Department of Chemical Engineering, University of Florida, 1030 Center Drive, Gainesville, FL 32611, United States.
Eur J Pharm Biopharm. 2019 Jul;140:40-49. doi: 10.1016/j.ejpb.2019.04.016. Epub 2019 Apr 29.
Ophthalmic delivery via iontophoresis is currently achieved by placing an electrode on the cornea with a counter electrode on the ear or forehead. Here we test the feasibility of placing both electrodes diametrically opposite on a contact lens to create field gradients to transport ionic drugs into the cornea. Commercial lenses loaded with nile blue and fluorescein as hydrophobic and hydrophilic drug analogs, respectively were placed on cadaver rabbit eyes. Electric field gradients were created by placing cathode and anode on the lens diametrically opposite to each other. The incorporation of an electric field (0.125 m-0.250 mA), showed an increased uptake of nile blue and the quantity was a function of the duration of the electric field and the amount of applied current. Similar increases in flux were observed for fluorescein. Confocal fluorescence imaging also shows increased penetration of the dyes in presence of the field. An equivalent circuit model suggests that the field gradients are much stronger in the direction perpendicular to the cornea, which results is minimal short circuiting of current through the tear film. The incorporation of an electric field into a lens could be a less invasive and more effective approach to achieve ophthalmic drug delivery via iontophoresis.
经皮给药是目前通过将一个电极放在角膜上,一个对电极放在耳朵或额头上来实现的。在这里,我们测试了在隐形眼镜上放置两个电极的可行性,这两个电极位于直径相对的位置,以产生场梯度,将离子药物输送到角膜中。商业隐形眼镜上分别装载了尼罗蓝和荧光素作为疏水性和亲水性药物类似物,然后将这些隐形眼镜放在已死亡的兔子眼睛上。通过将阴极和阳极放置在镜片直径相对的位置来产生电场梯度。结果表明,在施加电场(0.125-0.250mA)后,尼罗蓝的摄取量增加,其数量与电场的持续时间和施加电流的大小有关。对于荧光素,也观察到通量的相似增加。共聚焦荧光成像也显示在存在电场的情况下染料的穿透性增加。等效电路模型表明,垂直于角膜的方向上的场梯度要强得多,这导致电流通过泪膜的短路最小化。将电场纳入隐形眼镜可能是一种侵入性更小、更有效的方法,可通过电渗析实现眼部药物输送。