Fang J Y, Lin H H, Chen H I, Tsai Y H
School of Pharmacy, Chia Nan College of Pharmacy and Science, Tainan Hsien, Taiwan, ROC.
J Control Release. 1998 Aug 14;54(3):293-304. doi: 10.1016/s0168-3659(98)00010-8.
Iontophoresis and enhancers were performed to enhance percutaneous absorption of enoxacin so as to compare the enhancement between these two enhancing methods. The cationic surfactant of benzalkonium chloride showed the highest enhancing activity for enoxacin for all pH values of buffer vehicles. The enhancement factor of sodium laurylsulfate showed a dose-dependent property between the range of 0.1% to 3.0% concentration. Nonionic surfactant of Polysorbate 80 did not exhibit any enhancing effect on the percutaneous absorption of enoxacin. The highest enhancement factor of iontophoretic delivery was observed at pH 5.0 solution of anodal iontophoresis for cationic enoxacin. The cathodal iontophoresis of negative molecules and anodal iontophoresis of neutral molecules showed lower enhancing effect for enoxacin. The fact that the skin residuals of enoxacin after iontophoresis showed both tremendous and current density-dependent amounts for cationic enoxacin suggested local skin and soft tissue infections might be treated by this physical enhancement method. Combination of benzalkonium chloride and iontophoresis exerted a synergistic effect for anionic enoxacin in pH 10.0, which was possibly due to the shielding of negative charge in skin and the water molecules carried by chloride.
采用离子导入法和促渗剂来增强依诺沙星的经皮吸收，以便比较这两种增强方法之间的增强效果。对于缓冲介质的所有pH值，阳离子表面活性剂苯扎氯铵对依诺沙星表现出最高的增强活性。月桂醇硫酸酯钠的增强因子在0.1%至3.0%浓度范围内呈现剂量依赖性。聚山梨酯80非离子表面活性剂对依诺沙星的经皮吸收未表现出任何增强作用。对于阳离子型依诺沙星，在pH 5.0的阳极离子导入溶液中观察到离子导入给药的最高增强因子。阴性分子的阴极离子导入和中性分子的阳极离子导入对依诺沙星的增强作用较低。离子导入后依诺沙星在皮肤中的残留量对于阳离子型依诺沙星显示出巨大且与电流密度相关的量，这表明这种物理增强方法可能可用于治疗局部皮肤和软组织感染。在pH 10.0时，苯扎氯铵和离子导入的组合对阴离子型依诺沙星发挥协同作用，这可能是由于皮肤中负电荷的屏蔽以及氯离子携带的水分子所致。
