Ophthalmic delivery of brinzolamide by liquid crystalline nanoparticles: in vitro and in vivo evaluation.

Abstract	Brinzolamide (BLZ) is a drug used to treat glaucoma; however, its use is restricted due to some unwanted adverse events. The goal of this study was to develop BLZ-loaded liquid crystalline nanoparticles (BLZ LCNPs) and to figure out the possibility of LCNPs as a new therapeutic system for glaucoma. BLZ LCNPs were produced by a modified emulsification method and their physicochemical aspects were estimated. In vitro release study revealed BLZ LCNPs displayed to some extent prolonged drug release behavior in contrast to that of BLZ commercial product (Azopt®). The ex vivo apparent permeability coefficient of BLZ LCNP systems demonstrated a 3.47-fold increase compared with that of Azopt®. The pharmacodynamics was checked over by calculating the percentage fall in intraocular pressure and the pharmacodynamic test showed that BLZ LCNPs had better therapeutic potential than Azopt®. Furthermore, the in vivo ophthalmic irritation was evaluated by Draize test. In conclusion, BLZ LCNPs would be a promising delivery system used for the treatment of glaucoma, with advantages such as lower doses but maintaining the effectiveness, better ocular bioavailability, and patient compliance compared with Azopt®.
Authors	Weijun Wu, Jing Li, Lin Wu, Baoyan Wang, Zhongyuan Wang, Qunwei Xu, Hongliang Xin
Journal	AAPS PharmSciTech (AAPS PharmSciTech) Vol. 14 Issue 3 Pg. 1063-71 (Sep 2013) ISSN: 1530-9932 [Electronic] United States
PMID	23813437 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References	Carbonic Anhydrase Inhibitors Sulfonamides Thiazines brinzolamide
Topics	Administration, Ophthalmic Animals Carbonic Anhydrase Inhibitors (administration & dosage, pharmacokinetics, pharmacology) Chromatography, High Pressure Liquid Cornea (metabolism) Crystallization In Vitro Techniques Intraocular Pressure (drug effects) Microscopy, Electron, Transmission Nanoparticles Rabbits Scattering, Small Angle Sulfonamides (administration & dosage, pharmacokinetics, pharmacology) Thiazines (administration & dosage, pharmacokinetics, pharmacology)

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