Transdermal iontophoretic delivery of selegiline hydrochloride (SH) across dermatomed human skin was studied. Electrochemical stability and various factors affecting the skin permeation were investigated. SH was stable under the influence of an electrical field. The permeation of SH was very low by passive delivery (2.29 +/- 0.05 microg/cm(2)/h) as compared to iontophoresis at 0.5 mA/cm(2) (65.10 +/- 5.04 microg/cm(2)/h). An increase in drug concentration from 1 to 20 mg/mL increased the iontophoretic flux by 13-fold. Optimal pH and salt (NaCl) concentration for iontophoretic delivery of SH were found to be pH 5 and 100 mM, respectively. Overall, with 20 mg/mL SH and a current density of 0.4 mA/cm(2), a maximum flux of 305.5 microg/cm(2)/h was obtained. Based on reported pharmacokinetic parameters, input target delivery rate to achieve effective plasma concentration of SH (2.2 ng/mL) was calculated. With a surface area of 40 cm(2), iontophoretic delivery can provide six to seven times higher levels of SH than the target delivery rate, which enables lowering of the dose and/or patch surface area. Further in vivo studies will be required to prove the efficacy of ionophoresis for enhanced delivery of SH.
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机译：研究了盐酸司来吉兰（SH）在皮肤皮肤皮肤上的透皮离子电渗传递。研究了电化学稳定性和影响皮肤渗透的各种因素。 SH在电场的影响下是稳定的。与离子电渗疗法在0.5 mA / cm（2）（65.10 +/- 5.04 microg / cm（2）//）相比，通过被动递送SH的渗透率非常低（2.29 +/- 0.05 microg / cm（2）/ h） H）。药物浓度从1增加到20 mg / mL，离子电渗流增加了13倍。发现离子电渗入SH的最佳pH和盐（NaCl）浓度分别为pH 5和100 mM。总体而言，使用20 mg / mL SH和0.4 mA / cm（2）的电流密度，可获得305.5 microg / cm（2）/ h的最大通量。根据报告的药代动力学参数，计算出达到SH的有效血浆浓度（2.2 ng / mL）的输入目标递送速率。离子电渗疗法的表面积为40 cm（2），可提供的SH水平比目标递送速率高六至七倍，从而可以降低剂量和/或贴剂表面积。需要进一步的体内研究来证明离子载体疗法对增强SH的递送的功效。
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