Development of Multiple Microemulsion Eye Drops for Sustained Release of New Glaucoma Drug

Abstract

Persistent or repeated elevation of intraocular pressure (IOP) is a primary risk factor of visual field loss in glaucoma, therefore IOP reduction is the first-line therapeutic option in the disease management. Unfortunately, the current therapies are associated with a lot of deficiencies including several daily dosing, reduced efficacy and systemic side effects all of which resulted in poor patient compliance. Previously we have identified Calcium voltage-gated channel auxiliary subunit Alpha2delta 1 gene (Cacna2d1) as a novel modulator of IOP and confirmed that pregabalin targeted CACNA2D1 in eye tissues (ciliary body and trabecular meshwork) to lower IOP in a dose-dependent manner. The research presented in this dissertation aimed to develop a once-daily ocular pregabalin-loaded multiple water-in-oil-in-water microemulsion eye drops. Several in vitro and in vivo evaluations were used to characterize the prepared ophthalmic formulations. Also stability study at 5°C, 25°C, 30°C and 40°C was conducted for four months. All the formulations components were carefully selected to be highly biocompatible that provided a highly transparent eye drops with a miniscule droplet size

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