Jaskari T, Vuorio M, Kontturi K, Urtti A, Manzanares J A, Hirvonen J
Department of Pharmaceutics, University of Kuopio, P.O. Box 1627, FIN-70211, Kuopio, Finland.
J Control Release. 2000 Jul 3;67(2-3):179-90. doi: 10.1016/s0168-3659(00)00204-2.
The objective of this study was to assess the transdermal delivery of drugs using iontophoresis with cation- and anion-exchange fibers as controlled drug delivery vehicles. Complexation of charged model drugs with the ion-exchange fibers was studied as a method to achieve controlled transdermal drug delivery. Drug release from the cation-exchange fiber into a physiological saline was dependent on the lipophilicity of the drug. The release rates of lipophilic tacrine and propranolol were significantly slower than that of hydrophilic nadolol. Permeation of tacrine across the skin was directly related to the iontophoretic current density and drug concentration used. Anion-exchange fiber was tested with anionic sodium salicylate. The iontophoretic flux enhancement of sodium salicylate from the fiber was substantial. As the drug has to be released from the ion-exchange fiber before permeating across the skin, a clear reduction in the drug fluxes from the cationic and anionic fibers were observed compared to the respective fluxes of the drugs in solution. Overall, the ion-exchange fibers act as a drug reservoir, controlling the release and iontophoretic transdermal delivery of the drug.
本研究的目的是评估使用离子导入法，以阳离子和阴离子交换纤维作为可控药物递送载体时药物的透皮递送情况。研究了带电模型药物与离子交换纤维的络合作用，作为实现可控透皮药物递送的一种方法。阳离子交换纤维中药物向生理盐水的释放取决于药物的亲脂性。亲脂性的他克林和普萘洛尔的释放速率明显慢于亲水性的纳多洛尔。他克林透过皮肤的渗透与所使用的离子导入电流密度和药物浓度直接相关。用阴离子型的水杨酸钠对阴离子交换纤维进行了测试。水杨酸钠从纤维中的离子导入通量增强显著。由于药物在透过皮肤之前必须先从离子交换纤维中释放出来，因此与溶液中药物各自的通量相比，观察到阳离子和阴离子纤维中的药物通量明显降低。总体而言，离子交换纤维起到了药物储库的作用，控制着药物的释放和离子导入透皮递送。
