title: A potential new therapeutic system for glaucoma: solid lipid nanoparticles containing methazolamide.
abstract: Methazolamide (MTA) is an antiglaucoma drug; however, there are many side effects of its systemic administration with insufficient ocular therapeutic concentrations. The aim of this study was to formulate MTA-loaded solid lipid nanoparticles (SLNs) and evaluate the potential of SLNs as a new therapeutic system for glaucoma. SLNs were prepared by a modified emulsion-solvent evaporation method and their physicochemical characteristics were evaluated. The pharmacodynamics was investigated by determining the percentage decrease in intraocular pressure. The ocular irritation was studied by Draize test. Despite a burst release of SLNs, the pharmacodynamic experiment indicated that MTA-SLNs had higher therapeutic efficacy, later occurrence of maximum action, and more prolonged effect than drug solution and commercial product. Formulation of MTA-SLNs would be a potential delivery carrier for ocular delivery, with the advantages of a more intensive treatment for glaucoma, lower in doses and better patient compliance compared to the conventional eye drops.
authors.affiliation: School of Pharmacy, Nanjing Medical University, 140 Hanzhong Road, Nanjing 210029, People's Republic of China.
authors.forename: Rui
authors.initials: R
authors.lastname: Li
authors.forename: Sunmin
authors.initials: S
authors.lastname: Jiang
authors.forename: Dongfei
authors.initials: D
authors.lastname: Liu
authors.forename: Xinyun
authors.initials: X
authors.lastname: Bi
authors.forename: Fengzhen
authors.initials: F
authors.lastname: Wang
authors.forename: Qing
authors.initials: Q
authors.lastname: Zhang
authors.forename: Qunwei
authors.initials: Q
authors.lastname: Xu
mesh_terms: D000818:Animals; D002257:Carbonic Anhydrase Inhibitors / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D016503:Drug Delivery Systems; D005260:Female; D005901:Glaucoma / Q000188:drug therapy*; D006801:Humans; D008055:Lipids / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D008297:Male; D008704:Methazolamide / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D053758:Nanoparticles / Q000737:chemistry*; D011817:Rabbits
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D008055:Lipids; D008704:Methazolamide