Ocular Delivery of Flurbiprofen Based on Eudragit® E-Flurbiprofen Complex Dispersed in Aqueous Solution: Preparation, Characterization, In Vitro Corneal Penetration, and Ocular Irr...

Autores
Quinteros, Daniela Alejandra; Tartara, Luis Ignacio; Palma, Santiago Daniel; Manzo, Ruben Hilario; Allemandi, Daniel Alberto
Año de publicación
2014
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
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–FBH50Cl50, 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 ToleraneR (a marketed formulation). This complex formulation was shown to be innocuous for rabbit ocular tissues because no irritant effects were evidenced.
Fil: Quinteros, Daniela Alejandra. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Fil: Tartara, Luis Ignacio. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Fil: Palma, Santiago Daniel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Fil: Manzo, Ruben Hilario. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Fil: Allemandi, Daniel Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Materia
Flurbiprofen
Eudragit
Complex
Ophthalmic Solution
Permeability
Polymeric Drug Delivery Systems
Controlled Release
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/32360
Acceder
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network_name_str CONICET Digital (CONICET)
spelling Ocular Delivery of Flurbiprofen Based on Eudragit® E-Flurbiprofen Complex Dispersed in Aqueous Solution: Preparation, Characterization, In Vitro Corneal Penetration, and Ocular IrritationQuinteros, Daniela AlejandraTartara, Luis IgnacioPalma, Santiago DanielManzo, Ruben HilarioAllemandi, Daniel AlbertoFlurbiprofenEudragitComplexOphthalmic SolutionPermeabilityPolymeric Drug Delivery SystemsControlled Releasehttps://purl.org/becyt/ford/3.2https://purl.org/becyt/ford/3A novel ophthalmic formulation based on the ionic complexation between Eudragit E 100 (EU) and flurbiprofen (FB) is proposed. The selected complex composition, named EU–FBH50Cl50, 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 ToleraneR (a marketed formulation). This complex formulation was shown to be innocuous for rabbit ocular tissues because no irritant effects were evidenced.Fil: Quinteros, Daniela Alejandra. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; ArgentinaFil: Tartara, Luis Ignacio. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; ArgentinaFil: Palma, Santiago Daniel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; ArgentinaFil: Manzo, Ruben Hilario. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; ArgentinaFil: Allemandi, Daniel Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; ArgentinaElsevier2014-08info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/32360Allemandi, Daniel Alberto; Manzo, Ruben Hilario; Palma, Santiago Daniel; Tartara, Luis Ignacio; Quinteros, Daniela Alejandra; Ocular Delivery of Flurbiprofen Based on Eudragit® E-Flurbiprofen Complex Dispersed in Aqueous Solution: Preparation, Characterization, In Vitro Corneal Penetration, and Ocular Irritation; Elsevier; Journal of Pharmaceutical Sciences; 103; 12; 8-2014; 3859-38680022-3549CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/doi/10.1002/jps.24153info:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0022354915302835info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-29T10:41:55Zoai:ri.conicet.gov.ar:11336/32360instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982025-09-29 10:41:55.992CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Ocular Delivery of Flurbiprofen Based on Eudragit® E-Flurbiprofen Complex Dispersed in Aqueous Solution: Preparation, Characterization, In Vitro Corneal Penetration, and Ocular Irritation
title Ocular Delivery of Flurbiprofen Based on Eudragit® E-Flurbiprofen Complex Dispersed in Aqueous Solution: Preparation, Characterization, In Vitro Corneal Penetration, and Ocular Irritation
spellingShingle Ocular Delivery of Flurbiprofen Based on Eudragit® E-Flurbiprofen Complex Dispersed in Aqueous Solution: Preparation, Characterization, In Vitro Corneal Penetration, and Ocular Irritation
Quinteros, Daniela Alejandra
Flurbiprofen
Eudragit
Complex
Ophthalmic Solution
Permeability
Polymeric Drug Delivery Systems
Controlled Release
title_short Ocular Delivery of Flurbiprofen Based on Eudragit® E-Flurbiprofen Complex Dispersed in Aqueous Solution: Preparation, Characterization, In Vitro Corneal Penetration, and Ocular Irritation
title_full Ocular Delivery of Flurbiprofen Based on Eudragit® E-Flurbiprofen Complex Dispersed in Aqueous Solution: Preparation, Characterization, In Vitro Corneal Penetration, and Ocular Irritation
title_fullStr Ocular Delivery of Flurbiprofen Based on Eudragit® E-Flurbiprofen Complex Dispersed in Aqueous Solution: Preparation, Characterization, In Vitro Corneal Penetration, and Ocular Irritation
title_full_unstemmed Ocular Delivery of Flurbiprofen Based on Eudragit® E-Flurbiprofen Complex Dispersed in Aqueous Solution: Preparation, Characterization, In Vitro Corneal Penetration, and Ocular Irritation
title_sort Ocular Delivery of Flurbiprofen Based on Eudragit® E-Flurbiprofen Complex Dispersed in Aqueous Solution: Preparation, Characterization, In Vitro Corneal Penetration, and Ocular Irritation
dc.creator.none.fl_str_mv Quinteros, Daniela Alejandra
Tartara, Luis Ignacio
Palma, Santiago Daniel
Manzo, Ruben Hilario
Allemandi, Daniel Alberto
author Quinteros, Daniela Alejandra
author_facet Quinteros, Daniela Alejandra
Tartara, Luis Ignacio
Palma, Santiago Daniel
Manzo, Ruben Hilario
Allemandi, Daniel Alberto
author_role author
author2 Tartara, Luis Ignacio
Palma, Santiago Daniel
Manzo, Ruben Hilario
Allemandi, Daniel Alberto
author2_role author
author
author
author
dc.subject.none.fl_str_mv Flurbiprofen
Eudragit
Complex
Ophthalmic Solution
Permeability
Polymeric Drug Delivery Systems
Controlled Release
topic Flurbiprofen
Eudragit
Complex
Ophthalmic Solution
Permeability
Polymeric Drug Delivery Systems
Controlled Release
purl_subject.fl_str_mv https://purl.org/becyt/ford/3.2
https://purl.org/becyt/ford/3
dc.description.none.fl_txt_mv 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–FBH50Cl50, 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 ToleraneR (a marketed formulation). This complex formulation was shown to be innocuous for rabbit ocular tissues because no irritant effects were evidenced.
Fil: Quinteros, Daniela Alejandra. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Fil: Tartara, Luis Ignacio. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Fil: Palma, Santiago Daniel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Fil: Manzo, Ruben Hilario. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Fil: Allemandi, Daniel Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
description 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–FBH50Cl50, 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 ToleraneR (a marketed formulation). This complex formulation was shown to be innocuous for rabbit ocular tissues because no irritant effects were evidenced.
publishDate 2014
dc.date.none.fl_str_mv 2014-08
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
http://purl.org/coar/resource_type/c_6501
info:ar-repo/semantics/articulo
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/11336/32360
Allemandi, Daniel Alberto; Manzo, Ruben Hilario; Palma, Santiago Daniel; Tartara, Luis Ignacio; Quinteros, Daniela Alejandra; Ocular Delivery of Flurbiprofen Based on Eudragit® E-Flurbiprofen Complex Dispersed in Aqueous Solution: Preparation, Characterization, In Vitro Corneal Penetration, and Ocular Irritation; Elsevier; Journal of Pharmaceutical Sciences; 103; 12; 8-2014; 3859-3868
0022-3549
CONICET Digital
CONICET
url http://hdl.handle.net/11336/32360
identifier_str_mv Allemandi, Daniel Alberto; Manzo, Ruben Hilario; Palma, Santiago Daniel; Tartara, Luis Ignacio; Quinteros, Daniela Alejandra; Ocular Delivery of Flurbiprofen Based on Eudragit® E-Flurbiprofen Complex Dispersed in Aqueous Solution: Preparation, Characterization, In Vitro Corneal Penetration, and Ocular Irritation; Elsevier; Journal of Pharmaceutical Sciences; 103; 12; 8-2014; 3859-3868
0022-3549
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/doi/10.1002/jps.24153
info:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0022354915302835
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
application/pdf
application/pdf
dc.publisher.none.fl_str_mv Elsevier
publisher.none.fl_str_mv Elsevier
dc.source.none.fl_str_mv reponame:CONICET Digital (CONICET)
instname:Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str CONICET Digital (CONICET)
collection CONICET Digital (CONICET)
instname_str Consejo Nacional de Investigaciones Científicas y Técnicas
repository.name.fl_str_mv CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas
repository.mail.fl_str_mv dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar
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score 13.070432

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