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通过电穿孔实现芬太尼的经皮给药。I. 电学因素的影响。

Transdermal delivery of fentanyl by electroporation. I. Influence of electrical factors.

作者信息

Vanbever R, LeBoulengé E, Préat V

机构信息

Université catholique de Louvain, Unité de Pharmacie Galénique, Brussels, Belgium.

出版信息

Pharm Res. 1996 Apr;13(4):559-65. doi: 10.1023/a:1016093920875.

Abstract

PURPOSE

Electroporation, a method of reversibly permeabilizing lipid bilayers by the application of an electric pulse, has been shown to induce increased transdermal passage of molecules. The aim of the present report was to study in vitro with hairless rat skin the potential of electroporation for transdermal delivery of fentanyl.

RESULTS

The application of electric pulses can strongly promote transdermal delivery of fentanyl compared to passive diffusion through untreated skin. We also point out that the choice of the waveform of the electric pulses is important: at the same applied energy, a few exponentially-decaying (ED) pulses increased fentanyl permeation more than a few square-wave pulses and to the same extent as the repeated application of higher voltage-shorter duration ED pulses. A factorial design showed that the voltage, duration, and number of ED pulses allowed control of the quantity of drug transported through the skin.

CONCLUSIONS

Skin electroporation could be a good way to improve the transdermal diffusion of fentanyl.

摘要

目的

电穿孔是一种通过施加电脉冲使脂质双层可逆性通透的方法,已被证明可增加分子的经皮透过。本报告的目的是在无毛大鼠皮肤上进行体外研究,以探讨电穿孔用于芬太尼经皮给药的潜力。

结果

与通过未处理皮肤的被动扩散相比,施加电脉冲可强烈促进芬太尼的经皮给药。我们还指出,电脉冲波形的选择很重要:在相同的施加能量下,几个指数衰减(ED)脉冲比几个方波脉冲更能增加芬太尼的渗透,且与重复施加更高电压 - 更短持续时间的ED脉冲的效果相同。析因设计表明,ED脉冲的电压、持续时间和数量可控制透过皮肤转运的药量。

结论

皮肤电穿孔可能是改善芬太尼经皮扩散的一种好方法。

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