Development of sinomenine hydrochloride-loaded polyvinylalcohol/maltose microneedle for transdermal delivery

The microneedle array of sinomenine hydrochloride(SH) was prepared by casting method using polyvinyl alcohol (PVA) and maltose (MT). The microneedle array was inserted into the foil and rat’s skin to evaluate the mechanical property. Its in vitro permeation was examined to calculate the accumulation osmolality and permeation rate. In the in vivo transdermal penetration studies, blood samples were obtained to determine the concentrations of SH in plasma after administrated by SH-loaded MT/PVA microneedle array and SH-loaded hydrogel, and the pharmacokinetic parameters were determined. The average grade of irritation was calculated to evaluate the level of irritation. The developed microneedle arrays were strength enough to insert into the foil and rat’s skin. The permeation rate was stable within 48h after microneedle array administration in vitro. The in vivo transdermal penetration studies of SH-loaded hydrogel and SH-loaded MT/PVA microneedle arrays showed the date of in vivo pharmacokinetic parameters. Such as, their AUC0−t and AUC0−inf were 5.38 ± 0.53 μg (mL h)−1 and 35.35 ± 1.27 μg (mL h)−1, 5.75 ± 0.49 μg (mL h)−1 and 45.36 ± 2.36 μg (mL h)−1, respectively. Skin irritation test showed that microneedle array has slight irritation to the rat skin. These results indicated that the SH-loaded PVA/MT microneedle array may be an ideal approach to achieve a transdermal delivery for SH.

The blood concentration of SH-loaded MT/PVA microneedle arrays group (◆)was lower than that of SH-loaded hydrogel group (●) within the first 8 hours, but gradually increased from 8 hours. It exhibited higher from 8 to 48 hours versus hydrogel group. The MT/PVA microneedle arrays may be an ideal approach to achieve a transdermal delivery system for SH.Figure optionsDownload as PowerPoint slide