Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, Mercer University, Atlanta, GA 30341, United States.
Int J Pharm. 2010 Mar 30;388(1-2):24-31. doi: 10.1016/j.ijpharm.2009.12.029. Epub 2009 Dec 16.
The objective of this study was to determine the effect of iontophoresis on the delivery of terbinafine hydrochloride (4%, w/w) into and across hairless rat skin. In vitro skin uptake and permeation studies were performed using Franz diffusion cells. Anodal iontophoresis was applied for 1h at current densities of 0.2, 0.3 and 0.4mA/cm(2). In addition, iontophoresis was applied for 15, 30, 45 and 60min. Studies were conducted in which the formulation was either removed or left in contact with the skin following iontophoresis and then passive delivery was assessed 23h later. Tape stripping and skin extraction were performed to quantify drug levels in the stratum corneum and the underlying skin, respectively. The samples were analyzed using HPLC. The amount of drug delivered into the stratum corneum following iontophoresis was not significantly different from the amount delivered passively (p>0.05). However, drug levels in the underlying skin were significantly higher for the iontophoretic group. The amount of terbinafine delivered into the skin layers was influenced by current density and duration of current application. Leaving the drug formulation in contact with the skin during the post-iontophoretic period had a significant effect on drug levels delivered into skin layers. Iontophoresis enhanced the delivery of terbinafine hydrochloride into the skin layers and, therefore, may be used to improve the treatment of skin fungal infections.
本研究旨在确定离子电渗对盐酸特比萘芬(4%,w/w)递送入无毛大鼠皮肤及经皮渗透的影响。采用 Franz 扩散池进行体外皮肤渗透实验。在 0.2、0.3 和 0.4mA/cm2 的电流密度下进行 1 小时的阳极离子电渗。此外,还进行了离子电渗 15、30、45 和 60 分钟的实验。在这些实验中,制剂在离子电渗后被移除或保留在皮肤上,然后在 23 小时后评估被动渗透。采用胶带剥离和皮肤提取分别定量评估角质层和皮肤下层的药物水平。采用 HPLC 对样品进行分析。离子电渗后角质层中药物的递送量与被动递送量无显著差异(p>0.05)。然而,离子电渗组皮肤下层的药物水平明显更高。药物在皮肤层中的递送量受电流密度和电流应用时间的影响。在离子电渗后期间让药物制剂保留在皮肤上对递送入皮肤层的药物水平有显著影响。离子电渗增强了盐酸特比萘芬进入皮肤层的递送,因此可能用于改善皮肤真菌感染的治疗。