Lambrecht Renzo, Clarys Peter, Clijsen Ron, Barel André O
Faculty of Physical Education and Physiotherapy, Vrije Universiteit Brussel, BIOM, Plainlaan 2, 1050 Brussels, Belgium.
Skin Res Technol. 2006 Aug;12(3):211-6. doi: 10.1111/j.0909-752X.2006.00161.x.
BACKGROUND/AIMS: In this study, we investigated the bioavailability of iontophoretically delivered diclofenac with the methylnicotinate (MN) test. The inhibition of an erythema provoked by MN is proportional to the bioavailability of diclofenac in the skin. It was our aim to use this procedure in the determination of the contribution of, respectively, passive diffusion, occlusion and electrically assisted delivery during an iontophoretic procedure as used in physiotherapy.
A total of six application sites were marked on the volar forearms of each volunteer (n=12), for the following treatment and/or control modes: A=cathodal iontophoresis of 12 mg/cm(2) Voltaren Emulgel (diethylammonii diclofenac 1%) for 20 min; B=passive diffusion under a contact sponge; C=passive diffusion without any covering; D=current alone; E=standard MN response; and F=blanco site. Tristimulus surface colorimetry and Laser Doppler flowmetry were used to measure, respectively, the skin color and the perfusion of the microcirculation. Bioavailability was assessed by quantification of an MN-induced erythema under the different conditions.
A significant reduction of the MN-induced erythema was observed with the Chromameter and Laser Doppler measurements for the following treatment modalities: (1) electrically assisted delivery: respectively, 65% and 100%, (2) application under a contact sponge: 66% and 97% and (3) passive diffusion without any covering: 32% and 65%. A significant reduction was equally observed for the site treated with the current alone: 19% and 42%. There was no significant difference between the response after iontophoretic-delivered diclofenac (mode A) and application of diclofenac under a contact sponge (mode B).
The procedure used enabled us to evaluate the bioavailability of a non-steroidal anti-inflammatory drug in the skin. Under the conditions used, we did not find an increased bioavailability after electrically assisted delivery of diclofenac compared with the passive percutaneous penetration under the contact sponge.
背景/目的：在本研究中，我们通过甲基烟酸盐（MN）试验研究了离子导入法递送双氯芬酸的生物利用度。MN引发的红斑抑制作用与双氯芬酸在皮肤中的生物利用度成正比。我们的目的是使用该程序来确定在物理治疗中使用的离子导入过程中被动扩散、封闭和电辅助递送各自的贡献。
在每位志愿者（n = 12）的掌侧前臂上标记总共六个应用部位，用于以下治疗和/或对照模式：A = 12 mg/cm²扶他林乳胶剂（双氯芬酸二乙胺1%）阴极离子导入20分钟；B = 在接触海绵下被动扩散；C = 无任何覆盖物的被动扩散；D = 仅电流；E = 标准MN反应；F = 空白部位。分别使用三刺激表面比色法和激光多普勒血流仪测量皮肤颜色和微循环灌注。通过量化不同条件下MN诱导的红斑来评估生物利用度。
对于以下治疗方式，使用色度计和激光多普勒测量观察到MN诱导的红斑有显著减少：（1）电辅助递送：分别为65%和100%，（2）在接触海绵下应用：66%和97%，以及（3）无任何覆盖物的被动扩散：32%和65%。仅用电流处理的部位也观察到显著减少：19%和42%。离子导入递送双氯芬酸（模式A）和在接触海绵下应用双氯芬酸（模式B）后的反应之间没有显著差异。
所使用的程序使我们能够评估皮肤中一种非甾体抗炎药的生物利用度。在所使用的条件下，与在接触海绵下的被动经皮渗透相比，我们没有发现双氯芬酸电辅助递送后生物利用度增加。
