title: Development of gatifloxacin-loaded cationic polymeric nanoparticles for ocular drug delivery.
abstract: The present investigation aimed at improving the ocular bioavailability of gatifloxacin by prolonging its residence time in the eye and reducing problems associated with the drug re-crystallization after application through incorporation into cationic polymeric nanoparticles. Gatifloxacin-loaded nanoparticles were prepared via the nanoprecipitation and double emulsion techniques. A 50:50 Eudragit® RL and RS mixture was used as cationic polymer with other formulation parameters varied. Prepared nanoparticles were evaluated for size, zeta potential, and drug loading. An optimized formulation was selected and further characterized for in vitro drug release, cytotoxicity, and antimicrobial activity. The double emulsion method produced larger nanoparticles than the nanoprecipitation method (410 nm and 68 nm, respectively). Surfactant choice also affected particle size and zeta potential with Tween 80 producing smaller-sized particles with higher zeta potential than PVA. However, the zeta potential was positive at all experimental conditions investigated. The optimal formulation produced by double emulsion technique and has achieved 46% drug loading. This formulation had optimal physicochemical properties with acceptable cytotoxicity results, and very prolonged release rate. The particles antimicrobial activities of the selected formulation have been tested against Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus and showed prolonged antimicrobial effect for gatifloxacin.
authors.affiliation: a Faculty of Medical and Health Sciences , School of Pharmacy, The University of Auckland , Auckland , New Zealand .
authors.forename: Linda
authors.initials: L
authors.lastname: Duxfield
authors.affiliation: a Faculty of Medical and Health Sciences , School of Pharmacy, The University of Auckland , Auckland , New Zealand .
authors.forename: Rubab
authors.initials: R
authors.lastname: Sultana
authors.affiliation: a Faculty of Medical and Health Sciences , School of Pharmacy, The University of Auckland , Auckland , New Zealand .
authors.forename: Ruokai
authors.initials: R
authors.lastname: Wang
authors.affiliation: a Faculty of Medical and Health Sciences , School of Pharmacy, The University of Auckland , Auckland , New Zealand .
authors.forename: Vanessa
authors.initials: V
authors.lastname: Englebretsen
authors.affiliation: a Faculty of Medical and Health Sciences , School of Pharmacy, The University of Auckland , Auckland , New Zealand .
authors.forename: Samantha
authors.initials: S
authors.lastname: Deo
authors.affiliation: c Department of Molecular Medicine and Pathology , Faculty of Medical and Health Sciences, University of Auckland , Auckland , New Zealand.
authors.forename: Simon
authors.initials: S
authors.lastname: Swift
authors.affiliation: b Buchanan Ocular Therapeutics Unit, Department of Ophthalmology, New Zealand National Eye Centre, Faculty of Medical and Health Sciences, University of Auckland , Auckland , New Zealand , and.
authors.forename: Ilva
authors.initials: I
authors.lastname: Rupenthal
authors.affiliation: a Faculty of Medical and Health Sciences , School of Pharmacy, The University of Auckland , Auckland , New Zealand .
authors.forename: Raida
authors.initials: R
authors.lastname: Al-Kassas
mesh_terms: D000890:Anti-Infective Agents / Q000008:administration & dosage / Q000737:chemistry; D001419:Bacteria / Q000187:drug effects; D001682:Biological Availability; D002412:Cations / Q000008:administration & dosage / Q000737:chemistry*; D002478:Cells, Cultured; D002626:Chemistry, Pharmaceutical / Q000379:methods; D016503:Drug Delivery Systems / Q000379:methods; D065546:Drug Liberation; D004655:Emulsions / Q000008:administration & dosage / Q000737:chemistry; D005123:Eye / Q000378:metabolism*; D024841:Fluoroquinolones / Q000008:administration & dosage / Q000737:chemistry*; D000077734:Gatifloxacin; D006801:Humans; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry*; D010316:Particle Size; D011108:Polymers / Q000008:administration & dosage / Q000737:chemistry*; D011136:Polysorbates / Q000737:chemistry; D013501:Surface-Active Agents / Q000008:administration & dosage / Q000737:chemistry
chemical_list: D000890:Anti-Infective Agents; D002412:Cations; D004655:Emulsions; D024841:Fluoroquinolones; D011108:Polymers; D011136:Polysorbates; D013501:Surface-Active Agents; D000077734:Gatifloxacin
keywords: Eudragit; gatifloxacin; nanoparticles; ocular drug delivery