FORMULATION AND EVALUATION OF DORZOLAMIDE AND TIMOLOL OCUSERTS

Abstract

Objective: This study aims to formulate novel dorzolamide hydrochloride and timolol maleate ocuserts to enhance patient compliance through providing controlled drugs release from polymeric matrix. Methods: Ocuserts were prepared by solvent-casting method using different polymers Ethyl Cellulose, Eudragit S100 and Hydroxy propyl methyl cellulose in different ratios. The prepared ocusters were physcochemichally evaluated for their weight, thickness, drug content uniformity, surface pH, Swelling Index (SI) and folding endurance. In-vitro drug release was studied from the prepared formulas and the results were analyzed by drug release kinetic models. The ocuserts stability after three month's storage at 40 +/- 0.5 degrees C and 75 +/- 5% RH was estimated. In-vivo tests were done to study the release profile and estimate the safety of the incorporated drugs in rabbits' eyes. Results: The prepared ocuserts show uniform weight, thickness and drug content. Their surface pH was in the physiological range and showed acceptable folding endurance. HPMC Formulas had higher SI values. Results of in-vivo testing for one of the prepared ocuserts shows slow release of both drugs up to 24 hours with no signs of eye sensitivity. Conclusion: One of the prepared ocuserts is promising for once-daily effective and safe drug delivery system of DHCL and TM for glaucoma treatment.