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基于接触镜的药物经离子导入递送至兔眼后段。

Contact Lens Based Drug Delivery to the Posterior Segment Via Iontophoresis in Cadaver Rabbit Eyes.

机构信息

Department of Chemical Engineering, University of Florida, 1030 Center Drive, Gainesville, Florida, 32611, USA.

出版信息

Pharm Res. 2019 Apr 19;36(6):87. doi: 10.1007/s11095-019-2625-4.

Abstract

PURPOSE

A drug loaded contact lens combined with electrodes positioned diametrically opposite and beyond the limbus can potentially deliver ionic drugs directly to the vitreous.

METHODS

Commercial lenses are loaded with nile blue or fluorescein as the drug analogs and placed on cadaver rabbit eyes. Electrodes (19.6 mm) are placed atop at opposite sides of the sclera to apply a constant current (0.125-0.250 mA) for 1-2 h. COMSOL simulations are conducted to determine the field distribution and the potential drop across various tissue layers and equivalent circuit model is developed to calculate the electrophoretic velocity and estimate the drug flux.

RESULTS

The device delivered both hydrophobic and hydrophilic dyes to the tissue. The amount of fluorescein delivered to the vitreous directly correlated with the applied current and time duration. The electrophoretic mobility from the experimental data agreed with the model estimates. Confocal microscopy showed that nile blue penetrated through the conjunctiva-sclera barrier to reach the retina showing that the electric field can transport molecules through the ocular tissue and into the vitreous. The ex vivo model neglects transport into flowing capillaries in the choroid. However, the time scale for electrophoretic transport across the choroid was found to be 550-1300 fold shorter than that for uptake into the choroidal capillaries.

CONCLUSION

Incorporation of an electric field with multiple electrodes on a single lens can effectively deliver ionic drugs to the posterior region at levels comparable to current methods with the benefits of being safer and less invasive.

摘要

目的

载药接触镜与位于角膜缘对侧并超出其范围的电极相结合,可将离子药物直接递送至玻璃体。

方法

将尼罗蓝或荧光素等药物类似物载入商业镜片,并将其置于尸体兔眼上。将电极(19.6 毫米)置于巩膜相对侧的顶部,施加恒定电流(0.125-0.250 mA)1-2 小时。通过 COMSOL 模拟确定电场分布和各组织层之间的电位降,并建立等效电路模型以计算电泳速度并估算药物通量。

结果

该装置可将疏水性和亲水性染料递送至组织中。递送至玻璃体的荧光素量与施加的电流和时间直接相关。从实验数据得出的电泳迁移率与模型估计值一致。共焦显微镜显示,尼罗蓝穿透结膜-巩膜屏障到达视网膜,表明电场可以将分子通过眼部组织输送到玻璃体中。离体模型忽略了脉络膜中流动毛细血管的转运。然而,发现电泳穿过脉络膜的时间尺度比进入脉络膜毛细血管的时间尺度短 550-1300 倍。

结论

在单个镜片上结合多个电极的电场可有效地将离子药物递送至后节区域,其水平可与当前方法相媲美,同时具有更安全、侵入性更小的优点。

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