Enhancement of transdermal absorption of puerarin by microneedle-assisted microemulsion / 中草药

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.