Abstract

FORMULATION AND EVALUATION OF OPHTHALMIC DRUG DELIVERY SYSTEM FOR LEVOFLOXACIN HEMIHYDRATE AND KETOROLAC TROMETHAMINE

Shramika A. Chore* and Dr. S. J. Dighade

Abstract

Eye is a very sensitive organ and can get infected from bacteria, fungi, or viruses. Common eye infection are conjunctivitis and corneal ulcers. Conjunctivitis is a swelling (inflammation) or infection of the membrane lining the eyelids. Corneal ulcers are characterized by corneal edema, cellular infiltration and ciliary congestion. Currently available antimicrobials used in the prevention and treatment of these infections include antivirals, antifungals and antibacterials. Common topical antibacterial used in treatment of ocular infectious diseases include sulfonamides, aminoglycosides, polymyxin based combinations and fluoroquinolones.[10] Levofloxacin is a third generation fluoroquinolone derivative used to treat acute and sub-acute infections of the eye viz. conjunctivitis, bacterial keratitits and ketorolac conjunctivitis. Levofloxacin represent an expanding class of broad spectrum antibacterial which are effective against most of the gram negative and anaerobic species responsible for ocular infection. Ketorolac is a non steroidal anti inflammatory drug (NSAID) used to treat inflammation and sub acute inflammation of the eye. This can be achieved by using in situ gel forming ophthalmic drug delivery systems prepared from polymers that exhibit reversible phase transitions (sol-gel-sol) and pseudoplastic behavior. Out of various ophthalmic dosage forms, ophthalmic solutions are the most preferred dosage form due to the obvious reasons of patient convenience. 90% of the currently available ophthalmic formulations are solutions. However, they suffer from shorter residence time at the site of action and faster nasolacrimal drainage which subsequently leads to the need for frequent instillation.[48] This situation is more common when the patient is suffering from acute infections caused by pathogenesis bacteria and is undergoing treatment with potent antibacterial agents like Levofloxacin Hemihydrate. In the present study, an attempt has been made to develop and evaluate in situ gel forming ophthalmic drug delivery system of Levofloxacin Hemihydrate and Ketorolac Tromethamine by using various polymers like Poloxamer 407, Carbopol 974, HEC, HPMC. In the present study, various in-situ gelling opthalamic formulations of poloxamer 407 in concentration of 16-20% w/w (P1-P5). Further, different formulations of poloxamer 407 (18%w/w) were prepared by combining with HEC in concentration of 0.2, 0.4, 0.6%w/w (P12-P14) and HPMC E50 LV in concentration of 0.2, 0.4, 0.6%w/w (P15-P17). All above are prepared with Levofloxacin Hemihydrate. So, with Ketorolac Tromethamine three batches also prepared i.e poloxamer 407(18%w/w), poloxamer (18%w/w) and HEC (0.4%w/w) last one poloxamer407 (18%w/w) and HPMC E50 LV (0.4%w/w). All these opthalamic formulations were evaluated for appearance, clarity, pH, gelling ability, viscosity and percent drug release. The formulations showing transparent and clear appearance, quick and stable gelation, shear thinning properties, excellent sustained drug release upto 75-85% after 8hrs were selected for further characterization. The optimized formulations P21, P22 and P23 showed excellent mucoadhesion and drug release. These formulations were found to be stable to autoclaving, at ambient conditions and non-irritant to eye.

Keywords: Levofloxacin Hemihydrate, Ketorolac Tromethamine, poloxamer 407, HPMC E50 LV, Carbopol 974 etc.