Many effective anti-glaucoma drugs available for the treatment of ocular hypertension and open angle glaucoma
are associated with rapid and extensive precorneal loss caused by the drainage and high tear fluid turnover. The present
study involved design of mucoadhesive nanoparticulate carrier system containing betaxolol hydrochloride for ocular
delivery to improve its corneal permeability and precorneal residence time. Nanoparticles were prepared by spontaneous
emulsification method and had a particle size of 168-260nm with zeta potential of 25.2-26.4 mV. The in vitro release studies
in simulated tear fluid exhibited biphasic release pattern with an initial burst followed by sustained release upto 12 h.
The sterility tests confirmed that formulation was free from viable microorganisms and suitable for ocular delivery. The
ocular tolerance of nanoparticles was evaluated using Hen Egg-Chorion Allantoic Membrane (HE-CAM) method and was
found to be non-irritant. Stability studies of nanoparticles revealed that there was no significant change in particle size and
drug content after storage at 25±2°C/60±5% RH over a period of 3 months. In vivo pharmacodynamic studies were carried
out in dexamethasone induced glaucoma model in rabbits. The developed nanoparticles showed significant decrease in intraocular
pressure (IOP) compared to marketed formulation. Optimized formulation of BN3 showed gradual reduction of
IOP reaching peak value of 9.9±0.5mm Hg, equivalent to 36.39±1.84% reduction in IOP compared to control at the end of
5 h which was significant (p < 0.05) compared to marketed formulation. Thus, our studies demonstrate that developed
nanoparticles offer a promising delivery system for the management of glaucoma.
Keywords: Betaxolol, glaucoma, chitosan, nanoparticles, ocular delivery.
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