title: Improved corneal bioavailability of ofloxacin: biodegradable microsphere-loaded ion-activated in situ gel delivery system.
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 and OFX microspheres. In vivo results in rabbits showed that OFX-loaded microspheres in situ gel formula improved the relative bioavailability by 11.7-fold compared with the commercially available OFX eyedrops. In addition, the longer duration of action of OFX-loaded microspheres in situ gel formula preparations is thought to avoid frequent instillations, which improves patient tolerability and compliance.
authors: Department of Pharmaceutical Technology, Faculty of Pharmacy, Minia University, Minia, Egypt.
authors: Elshaimaa G
authors: EG
authors: Sayed
authors: Department of Pharmaceutical Technology, Faculty of Pharmacy, Minia University, Minia, Egypt.
authors: Amal K
authors: AK
authors: Hussein
authors: Department of Pharmaceutical Technology, Faculty of Pharmacy, Minia University, Minia, Egypt.
authors: Khaled A
authors: KA
authors: Khaled
authors: Department of Pharmaceutical Technology, Faculty of Pharmacy, Minia University, Minia, Egypt ; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia.
authors: Osama A A
authors: OA
authors: Ahmed
mesh_terms: D000818:Animals; D001682:Biological Availability; D003315:Cornea / Q000378:metabolism*; D016503:Drug Delivery Systems; D005782:Gels / Q000008:administration & dosage* / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D007477:Ions / Q000737:chemistry; D008297:Male; D008863:Microspheres; D015242:Ofloxacin / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D010316:Particle Size; D011098:Polyglactin 910 / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D011135:Polysaccharides, Bacterial / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D011817:Rabbits; D013499:Surface Properties
chemical_list: D005782:Gels; D007477:Ions; D011135:Polysaccharides, Bacterial; D011098:Polyglactin 910; C048288:gellan gum; D015242:Ofloxacin
keywords: Gelrite; corneal delivery; fluoroquinolones; gellan gum; simulated tear fluid