title: Ocular delivery of flurbiprofen based on Eudragit(®) E-flurbiprofen complex dispersed in aqueous solution: preparation, characterization, in vitro corneal penetration, and ocular irritation.
abstract: A novel ophthalmic formulation based on the ionic complexation between Eudragit E 100 (EU) and flurbiprofen (FB) is proposed. The selected complex composition, named EU-FBH50 Cl50 , had the basic groups of EU completely neutralized with equal molar amounts of FB and HCl. This complex, obtained in the solid state, exhibited a high aqueous compatibility producing a colloidal dispersion with a high positive electrokinetic potential, in which more than 99% of FB was ionically condensed with EU. In bicompartimental Franz cells, FB diffusion from the complex was very slow. However, dispersion in 0.9% NaCl increased the FB release through an ionic exchange, providing an optimal constant rate of delivery. Corneal FB permeation from 0.1% EU-FBH50 -Cl50 dispersed in 0.9% NaCl solution was substantially more effective compared with 0.1% FB solution, EU-FBH50 -Cl50 (Dex), or Tolerane(®) (a marketed formulation). This complex formulation was shown to be innocuous for rabbit ocular tissues because no irritant effects were evidenced.
authors.affiliation: Unidad de Investigación y Desarrollo en Tecnología Farmacéutica (UNITEFA)CONICET; Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, 5000-Córdoba, Argentina. Electronic address: dalemand@fcq.unc.edu.ar.
authors.forename: Daniela Alejandra
authors.initials: DA
authors.lastname: Quinteros
authors.affiliation: Unidad de Investigación y Desarrollo en Tecnología Farmacéutica (UNITEFA)CONICET; Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, 5000-Córdoba, Argentina.
authors.forename: Luis Ignacio
authors.initials: LI
authors.lastname: Tártara
authors.affiliation: Unidad de Investigación y Desarrollo en Tecnología Farmacéutica (UNITEFA)CONICET; Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, 5000-Córdoba, Argentina.
authors.forename: Santiago Daniel
authors.initials: SD
authors.lastname: Palma
authors.affiliation: Unidad de Investigación y Desarrollo en Tecnología Farmacéutica (UNITEFA)CONICET; Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, 5000-Córdoba, Argentina.
authors.forename: Ruben Hilario
authors.initials: RH
authors.lastname: Manzo
authors.affiliation: Unidad de Investigación y Desarrollo en Tecnología Farmacéutica (UNITEFA)CONICET; Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, 5000-Córdoba, Argentina.
authors.forename: Daniel Alberto
authors.initials: DA
authors.lastname: Allemandi
mesh_terms: D000818:Animals; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003315:Cornea / Q000187:drug effects*; D004337:Drug Carriers / Q000008:administration & dosage; D016503:Drug Delivery Systems / Q000379:methods; D004355:Drug Stability; D005480:Flurbiprofen / Q000008:administration & dosage*; D008768:Methylmethacrylates / Q000008:administration & dosage*; D009883:Ophthalmic Solutions / Q000008:administration & dosage*; D010316:Particle Size; D010539:Permeability; D011817:Rabbits
chemical_list: D004337:Drug Carriers; D008768:Methylmethacrylates; D009883:Ophthalmic Solutions; C102808:Eudragit-E; D005480:Flurbiprofen
keywords: Controlled release; Eudragit; Permeability; Polymeric drug delivery systems; complex; flurbiprofen; ophthalmic solution