Abstract
IMPROVED CORNEAL ABSORPTION OF TIMOLOL MALEATE BY FORMULATING AS NANOPARTICULATED MUCOADHESIVE OCULAR DRUG DELIVERY SYSTEM

Senthil Venkatachalam*, Nirmal Franklin and Merikanapalli V. Harsha

ABSTRACT

Glaucoma is one of the major causes of blindness in the world after cataract. Management of glaucoma through eye drops that reduce IOP (Intra ocular pressure) has major deficiencies including low patient compliance and low bioavailability. Many current anti-glaucoma drugs, available for the treatment of ocular hypertension and open angle glaucoma are associated with rapid and extensive pre-corneal loss caused by drainage and high tear fluid turnover. The objective of this study was design and development of mucoadhesive nanoparticles of Timolol Maleate for increasing the ocular bioavailability from 1-3% to at least 15-20% and to provide sustained release of the drug. The NPs (Nanoparticles) were prepared by using mucoadhesive polymers such as chitosan and poly(acrylic acid). The mean size of NPs was found to be 141.29 nm with PI of 0.339 and zeta potential of the NPs was positive (+23.30 mV). Irritancy Test (HET-CAM Method) no hemorrhage were observed and hence the study certified that the developed formulation is nonirritant. The encapsulation efficiency of the optimized batch showed 69.73% release profile of Timolol Maleate loaded nanoparticles initial burst followed by a very slow drug release and total cumulative release within 24 h ranged from 75 to 90%. In vitro release of the drug loaded batch showed that that the formulation undergo anomalous diffusion. In conclusion, the polymerization time extended it showed the maximum entrapment efficiency of 69.75 % and gives a sustained effect in ocular milieu.

Keywords: Ocular drug delivery, Chitosan, Timolol Maleate, Mucoadhesive nanoparticles, Glaucoma.


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