Purpose

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).

Methods

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/cm² 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/cm²) and on-off current dosing pattern (1 h/3 h, 0.5 h/3.5 h, and 0.2 h/3.8 h).

Results

Both 6- and 12-cycle PDC iontophoresis protocols provided modulation of the permeation profile but delivered smaller amounts of PXCl (396 and 400 μg/cm², respectively) as compared with continuous DC iontophoresis (482 μg/cm²) at 24 h after 0.5 mA/cm² and 180 mA/cm² × min current dose application. Increasing applied current density from 0.1 to 0.5 mA/cm² increased the PDC iontophoretic flux of PXCl linearly from 5.3 to 14.6 μg/cm²·h (R² = 0.887). Varying the current level and duration but at the same applied current dose (36 mA/cm² × 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/cm²).

Conclusions

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.

中文翻译：

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脉冲直流电对普拉克索体外经人表皮膜离子电渗输送的影响

目的

脉冲直流 (PDC) 离子电渗疗法通过允许皮肤去极化，被建议提供更有效的离子传输，但其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。本研究检验了 PDC 离子电渗疗法对二盐酸普拉克索 (PXCl) 透皮给药的影响。

方法

使用连续直流电 (DC) 和 6 和 12 周期 PDC 离子电渗疗法（0.5 mA/cm ²和总应用持续时间 6 小时），在体外进行 PXCl 从 pH 7.0 溶液穿过人表皮膜的离子电渗输送。研究了 PDC 离子电渗疗法的不同参数，包括电流密度（0.1、0.2 和 0.5 mA/cm ²）和开关电流剂量模式（1 h/3 h、0.5 h/3.5 h 和 0.2 h/3.8 h）。

结果

与连续 DC 离子电渗疗法 (482 μg/cm ² )相比，6 循环和 12 循环 PDC 离子电渗疗法均提供了渗透曲线的调节，但在 24 小时后提供了更少量的 PXCl（分别为396 和 400 μg/cm ²）0.5 mA/cm ² 和 180 mA/cm ²  × min 电流剂量应用。将施加的电流密度从 0.1 增加到 0.5 mA/cm ²使 PXCl 的 PDC 离子电渗通量从 5.3 线性增加到 14.6 μg/cm ² ·h (R ²  = 0.887)。改变电流水平和持续时间，但施加相同的电流剂量 (36 mA/cm ² × min)，PDC 离子电渗疗法在 24 小时内递送的 PXCl 总量与所研究的开关剂量模式无关 (114–128 μg/cm ² )。

结论

结果表明，在所研究的条件下，与连续 DC 离子电渗疗法相比，PDC 离子电渗疗法在控制其渗透方面有利于 PXCl 的透皮递送，但不会增强离子电渗疗法的传输。