Eljarrat-Binstock Esther, Domb Abraham J, Orucov Faik, Frucht-Pery Joseph, Pe'er Jacob
Department of Medicinal Chemistry and Natural Products, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel.
Curr Eye Res. 2007 Jul-Aug;32(7-8):639-46. doi: 10.1080/02713680701528674.
To evaluate methotrexate penetration and distribution profile in ocular structures after short low current transscleral hydrogel iontophoresis.
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/cm2 for 4 min. Ocular drug levels were also determined two hours after iontophoretic treatment of 5 mA/cm2, compared to mock iontophoresis and intravitreal injection of methotrexate.
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.
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.
评估短时间低电流经巩膜水凝胶离子电渗疗法后甲氨蝶呤在眼部结构中的渗透和分布情况。
在兔子身上使用安装在便携式离子电渗装置上的载药水凝胶研究甲氨蝶呤离子电渗疗法。在以1.6 mA/cm²的电流进行4分钟离子电渗治疗后2、4和8小时评估药物分布情况。与假离子电渗疗法和玻璃体内注射甲氨蝶呤相比，在以5 mA/cm²的电流进行离子电渗治疗两小时后也测定眼内药物水平。
离子电渗治疗后，巩膜和视网膜中的治疗药物水平至少维持8小时，房水中维持2小时。提高电流密度后，玻璃体内的浓度提高了两倍，视网膜和巩膜中的浓度提高了8至20倍。
使用载有甲氨蝶呤的水凝胶进行短时间低电流非侵入性离子电渗治疗在治疗眼部炎症性疾病和眼内淋巴瘤方面具有潜在的临床价值。
