FORMULATION AND ASSESSMENT OF GEMIFLOXACIN MESYLATE OCULAR IN SITU GELLING SYSTEM

Abstract

In situ gels are one of the most successful means of delivering the drug at ocular site with maximum bioavailability, which undergoes gelation upon instillation as drops into the eye due to physicochemical changes inherent to the biological fluids. The main aim of the present investigation was to obtain an ophthalmic drug delivery system with improved mucoadhesive and mechanical properties that could provide extended retention time for the treatment of ocular infections. For this in situ gels of Gemifloxacin Mesylate comprised of the combination of a thermosetting polymer, polaxamer with a mucoadhesive agent chitosan was developed. Fourier Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry techniques (DSC) were performed to know the compatibilities between drug and polymer. FTIR spectra and DSC thermograph of Gemifloxacin Mesylate formulations showed that there is no chemical interaction between drug and polymer and confirmed the stability of the drug. The gels were evaluated for pH, Gel strength, Gelling capacity, Rheology, Drug content uniformity and Ocular irritancy studies. In vitro drug release studies reveal that all the formulations showed sustained release of the drug in the range of 70.82 to 76.43 % for a period of 8 h. The optimized formulation was tested for ocular irritation study on male albino rabbit and the result indicated that the formulation was well tolerated, non-irritating and therapeutically efficacious. In conclusion in situ gelling systems containing polaxamer / chitosan solution are viable alternative to enhance bioavailability thus leads to an excellent potential alternative ophthalmic sustained-release formulation of Gemifloxacin Mesylate in ocular infections.