微针辅助条件下葛根素微乳的经皮吸收研究  

Enhancement of transdermal absorption of puerarin by microneedle-assisted microemulsion

作　　者：晏雨露 徐驿 赵继会[1] 冯年平[1] YAN Yu-lu XU Yi ZHAO Ji-hui FENG Nian-ping(Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China)

机构地区：[1]上海中医药大学,上海201203

出　　处：《中草药》2017年第1期95-101,共7页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金资助项目(81573619);上海中医药大学预算内科研项目(2015YSN09)

摘　　要：目的采用微针辅助促进难溶药物葛根素微乳经皮吸收。方法以葛根素微乳作为对照,通过体内、外实验方法评价微针辅助促进葛根素微乳经皮吸收的作用。结果大鼠体外透皮实验中,微针辅助条件下葛根素微乳组和葛根素微乳组的24h累积体外透过量分别为137.36、10.25μg/cm^2。与微乳相比,微针辅助条件下微乳组可将葛根素在24h内透过离体大鼠皮肤的累积体外透过量提高12.4倍。大鼠在体微透析实验中,微针辅助条件下葛根素微乳组和葛根素微乳组的葛根素峰浓度(C_(max))分别为(713.51±72.23)ng/mL和(108.56±5.72)ng/mL;大鼠在体微透析接收液中葛根素浓度-时间曲线下面积(AUC)分别为(5021.45±547.09)ng·h/L和(622.36±41.21)ng·h/L。与微乳相比,微针辅助条件下微乳组可将葛根素在大鼠在体微透析实验中C_(max)和AUC分别提高5.57倍和7.07倍。大鼠体内药动学实验中,微针辅助条件下葛根素微乳组在大鼠血浆中的C_(max)为(234.35±25.02)ng/mL,AUC为(3047.13±486.51)ng·h/L;葛根素微乳组在大鼠血浆中的药物浓度未检出。结论微针辅助条件下微乳可明显促进葛根素经皮吸收。本研究为葛根素新型经皮给药系统的研究奠定了初步的基础。Objective To enhance the percutaneous absorption of puerarin, a water insoluble drug, using microneedle-assisted microemulsion. Methods With puerarin microemulsion as control, in vivo and in vitro experiments were conducted to evaluate permeation amount of puerarin, which was increased by 12.4 times using microneedle-assisted microemulsion. In rat skin microdialysis experiments in vivo, the peak concentration （Cmax） of puerarin in reception medium was （713.51 ± 72.23） ng/mL for microneedle- assisted microemulsion group and （108.56 ± 5.72） ng/mL for microemulsion group; The areas under concentration-time curves （AUCs） ofpuerarin were （5 021.45 ± 547.09） ng.h/L for microneedle-assisted microemulsion group and （622.36±41.21） ng.h/L for microemulsion group, respectively. Compared with microemulsion, the Cm^x and AUC of puerarin in rat skin microdialysis experiments in vivo were increased by 5.57 times and 7.07 times, respectively, when microneedle-assisted microemulsion was used. In pharmacokinetic experiments in rats, the Cmax and AUC ofpuerarin in rat plasma were （234.35 ± 25.02） ng/mL and （3 047.13 ± 486.51） ng.h/L for the microneedle-assisted microemulsion group. The puerarin concentration in rat plasma for the microemulsion group were lower than the limit of detection. Conclusion The transdermal absorption of puerarin could be enhanced obviously using microneedle-assisted microemulsion. By conducting this research, a preliminary foundation is laid for the development of novel delivery systems for puerarin.

关 键 词：葛根素 微乳 微针 体外透皮 在体微透析 药动学 

分 类 号：R283.6[医药卫生—中药学]