Fukushima S, Kishimoto S, Horai S, Miyawaki K, Kamiyabu S, Kamata Y, Yamaoka Y, Takeuchi Y
Department of Pharmaceutics, Faculty of Pharmaceutical Science, Kobe Gakuin University, Japan.
Biol Pharm Bull. 2001 Sep;24(9):1027-31. doi: 10.1248/bpb.24.1027.
Transdermal enhancement effects of electroporation applied only on the stratum corneum by two electrode types, the stamp-type electrode and the frog-type electrode, were investigated in vitro using excised rat skin. Carboxyfluorescein (CF) was selected as a model compound. The excised skin was set in a Franz type diffusion cell and a square wave electric pulse was applied to the stratum corneum under various electric pulse conditions. We determined the permeability of CF to the receptor compartment under these conditions. Voltage, electric pulse length, and number of electric pulses, were varied from 10 to 1000 V, 50 micros to 15 ms and 5 to 30 pulses, respectively. Flux rate was enhanced as the electric pulse condition strengthened. However, the maximum value was attained in the flux rate, above which no increase was observed despite strengthening of the electric pulse. Although at low electric pulses, the enhancement effect of the frog-type electrode was superior to that of the stamp-type electrode, the maximum flux rates were the same. These results indicate that electroporation on the stratum corneum using the stamp-type electrode or frog-type electrode, is useful for transdermal drug delivery.
使用切除的大鼠皮肤在体外研究了仅通过两种电极类型(印章型电极和蛙型电极)对角质层施加电穿孔的透皮增强效果。选择羧基荧光素(CF)作为模型化合物。将切除的皮肤置于Franz型扩散池中,并在各种电脉冲条件下对角质层施加方波电脉冲。我们测定了在这些条件下CF向接受室的渗透率。电压、电脉冲长度和电脉冲数分别在10至1000 V、50微秒至15毫秒和5至30个脉冲之间变化。通量率随着电脉冲条件的增强而增加。然而,通量率达到最大值后,尽管电脉冲增强,通量率也不再增加。虽然在低电脉冲时,蛙型电极的增强效果优于印章型电极,但最大通量率是相同的。这些结果表明,使用印章型电极或蛙型电极对角质层进行电穿孔,对于透皮给药是有用的。