Femenía-Font A, Balaguer-Fernández C, Merino V, López-Castellano A
Departamento de Fisiología, Farmacología y Toxicología, Facultad de Ciencias Experimentales y de la Salud, Universidad Cardenal Herrera-CEU, 46113 Moncada, Spain.
Int J Pharm. 2006 Oct 12;323(1-2):125-30. doi: 10.1016/j.ijpharm.2006.05.049. Epub 2006 Jun 2.
The aim of the present work was to characterize in vitro sumatriptan transdermal absorption through human skin and to investigate the effect of chemical enhancers and iontophoresis applied both individually and in combination. A secondary objective was to compare the results obtained with those in porcine skin under the same conditions, in order to characterize the relationship between the two skin models and validate the porcine model for further research use. Transdermal flux of sumatriptan was determined in different situations: (a) after pre-treatment of human skin with ethanol, Azone (1-dodecyl-azacycloheptan-2-one), polyethylene glycol 600 and R-(+)-limonene, (b) under iontophoresis application (0.25 and 0.50 mA/cm(2)) and (c) combining chemical pre-treatment and iontophoresis at 0.50 mA/cm(2) current density. All the strategies applied enhance sumatriptan transdermal absorption. A linear relationship between the fluxes in the two skin models in the different conditions assayed can be established. The combination of both strategies, Azone and iontophoresis, proved to be the most effective of the techniques for enhancing the transdermal absorption of sumatriptan. The flux obtained with porcine skin in vitro is approximately double that obtained in human skin.
本研究的目的是表征舒马曲坦经人体皮肤的体外透皮吸收情况，并研究化学促进剂和离子导入单独及联合应用的效果。第二个目标是比较在相同条件下猪皮肤的实验结果，以表征两种皮肤模型之间的关系，并验证猪模型在进一步研究中的应用。在不同情况下测定舒马曲坦的透皮通量：(a) 用乙醇、氮酮（1-十二烷基氮杂环庚烷-2-酮）、聚乙二醇600和R-(+)-柠檬烯预处理人体皮肤后；(b) 在离子导入应用（0.25和0.50 mA/cm²）下；(c) 在0.50 mA/cm²电流密度下将化学预处理和离子导入相结合。所有应用的策略均能增强舒马曲坦的透皮吸收。在测定的不同条件下，可以建立两种皮肤模型通量之间的线性关系。氮酮和离子导入这两种策略的联合应用被证明是增强舒马曲坦透皮吸收最有效的技术。体外猪皮肤获得的通量约为人体皮肤的两倍。
