title: Development and evaluation of a novel in situ gel of sparfloxacin for sustained ocular drug delivery: in vitro and ex vivo characterization.
abstract: Conventional eye drops are the most popular delivery systems in the treatment of various eye infections. However, the major problem encountered in these dosage forms is precorneal elimination of the drug, resulting in poor bioavailability and therapeutic response. To overcome the side effects of pulsed dosing, an attempt has been made to formulate and evaluate a novel in situ gelling system of Sparfloxacin for sustained ocular drug delivery (ion and pH triggered gelling system). These gelling systems involve the use of sodium alginate (ion sensitive polymer) used as gelling agent and methylcellulose as viscosity-enhancing agent. The developed formulations were evaluated for clarity, pH, gelling capacity, rheological study, in vitro release study, ex vivo corneal permeation study, ocular irritation studies (HET-CAM test) and histopathological study using isolated goat corneas. The formulations were found to be stable, non-irritant and showed sustained release of the drug for a period up to 24 h with no ocular damage. In situ gel of sparfloxacin could be prepared successfully promising their use in ophthalmic delivery.
authors.affiliation: Department of Pharmaceutics , Faculty of Pharmacy, Jamia Hamdard, New Delhi , India.
authors.forename: Nazia
authors.initials: N
authors.lastname: Khan
authors.forename: Mohammed
authors.initials: M
authors.lastname: Aqil
authors.forename: Syed Sarim
authors.initials: SS
authors.lastname: Imam
authors.forename: Asgar
authors.initials: A
authors.lastname: Ali
mesh_terms: D000464:Alginates / Q000737:chemistry*; D000818:Animals; D000890:Anti-Infective Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D003315:Cornea / Q000378:metabolism*; D003692:Delayed-Action Preparations / Q000737:chemistry*; D024841:Fluoroquinolones / Q000008:administration & dosage* / Q000493:pharmacokinetics; D005782:Gels / Q000737:chemistry; D020723:Glucuronic Acid / Q000737:chemistry; D006041:Goats; D006603:Hexuronic Acids / Q000737:chemistry; D006863:Hydrogen-Ion Concentration; D008747:Methylcellulose / Q000737:chemistry*; D009883:Ophthalmic Solutions / Q000737:chemistry; D014783:Viscosity
chemical_list: D000464:Alginates; D000890:Anti-Infective Agents; D003692:Delayed-Action Preparations; D024841:Fluoroquinolones; D005782:Gels; D006603:Hexuronic Acids; D009883:Ophthalmic Solutions; D020723:Glucuronic Acid; D008747:Methylcellulose; C061363:sparfloxacin
keywords: HET-CAM; in situ gel; methylcellulose; sodium alginate; sparfloxacin