Extended Release of Timolol from Ethyl Cellulose Microparticles Laden Hydrogel Contact Lenses

摘要

Glaucoma is a second leading cause of blindness globally after cataract, which is managed through eye drops, which are highly inefficient due to a low bioavailability of less than 1-5%. Frequent administration of eye drops leads to incompliance in patients, so there is a great need for medical device such as contact lenses to treat glaucoma. The objective of research was to provide sustained ocular delivery of timolol via prototype poly (hydroxyethyl methacrylate) hydrogel contact lenses which may improve bioavailability due to increase in ocular residence time of drug. The present work was to encapsulate drug in ethylcellulose microparticles, and to entrap these microparticles in the hydrogel. Microparticles were prepared by spray drying method using different ratios of drug to ethylcellulose. The solid state characterization studies of drug loaded microparticles revealed the transformation of drug to an amorphous state. The hydrogels were characterized by studying their optical and physical properties to determine their suitability as extended wear contact lenses. Microparticles laden hydrogels were compared with direct drug loaded hydrogels. The study of microparticles laden hydrogels showed reduction in optical and physical properties and the impact was proportional to the amount of microparticles in hydrogels. The results suggest the application of optimization and nanotechnology. In vitro drug release study revealed that direct loading batch delivers drug for 22 hours with high drug loading of 150 μg, while microparticles laden hydrogel deliver drug up to 48 hours (zero order kinetics) with low drug loading of 50 μg. The hydrogels appeared safe in the cytotoxicity study. The study demonstrated the promising potential of loading the ethyl cellulose microparticles into hydrogels to serve as a good platform for sustained ophthalmic drug delivery.