Facultad de Estudios Superiores Cuautitlán, Laboratorio de Posgrado en Tecnología Farmacéutica, Universidad Nacional Autónoma de México, Avenida 1 de Mayo s/n, Cuautitlán Izcalli CP 54743, México.
J Microencapsul. 2013;30(1):72-80. doi: 10.3109/02652048.2012.700956. Epub 2012 Jul 3.
The aim of this study was to evaluate the passive and iontophoretic permeation of triclosan in human skin using a triclosan solution and triclosan-loaded cationic nanospheres in order to determine which of the two strategies is more effective in allowing the deposition of triclosan within the skin. Triclosan-loaded nanospheres were prepared by the emulsification-solvent displacement technique using aminoalkyl methacrylate (Eudragit® RL 100) as polymer matrix. Nanospheres of 261.0 ± 15.1 nm with a positive surface charge (Ψz = 26.0 ± 3.2 mV) were obtained. Drug loading was 62.0 ± 1.7%. Results demonstrated that the amount of triclosan retained within the skin was significantly greater (8.5-fold) when this was encapsulated into cationic nanospheres and administered by passive diffusion than when the triclosan solution was employed. The amount of triclosan retained within the skin when the cationic nanospheres were administered by iontophoresis was 3.1-fold greater than when the triclosan solution was administered by passive diffusion. Iontophoresis proved to be effective in enhancing the passage of triclosan in solution throughout the skin, whereas the triclosan nanospheres could achieve a local effect by forming a controlled release dermal depot.
本研究旨在评估三氯生在人体皮肤中的被动和离子导入渗透,使用三氯生溶液和载三氯生的阳离子纳米球,以确定这两种策略中哪一种更有效地使三氯生沉积在皮肤内。载三氯生的纳米球通过乳化-溶剂置换技术制备,使用氨基烷基甲基丙烯酸酯(Eudragit® RL 100)作为聚合物基质。得到粒径为 261.0±15.1nm、表面带正电荷(Ψz=26.0±3.2mV)的纳米球。药物载量为 62.0±1.7%。结果表明,当三氯生被包裹在阳离子纳米球中并通过被动扩散给药时,其在皮肤内的保留量显著增加(8.5 倍),而当使用三氯生溶液时则不然。当阳离子纳米球通过离子导入给药时,其在皮肤内的保留量是通过被动扩散给药时的 3.1 倍。离子导入被证明可以有效地增强溶液中三氯生在整个皮肤中的传递,而载三氯生的纳米球可以通过形成控制释放的皮肤储库来实现局部效果。