Padula Cristina, Sartori Francesca, Marra Fabio, Santi Patrizia
Dipartimento Farmaceutico, University of Parma, Parco Area delle Scienze, 43100 Parma, Italy.
Pharm Res. 2005 Sep;22(9):1519-24. doi: 10.1007/s11095-005-5884-1. Epub 2005 Aug 24.
The aim of this work was to explore the effect of iontophoresis on acyclovir (ACV) accumulation and permeation. In particular, the objectives were to check the efficacy of the transport mechanisms, electromigration and electrosmosis, on drug accumulation.
Permeation experiments were performed in vitro, using rabbit ear skin as barrier, from donor solutions at pH 3.0, 5.8, and 7.4. At the end of the experiments, drug accumulation in epidermis and dermis was measured. Anodal and cathodal iontophoresis were applied at pH 3.0, whereas only anodal iontophoresis was used at pH 5.8 (current densities 0.06--0.50 mA/cm(2)) and 7.4.
Cathodal iontophoresis was more efficient than anodal iontophoresis on ACV permeation across the skin at pH 3.0. At pH 5.8, ACV flux and accumulation increased with current density during anodal iontophoresis. At pH 7.4, anodal iontophoresis produced a remarkable increase of flux and a modest increase of accumulation. Overall, anodal flux increased as the pH of the donor solution was increased as a result of the increase of the skin net negative charge.
From the results obtained in the present work, it can be concluded that iontophoresis application increases ACV flux and, to a limited extent, accumulation in the skin.
本研究旨在探讨离子电渗疗法对阿昔洛韦（ACV）蓄积和渗透的影响。具体而言，目的是检验电迁移和电渗这两种转运机制对药物蓄积的效果。
采用兔耳皮肤作为屏障进行体外渗透实验，供体溶液的pH值分别为3.0、5.8和7.4。实验结束时，测量表皮和真皮中的药物蓄积量。在pH值为3.0时采用阳极和阴极离子电渗疗法，而在pH值为5.8（电流密度0.06 - 0.50 mA/cm²）和7.4时仅采用阳极离子电渗疗法。
在pH值为3.0时，阴极离子电渗疗法在促进ACV透过皮肤方面比阳极离子电渗疗法更有效。在pH值为5.8时，阳极离子电渗疗法过程中ACV通量和蓄积量随电流密度增加。在pH值为7.4时，阳极离子电渗疗法使通量显著增加，蓄积量适度增加。总体而言，由于皮肤净负电荷增加，供体溶液pH值升高时阳极通量增加。
从本研究获得的结果可以得出结论，离子电渗疗法的应用增加了ACV通量，并在一定程度上增加了其在皮肤中的蓄积量。
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