title: Preparation and in vitro-in vivo evaluation of ofloxacin loaded ophthalmic nano structured lipid carriers modified with chitosan oligosaccharide lactate for the treatment of bacterial keratitis.
abstract: The objective of this study was to explore the potential of the nanostructured lipid carriers (NLCs) modified with chitosan oligosaccharide lactate (COL) for topical ocular application. Ofloxacin (OFX) loaded NLCs were prepared by microemulsion or high shear homogenization methods. For combination of NLCs Compritol HD5 ATO was used as solid lipid, oleic acid as liquid lipid, Tween 80 as surfactant, ethanol as co-surfactant. The optimum NLCs was modified with 0.75% COL. The properties of NLCs in the absence or presence of OFX (0.3%) were characterized as zeta potential, particle size, viscosity and pH, TEM, drug loading, encapsulation efficiency and anti-microbial properties. Ex-vivo penetration/permeation studies were performed with rabbit cornea in Franz-diffusion cells. The penetration rate of OFX from NM-COL4OFX and NH-COL4OFX were significantly higher than commercial solution. Based on the selected formulations, in vivo tests were carried out by eye-drop instillation of NLCs in rabbit. The addition of COL improved the preocular residence time, controlled the drug release and enhanced the corneal bioavailability. In conclusion, OFX COL modified NLCs prepared by high shear homogenization method could be offered as a promising strategy for ocular drug delivery.
authors.affiliation: Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Ege, 35100 Bornova, Izmir, Turkey. Electronic address: neslihanustundag@yahoo.com.
authors.forename: Neslihan
authors.initials: N
authors.lastname: Ustündağ-Okur
authors.affiliation: Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Ege, 35100 Bornova, Izmir, Turkey. Electronic address: evrenhomangokce@gmail.com.
authors.forename: Evren Homan
authors.initials: EH
authors.lastname: Gökçe
authors.affiliation: Clinic of Eye Diseases, Uşak State Hospital, 64200 Uşak, Turkey. Electronic address: duyguincibozbyk@gmail.com.
authors.forename: Duygu İnci
authors.initials: Dİ
authors.lastname: Bozbıyık
authors.affiliation: Department of Ophthalmology, School of Medicine, University of Ege, 35100 Bornova, Izmir, Turkey. Electronic address: saitegrilmez@gmail.com.
authors.forename: Sait
authors.initials: S
authors.lastname: Eğrilmez
authors.affiliation: Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Ege, 35100 Bornova, Izmir, Turkey. Electronic address: ozgen.ozer@ege.edu.tr.
authors.forename: Ozgen
authors.initials: O
authors.lastname: Ozer
authors.affiliation: Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Ege, 35100 Bornova, Izmir, Turkey. Electronic address: gokhan.ertan@ege.edu.tr.
authors.forename: Gökhan
authors.initials: G
authors.lastname: Ertan
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D048271:Chitosan / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry*; D004926:Escherichia coli / Q000187:drug effects; D006863:Hydrogen-Ion Concentration; D007634:Keratitis / Q000188:drug therapy*; D007773:Lactates / Q000737:chemistry; D008055:Lipids / Q000737:chemistry*; D008297:Male; D008826:Microbial Sensitivity Tests; D053758:Nanoparticles / Q000737:chemistry*; D015242:Ofloxacin / Q000737:chemistry / Q000494:pharmacology*; D010316:Particle Size; D011817:Rabbits; D013211:Staphylococcus aureus / Q000187:drug effects; D013499:Surface Properties; D014783:Viscosity
chemical_list: D000900:Anti-Bacterial Agents; D004337:Drug Carriers; D007773:Lactates; D008055:Lipids; D048271:Chitosan; D015242:Ofloxacin
keywords: Bacterial keratitis; Nanostructured lipid carriers; Ocular delivery; Ofloxacin; Topical application