滚轮微针技术对黄柏提取物乳膏中盐酸小檗碱经皮渗透的促进作用

Promoting Effect of Microneedle-roller Technology on Percutaneous Permeation of Berberine Hydrochloride from the Cream of Cortex Phellodendri Extracts

采用回流法制备黄柏提取物,再制成o/w型乳膏。用HPLC法测定盐酸小檗碱的含量。以离体裸鼠皮肤为屏障,用改良Franz扩散池法考察乳膏中盐酸小檗碱的体外透皮性能,探讨滚轮微针技术对黄柏提取物乳膏中盐酸小檗碱体外经皮渗透行为和皮肤滞留量的影响。结果显示,不用或采用微针处理组乳膏中盐酸小檗碱12 h的累积渗透量为（0.161±0.008）、（0.978±0.034）mg/cm^2,经皮渗透速率为（0.035±0.007）、（0.197±0.018）mg·cm^-2·h^-1,皮肤滞留量为（0.373±0.021）、（1.364±0.342）mg/cm^2。可见,滚轮微针技术能显著提高外用黄柏提取物乳膏中盐酸小檗碱的经皮渗透量（P〈0.05）,增加皮肤内药物滞留量（P〈0.05）。

An o/w type cream loaded with the extract of Cortex Phellodendri obtained by reflux method was prepared. The concentration of berberine hydrochloride （1） was determined by HPLC method. The in vitro permeation characteristics through excised nude mouse skin were investigated by modified Franz diffusion cells. The effects of microneedle-roller on the percutaneous penetration of 1 from the cream and the retention amount of 1 in skin were discussed. The results showed that the cumulative permeation amounts at 12 h in the groups without or with microneedle- roller skin treatment were （0.161±0.008） and （0.978±0.034）mg/cm^2, the percutaneous penetration rates were （0.035±0.007） and （0.197±0.018）mg·cm^-2h^-1, while the retention amounts of 1 in the two groups were （0.373±0.021） and （1.364±0.342）mg/cm^2. It indicated that microneedle-roller could significantly increase the percutaneous penetration amount of i and its retention amount in skin （P〈0.05）.