Department of Pharmacy, Faculty of Pharmacy, Mahidol University, 447 Sri-Ayuthaya Road, Rajathevi, Bangkok, 10400, Thailand.
Division of Pharmaceutical Sciences, College of Pharmacy, University of Cincinnati, Cincinnati, OH, 45267, USA.
Pharm Res. 2021 Jul;38(7):1187-1198. doi: 10.1007/s11095-021-03055-3. Epub 2021 Jun 16.
Pulsed direct current (PDC) iontophoresis, by allowing skin depolarization, was suggested to provide more efficient ion transport, but the extent of its enhancement effect was unclear. PDC could also offer electric-customized drug delivery. This study examined the effect of PDC iontophoresis on transdermal delivery of pramipexole dihydrochloride (PXCl).
Iontophoretic delivery of PXCl across human epidermal membrane from pH 7.0 solution was conducted in vitro using continuous direct current (DC) and 6- and 12-cycle PDC iontophoresis (0.5 mA/cm and total applied duration of 6 h). Different parameters of PDC iontophoresis were studied, including current density (0.1, 0.2 and 0.5 mA/cm) and on-off current dosing pattern (1 h/3 h, 0.5 h/3.5 h, and 0.2 h/3.8 h).
Both 6- and 12-cycle PDC iontophoresis protocols provided modulation of the permeation profile but delivered smaller amounts of PXCl (396 and 400 μg/cm, respectively) as compared with continuous DC iontophoresis (482 μg/cm) at 24 h after 0.5 mA/cm and 180 mA/cm × min current dose application. Increasing applied current density from 0.1 to 0.5 mA/cm increased the PDC iontophoretic flux of PXCl linearly from 5.3 to 14.6 μg/cm·h (R = 0.887). Varying the current level and duration but at the same applied current dose (36 mA/cm × min), the total amount of PXCl delivered by PDC iontophoresis at 24 h was independent of the on-off dosing pattern studied (114-128 μg/cm).
The results indicate that PDC iontophoresis can benefit transdermal delivery of PXCl in terms of controlling its permeation but does not enhance iontophoretic transport compared to continuous DC iontophoresis under the conditions studied.
脉冲直流（PDC）离子电渗通过使皮肤去极化，被认为可提供更有效的离子传输，但增强效果的程度尚不清楚。PDC 还可以提供电动定制药物输送。本研究考察了 PDC 离子电渗对盐酸普拉克索（PXCl）经皮传递的影响。
在体外使用连续直流（DC）和 6 周期和 12 周期 PDC 离子电渗（0.5 mA/cm 和总应用持续时间 6 小时）从 pH 7.0 溶液中传递人表皮膜中的 PXCl。研究了 PDC 离子电渗的不同参数，包括电流密度（0.1、0.2 和 0.5 mA/cm）和通断电流给药模式（1 h/3 h、0.5 h/3.5 h 和 0.2 h/3.8 h）。
6 周期和 12 周期 PDC 离子电渗方案均提供了渗透谱的调制，但与连续 DC 离子电渗（0.5 mA/cm 和 180 mA/cm×min 电流剂量应用 24 小时后分别为 482μg/cm 和 400μg/cm）相比，输送的 PXCl 量较小（分别为 396μg/cm 和 400μg/cm）。从 0.1 增加至 0.5 mA/cm 增加了 PXCl 的 PDC 离子电渗通量从 5.3μg/cm·h 线性增加至 14.6μg/cm·h（R=0.887）。在相同的应用电流剂量（36 mA/cm×min）下，改变电流水平和持续时间，但在研究的通断给药模式下，PDC 离子电渗传递的 PXCl 总量与给药模式无关（114-128μg/cm）。
结果表明，PDC 离子电渗在控制其渗透方面可以有益于 PXCl 的经皮传递，但在研究条件下与连续 DC 离子电渗相比，并未增强离子电渗传输。
