CIEPQPF, Departamento de Engenharia Química, Universidade de Coimbra, R. Sílvio Lima, 3030-790 Coimbra, Portugal.
CQE, Instituto Superior Técnico, Avenida Rovisco Pais, 1, Universidade de Lisboa, 1049-001 Lisbon, Portugal.
Eur J Pharm Biopharm. 2017 Nov;120:52-62. doi: 10.1016/j.ejpb.2017.08.006. Epub 2017 Aug 16.
Endophthalmitis, an inflammation of the eye due to perioperative infection, may occur after cataract surgery. Intraocular lenses (IOLs) loaded with an antibiotic have been proposed asan alternative to the conventional postoperative endophthalmitis prophylaxis, since the antibiotic is delivered directly to the target site. In this work, an IOL-based antibiotic releasing system was prepared from a copolymer used in the production of IOLs and a fluoroquinolone used in endophthalmitis prophylaxis (moxifloxacin, MFX). Argon plasma-assisted grafting with 2-hydroxyethyl methacrylate (HEMA) in the presence of MFX was the approach selected for surface modification, with MFX loaded both by entrapment in the grafted polyHEMA coating and by soaking. Surface and bulk properties were evaluated before and after surface modification and the MFX release profiles were obtained both in batch mode (sink conditions) and under hydrodynamic conditions, employing a purpose-built microfluidic cell, which simulated the hydrodynamic conditions around the eye lens. The effect of storage on the release profile of the best system was also assessed. The best system released MFX for ca. 15days above the minimum inhibitory concentration for Staphylococcus aureus and Staphylococcus epidermidis. The released MFX showed antimicrobial activity against these bacteria and was non-cytotoxic against corneal endothelial cells.
眼内炎是一种由于手术期感染引起的眼部炎症,可能发生在白内障手术后。载有抗生素的人工晶状体(IOL)已被提议作为传统术后眼内炎预防的替代方法,因为抗生素直接输送到目标部位。在这项工作中,一种基于 IOL 的抗生素释放系统是由用于生产 IOL 的共聚物和用于眼内炎预防的氟喹诺酮(莫西沙星,MFX)制备的。在存在 MFX 的情况下,用氩等离子体辅助接枝 2-羟乙基甲基丙烯酸酯(HEMA)是用于表面改性的方法,MFX 既通过接枝的聚 HEAM 涂层中的包埋又通过浸泡来负载。在表面改性前后评估了表面和体相性质,并在批处理模式(溶解条件)和使用定制的微流控细胞在水动力条件下获得了 MFX 释放曲线,该细胞模拟了晶状体周围的水动力条件。还评估了储存对最佳系统释放曲线的影响。最佳系统在释放 MFX 约 15 天以上,超过了金黄色葡萄球菌和表皮葡萄球菌的最小抑菌浓度。释放的 MFX 对这些细菌具有抗菌活性,并且对角膜内皮细胞无细胞毒性。