Abstract

Due to the unique structure of the eye, which inhibits the entry of drug molecules into the desired site, the ophthalmic delivery of the drug has been one of the most challenging tasks for a pharmaceutical scientist. For this reason, in this investigation a novel microsponge for an anti-glaucoma drug, Dorzolamide hydrochloride, was formulated as in situ gel for ocular administration with an aim to improve its therapeutic efficacy and reduce the systemic adverse effects. The microsponges were prepared by the quasi emulsion solvent diffusion method and was incorporated into 20% pluronic F-127 which led to consistent in situ gel at 35°C. They were evaluated for physicochemical properties like pH, gelling capacity, gelation time, rheological properties and release profile and ocular irritancy test. The prepared Dorzolamide hydrochloride microsponges showed high entrapment efficiency of 85% and mean particle size of 2 μm with polydispersity index (PDI) of 0.77 which are ideal for ocular delivery. These microsponges is formulated into in situ gel which showed higher therapeutic efficacy compared to free drug in gel. It was found to be non-irritant to the rabbit’s eye. These results confirms that Dorzolamide hydrochloride microsponges in situ gels have promising features, benefits and advantages for a novel ophthalmic drug delivery to treat glaucoma.

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