （Qn） used as the index. CPLM and SAXS were utilized in characterization of the optimal formulation. The in vitro transdermal delivery was performed by Franz diffusion cells. Results The optimized preparation （ phytantriol/methyl salicy late/wa te r,66？ 1 2 -2 2 , w/w/w） was proved a hexagonal phase,the Qn of methyl salicylate-loaded hexagonal liquid crystal was 2. 76 times higher than that of ointment commercially available. Conclusion The developed hexagonal liquid crystal significantly enhanced the penetration of methyl salicylate in vitro, which, was a promising carrier for transdermal delivery of methyl salicylate.