Improved corneal bioavailability of ofloxacin: biodegradable microsphere-loaded ion-activated in situ gel delivery system

Drug Design, Development and Therapy
Elshaimaa G SayedOsama A A Ahmed

Abstract

The aim of the study was to improve corneal penetration and bioavailability of ofloxacin (OFX) eye preparations. OFX was incorporated in poly (lactide-co-glycolide) as biodegradable microspheres using oil in oil emulsion solvent evaporation technique. The prepared OFX microspheres were then incorporated in Gelrite(®) in situ gel preparation. In addition, OFX Gelrite-based in situ gel formulations were prepared. OFX formulations were characterized for gelling capacity, viscosity, and rheological properties. Release studies for OFX microspheres, OFX in situ gel, and OFX-loaded microspheres in situ gel formulations were carried out to investigate release characteristics of the drug. The prepared OFX formulations were then investigated in vivo compared with commercially available OFX eyedrops. Results showed that the optimum Gelrite concentration was at 0.4%-0.7% w/v; the prepared formulations were viscous liquid transformed into a pourable gel immediately after the addition of simulated tear fluid with a gelling factor of 27-35. Incorporation of OFX-loaded microspheres in Gelrite solution (0.4% w/v) significantly altered the release profiles of OFX-loaded microspheres in situ gel formula compared with the corresponding OFX gels an...Continue Reading

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Young Lin Autochro - 3000
Winspec

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