Formulation Development and Characterisation of Gemifloxacin Mesylate and Loteprednol Etabonate Ophthalmic Ocuserts

Abstract

Gemifloxacin Mesylate is a fluoroquinolone antibacterial drug preferably used in the treatment of bacterial conjunctivitis. The addition of Loteprednol Etabonate enhances the anti-inflammatory activity of the developed formulation. The objective of the present work was to develop ocular inserts of Gemifloxacin Mesylate with Loteprednol Etabonate and thereby evaluate its potential as a sustained ocular delivery system. Poor bioavailability and poor therapeutic responses are associated with conventional ophthalmic solutions due to many pre-corneal constraints. These constrain trigger the researcher's mind to formulate a controlled and sustained drug delivery system. Ocular inserts based on the solvent cast technique were formulated and characterized by in vitro drug release studies using a flow-through apparatus that simulated the eye conditions. Compatibility of Gemifloxacin Mesylate, Loteprednol Etabonate, polymer, and excipients was checked based on preformulation studies. Different combinations of Gemifloxacin Mesylate, Loteprednol Etabonate, Carbopol 974, 98 981, PEG 400, and glycerine were formulated by the solvent cast method and evaluated. Clarity, smoothness, surface pH, drug content, and in-vitro drug release study were the various parameters evaluated on the formulated ocusert. Formula GLE 74 fulfilled the needs of all organoleptic parameters and also the in-vitro release study. Based on in vitro correlation stability studies, it was concluded that this ocular inserts formulation could be a promising controlled release formulation.