Palliyil Biji B, Li Cong, Owaisat Suzan, Lebo David B
Department of Pharmaceutical Sciences, School of Pharmacy, Temple University, 3307 N Broad Street, Suite 413, Philadelphia, Pennsylvania, 19140, USA.
AAPS PharmSciTech. 2014 Dec;15(6):1429-38. doi: 10.1208/s12249-014-0169-9. Epub 2014 Jun 27.
The main objective of the current work is to demonstrate the process of passive lateral diffusion in the human nail plate and its effect on the passive transungual permeation of antifungal drug ciclopirox olamine (CPO). A water soluble dye, methyl red sodium salt (MR) was used to visualize the process of lateral diffusion using a novel suspended nail experiment. The decline in concentration of CPO correlates with that of concentration of MR from the proximal to the distal end of the nail in suspended nail study. Three toenails each were trimmed to 5 mm × 5 mm (25 mm(2)), 7 mm × 7 mm (49 mm(2)), and 9 mm × 9 mm (81 mm(2)) to study the extent and effect of lateral diffusion of the CPO on its in vitro transungual permeation. The permeation flux of CPO decreased as the surface area of the toenail increased. There was a positive correlation between the concentrations of CPO and MR in the area of application and in the peripheral area of the toenails of the three surface areas, confirming the findings in the suspended nail experiment. Profound lateral diffusion of CPO was demonstrated and shown to reduce the in vitro passive transungual drug permeation and prolong the lag-time in human toenails. The study data implies that during passive in vitro transungual permeation experiments, the peripheral nail around the area of drug application has to be kept to a minimum, in order to get reliable data which mimics the in vivo situation.
当前工作的主要目的是证明人指甲板中的被动横向扩散过程及其对抗真菌药物环吡酮胺(CPO)被动经甲渗透的影响。使用一种新型的悬浮指甲实验,用水溶性染料甲基红钠盐(MR)来可视化横向扩散过程。在悬浮指甲研究中,从指甲近端到远端,CPO浓度的下降与MR浓度的下降相关。将每三个脚趾甲分别修剪为5毫米×5毫米(25平方毫米)、7毫米×7毫米(49平方毫米)和9毫米×9毫米(81平方毫米),以研究CPO横向扩散对其体外经甲渗透的程度和影响。随着脚趾甲表面积的增加,CPO的渗透通量降低。在三个表面积的脚趾甲的给药区域和周边区域,CPO和MR的浓度之间存在正相关,证实了悬浮指甲实验中的发现。已证明CPO存在显著的横向扩散,并显示其会降低体外被动经甲药物渗透并延长人脚趾甲中的滞后时间。研究数据表明,在体外被动经甲渗透实验期间,给药区域周围的周边指甲必须保持在最小程度,以便获得模拟体内情况的可靠数据。