Methotrexate delivery to the eye using transscleral hydrogel iontophoresis
Methotrexate delivery to the eye using transscleral hydrogel iontophoresis
复制标题
DOI：
10.1080/02713680701528674
复制
发表时间：
2007-01-01
影响因子：
2
通讯作者：
Pe'er, Jacob
中科院分区：
文献类型：
--
作者：
Eljarrat-Binstock, Esther;Domb, Abraham J.;Pe'er, Jacob
目的：目的：评价甲氨蝶呤经巩膜水凝胶离子导入后在眼内的渗透和分布。方法：采用便携式离子导入装置，以载药水凝胶为载体，对甲氨蝶呤离子导入家兔体内进行研究.以1.6 mA/cm（2）离子导入治疗4 min后2、4和8小时评价药物分布情况。以5 mA/cm（2）离子导入治疗2小时后测定眼部药物水平，并与模拟离子导入和玻璃体内注射甲氨蝶呤进行比较。结果如下：离子电渗治疗后，治疗药物水平在巩膜和视网膜处维持至少8小时，在房水处维持2小时。在增加电流密度后，在玻璃体处达到两倍高的浓度，在视网膜和巩膜处达到8至20倍高的浓度。结论：应用甲氨蝶呤水凝胶进行短时间低电流无创离子导入治疗眼部炎症性疾病和眼内淋巴瘤具有潜在的临床价值。
Purpose: To evaluate methotrexate penetration and distribution profile in ocular structures after short low current transscleral hydrogel iontophoresis. Methods: Methotrexate iontophoresis was studied in rabbits using drug - loaded hydrogels mounted on a portable iontophoretic device. Drug distribution profile was evaluated 2, 4, and 8 hours after iontophoretic treatment of 1.6 mA/cm(2) for 4 min. Ocular drug levels were also determined two hours after iontophoretic treatment of 5 mA/cm(2), compared to mock iontophoresis and intravitreal injection of methotrexate. Results: Therapeutic drug levels were maintained for at least 8 h at the sclera and retina and for 2 h at the aqueous humor following the iontophoretic treatment. After increasing the current density, a twice - higher concentration was achieved at the vitreous and 8 to 20 time higher concentrations at the retina and sclera. Conclusions: A short low current non - invasive iontophoretic treatment using methotrexate - loaded hydrogels has a potential clinical value in treating ocular inflammatory diseases and intraocular lymphoma.