Abstract

Levofloxacin is a fluoroquinolone antibacterial drug effective in the treatment of bacterial conjunctivitis. The objective of the present work was to develop ocular inserts of levofloxacin and evaluate their potential for sustained ocular delivery. Conventional ophthalmic solution shows the poor bioavailability and therapeutic response due t many pre-corneal constraints. These constrains necessitates the controlled and sustained drug delivery to become standard one in modern pharmaceutical era Matrix type ocular inserts were prepared by the film casting technique in Teflon coated Petri dishes and characterized in vitro by drug release studies using a flow through apparatus that simulated the eye conditions. Nine formulations were developed, which differed in the ratio of polymers - chitoson, polyvinyl alcohol (PVA). All the formulations were subjected to evaluation of thickness, weight variation, folding endurance, drug content uniformity, in vitro release study, Surface pH, Swelling Studies (Swelling Index), % Moisture absorption, Release Kinetics, and Ocular Irritation Studies. On the basis of in vitro drug release studies, the formulation L9 was found to be better than the other formulations and it was selected as an optimized formulation.

Highlights

  • Continuous delivery of drugs to the eye offers major advantages over conventional therapies that involve administration of drug solutions or suspensions as eye drops

  • Eye drop administration often results in poor bioavailability and therapeutic response due to rapid precorneal elimination of the drug and is associated with patient compliance problems 1-2

  • Levofloxacin eye drop is available in the market for the treatment of anti bacterials 12

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Summary

Introduction

Continuous delivery of drugs to the eye offers major advantages over conventional therapies that involve administration of drug solutions or suspensions as eye drops. Ophthalmic inserts offer many advantages over conventional dosages forms, like increased ocular residence, possibility of releasing drug at a slow and constant rate, accurate dosing, exclusion of preservatives and increased shelf life. Eye drops and eye ointments are conventional ocular dosage forms They have certain disadvantages like frequent administration, poor availability, massive and unpredictable doses, and drainage of medication by tear and naso-lacrimal fluid[6,7,8]. These factors require formulating a controlled release ocular drug delivery system which maintains a steady state drug release. An attempt was made to formulate ocuserts of levofloxacin using polymers like chitoson and PVA www.ssjournals.com

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