[关键词]
[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24 h累积体外透过量分别为137.36、10.25 μg/cm2。与微乳相比,微针辅助条件下微乳组可将葛根素在24 h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(Cmax)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(5 021.45±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Cmax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Cmax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。
[Key word]
[Abstract]
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) of puerarin 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 Cmax 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 of puerarin 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.
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[基金项目]
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)