Ciolino Joseph B, Hoare Todd R, Iwata Naomi G, Behlau Irmgard, Dohlman Claes H, Langer Robert, Kohane Daniel S
Department of Ophthalmology, Massachusetts Eye and Ear Infirmary, Harvard Medical School, Boston, Massachusetts 02115, USA.
Invest Ophthalmol Vis Sci. 2009 Jul;50(7):3346-52. doi: 10.1167/iovs.08-2826. Epub 2009 Jan 10.
To formulate and characterize a drug-eluting contact lens designed to provide extended, controlled release of a drug.
Prototype contact lenses were created by coating PLGA (poly[lactic-co-glycolic acid]) films containing test compounds with pHEMA (poly[hydroxyethyl methacrylate]) by ultraviolet light polymerization. The films, containing encapsulated fluorescein or ciprofloxacin, were characterized by scanning electron microscopy. Release studies were conducted in phosphate-buffered saline at 37 degrees C with continuous shaking. Ciprofloxacin eluted from the contact lens was studied in an antimicrobial assay to verify antimicrobial effectiveness.
After a brief and minimal initial burst, the prototype contact lenses demonstrated controlled release of the molecules studied, with zero-order release kinetics under infinite sink conditions for over 4 weeks. The rate of drug release was controlled by changing either the ratio of drug to PLGA or the molecular mass of the PLGA used. Both the PLGA and the pHEMA affected release kinetics. Ciprofloxacin released from the contact lenses inhibited ciprofloxacin-sensitive Staphylococcus aureus at all time-points tested.
A prototype contact lens for sustained drug release consisting of a thin drug-PLGA film coated with pHEMA could be used as a platform for ocular drug delivery with widespread therapeutic applications.
制备并表征一种旨在实现药物延长、控释的药物洗脱隐形眼镜。
通过紫外光聚合,用聚(甲基丙烯酸羟乙酯)(pHEMA)包覆含有测试化合物的聚乳酸-乙醇酸共聚物(PLGA)薄膜,从而制造出原型隐形眼镜。含有封装荧光素或环丙沙星的薄膜通过扫描电子显微镜进行表征。在37℃的磷酸盐缓冲盐水中持续振荡进行释放研究。对从隐形眼镜洗脱的环丙沙星进行抗菌试验,以验证其抗菌效果。
经过短暂且微量的初始突释后,原型隐形眼镜显示出对所研究分子的控释效果,在无限漏槽条件下呈零级释放动力学,持续超过4周。通过改变药物与PLGA的比例或所用PLGA的分子量来控制药物释放速率。PLGA和pHEMA均影响释放动力学。在所有测试时间点,从隐形眼镜释放的环丙沙星均能抑制对环丙沙星敏感的金黄色葡萄球菌。
一种由涂有pHEMA的薄药物-PLGA薄膜组成的用于持续药物释放的原型隐形眼镜,可作为具有广泛治疗应用的眼部药物递送平台。