Akomeah Franklin K, Martin Gary P, Brown Marc B
King's College London, Pharmaceutical Sciences Division, Franklin-Wilkins Building, 150 Stamford Street, London SE1 9NH, United Kingdom.
Int J Pharm. 2009 Feb 9;367(1-2):162-8. doi: 10.1016/j.ijpharm.2008.09.041. Epub 2008 Oct 2.
The effect of short-term current application (0.4mA for 10min) on the epidermal transport of two model penetrants (butyl paraben, BP; caffeine, CF) of differing lipohilicity was investigated and compared to that produced by employing an established method of skin penetration enhancement (delipidisation). The aim was to investigate the mechanism of enhancement and route of skin permeation associated with each penetrant and mode of treatment. Franz cell diffusion experiments were conducted using human epidermal sheets and a saturated buffer solution (pH 7.4) of the respective penetrant, at a pseudo-finite dose. The effects of electrode type (anodal or cathodal) and current treatment protocol (iontophoresis or post-iontophoresis) on solute permeation was found not to be significantly different (p>0.05). However, in contrast to BP, a significant increase in CF transport (3-5-fold) relative to untreated skin was observed when iontophoretic/post-iontophoretic treatment protocols were employed. The use of delipidised skin was found to enhance the permeation of both model penetrants to an extent greater than iontophoresis (BP: 3-fold; CF: 24-fold). Results from this study suggest that the permeation of the more hydrophilic CF across the skin, unlike BP, may involve multiple pathways. Electroperturbation of the epidermis was confirmed as the mechanism responsible for enhancing CF transport when electrical current was applied. Iontophoretic and post-iontophoretic enhancement may serve as a potential approach to enhance the topical delivery of CF in cosmetic or dermatological treatments (anti-cellulite, viral infections and psoriasis).
研究了短期施加电流（0.4mA，持续10分钟）对两种亲脂性不同的模型渗透剂（对羟基苯甲酸丁酯，BP；咖啡因，CF）经表皮转运的影响，并将其与采用既定的皮肤渗透增强方法（脱脂）所产生的影响进行比较。目的是研究与每种渗透剂和处理方式相关的增强机制及皮肤渗透途径。使用人表皮片和相应渗透剂的饱和缓冲溶液（pH 7.4），以伪有限剂量进行Franz细胞扩散实验。发现电极类型（阳极或阴极）和电流处理方案（离子导入或离子导入后处理）对溶质渗透的影响无显著差异（p>0.05）。然而，与BP不同，当采用离子导入/离子导入后处理方案时，观察到CF的转运相对于未处理皮肤有显著增加（3至5倍）。发现使用脱脂皮肤可使两种模型渗透剂的渗透增强程度大于离子导入（BP：3倍；CF：24倍）。本研究结果表明，与BP不同，亲水性更强的CF经皮肤渗透可能涉及多种途径。当施加电流时，表皮的电扰动被确认为增强CF转运的机制。离子导入和离子导入后增强可作为在化妆品或皮肤病治疗（抗橘皮组织、病毒感染和牛皮癣）中增强CF局部递送的一种潜在方法。
