Authors: Q. He, Z. Fang, M. Wang, Q.W. Xu, R. Chen, X.Z. Zhang, W.M. Yaun, D.M. Zhau, Jian Wu,
Affilation: Morehouse School of Medicine, United States
Pages: 401 - 404
Keywords: glucoma, nanoparticles ocular
Glaucoma, the leading cause of irreversible blindness in the world, is estimated to be affected by 67 million people. It is characterized by an increase in intraocular pressure (IOP). Carbonic anhydrase inhibitors (CAIs) are orally used for controlling IOP. Since CA II/IV/XII is present in many other tissues, systemic CAIs possess undesired side effects. In order to avoid these undesired side effects, we have developed topically methazolamide using lyceum chinense and calcium phosphate nanoparticles as a delivery system. Preliminary studies showed strong and long-lasting IOP lowering, being more effective than clinical used brinzolamide. The maximum lowering in normal white and pigmented rabbits were about 6.14±0.96 mmHg and 4.20±1.38 mmHg (mean±SEM) respectively. HPLC results showed the peak concentration in the aqueous humor appeared in 15 minutes (0.3µg/ml). Clinical and toxicity evaluation indicated there is no irritation and inflammation on the experimented eyes compared with the control group by histological examination and slit lamp. Also, there is no toxic effect in the acute toxicology and allergic experiment. Based on our findings, we suggest that lyceum chinense and calcium phosphate nanoparticles may favor the localized ocular delivery of CAIs for the treatment of glaucoma.