Development of fluorometholone-loaded PLGA nanoparticles for treatment of inflammatory disorders of anterior and posterior segments of the eye

The main objective of this study was the development and optimization of fluorometholone-loaded PLGA nanoparticles for the treatment of inflammatory conditions of the eye. Design of experiments was used to obtain nanoparticles with the best physicochemical characteristics. The optimized nanoparticle...

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Autores: González Pizarro, Roberto Carlos, Silva Abreu, Marcelle, Calpena Campmany, Ana Cristina, Egea Gras, Ma. Antonia, Espina García, Marta, García López, María Luisa
Tipo de documento: artigo
Estado:Versión aceptada para publicación
Data de publicação:2018
País:España
Recursos:Universidad de Barcelona
Repositório:Dipòsit Digital de la UB
OAI Identifier:oai:diposit.ub.edu:2445/146039
Acesso em linha:https://hdl.handle.net/2445/146039
Access Level:Acceso aberto
Palavra-chave:Sistemes d'alliberament de medicaments
Nanopartícules
Farmacologia ocular
Agents antiinflamatoris
Drug delivery systems
Nanoparticles
Ocular pharmacology
Antiinflammatory agents
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spelling Development of fluorometholone-loaded PLGA nanoparticles for treatment of inflammatory disorders of anterior and posterior segments of the eyeGonzález Pizarro, Roberto CarlosSilva Abreu, MarcelleCalpena Campmany, Ana CristinaEgea Gras, Ma. AntoniaEspina García, MartaGarcía López, María LuisaSistemes d'alliberament de medicamentsNanopartículesFarmacologia ocularAgents antiinflamatorisDrug delivery systemsNanoparticlesOcular pharmacologyAntiinflammatory agentsThe main objective of this study was the development and optimization of fluorometholone-loaded PLGA nanoparticles for the treatment of inflammatory conditions of the eye. Design of experiments was used to obtain nanoparticles with the best physicochemical characteristics. The optimized nanoparticles containing 1.5 mg·mL-1 of fluorometholone showed a negative surface charge (-30 mV) and an average size below 200 nm being suitable for ocular administration. Drug-polymer interaction studies confirmed no new bonds were formed during the synthesis. Nanoparticles performance was assessed with biopharmaceutical behavior studies, ocular tolerance, anti-inflammatory efficacy and bioavailability. The biopharmaceutical behavior of the drug from nanoparticles was adjusted to hyperbola order showing a significantly greater permeation in the cornea than in the sclera. The optimized formulation had significantly greater anti-inflammatory effects than the commercial formulation. In addition, nanoparticles increased drug penetration toward the vitreous. Polymeric nanoparticles of fluorometholone could provide a suitable alternative for the treatment of inflammatory disorders of the anterior and posterior segments of the eye against of conventional topical formulations. KEYWORDS: Drug delivery; Fluorometholone; Nanoparticles; Ocular anti-inflammatory; PLGA; PermeationElsevier B.V.2018info:eu-repo/semantics/articleinfo:eu-repo/semantics/acceptedVersionapplication/pdfhttps://hdl.handle.net/2445/146039Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica)reponame:Dipòsit Digital de la UBinstname:Universidad de BarcelonaInglésVersió postprint del document publicat a: https://doi.org/10.1016/j.ijpharm.2018.05.050International Journal of Pharmaceutics, 2018, vol. 547, num. 1-2, p. 338-346https://doi.org/10.1016/j.ijpharm.2018.05.050cc-by-nc-nd (c) Elsevier B.V., 2018http://creativecommons.org/licenses/by-nc-nd/3.0/esinfo:eu-repo/semantics/openAccessoai:diposit.ub.edu:2445/1460392026-05-27T06:46:51Z
dc.title.none.fl_str_mv Development of fluorometholone-loaded PLGA nanoparticles for treatment of inflammatory disorders of anterior and posterior segments of the eye
title Development of fluorometholone-loaded PLGA nanoparticles for treatment of inflammatory disorders of anterior and posterior segments of the eye
spellingShingle Development of fluorometholone-loaded PLGA nanoparticles for treatment of inflammatory disorders of anterior and posterior segments of the eye
González Pizarro, Roberto Carlos
Sistemes d'alliberament de medicaments
Nanopartícules
Farmacologia ocular
Agents antiinflamatoris
Drug delivery systems
Nanoparticles
Ocular pharmacology
Antiinflammatory agents
title_short Development of fluorometholone-loaded PLGA nanoparticles for treatment of inflammatory disorders of anterior and posterior segments of the eye
title_full Development of fluorometholone-loaded PLGA nanoparticles for treatment of inflammatory disorders of anterior and posterior segments of the eye
title_fullStr Development of fluorometholone-loaded PLGA nanoparticles for treatment of inflammatory disorders of anterior and posterior segments of the eye
title_full_unstemmed Development of fluorometholone-loaded PLGA nanoparticles for treatment of inflammatory disorders of anterior and posterior segments of the eye
title_sort Development of fluorometholone-loaded PLGA nanoparticles for treatment of inflammatory disorders of anterior and posterior segments of the eye
dc.creator.none.fl_str_mv González Pizarro, Roberto Carlos
Silva Abreu, Marcelle
Calpena Campmany, Ana Cristina
Egea Gras, Ma. Antonia
Espina García, Marta
García López, María Luisa
author González Pizarro, Roberto Carlos
author_facet González Pizarro, Roberto Carlos
Silva Abreu, Marcelle
Calpena Campmany, Ana Cristina
Egea Gras, Ma. Antonia
Espina García, Marta
García López, María Luisa
author_role author
author2 Silva Abreu, Marcelle
Calpena Campmany, Ana Cristina
Egea Gras, Ma. Antonia
Espina García, Marta
García López, María Luisa
author2_role author
author
author
author
author
dc.subject.none.fl_str_mv Sistemes d'alliberament de medicaments
Nanopartícules
Farmacologia ocular
Agents antiinflamatoris
Drug delivery systems
Nanoparticles
Ocular pharmacology
Antiinflammatory agents
topic Sistemes d'alliberament de medicaments
Nanopartícules
Farmacologia ocular
Agents antiinflamatoris
Drug delivery systems
Nanoparticles
Ocular pharmacology
Antiinflammatory agents
description The main objective of this study was the development and optimization of fluorometholone-loaded PLGA nanoparticles for the treatment of inflammatory conditions of the eye. Design of experiments was used to obtain nanoparticles with the best physicochemical characteristics. The optimized nanoparticles containing 1.5 mg·mL-1 of fluorometholone showed a negative surface charge (-30 mV) and an average size below 200 nm being suitable for ocular administration. Drug-polymer interaction studies confirmed no new bonds were formed during the synthesis. Nanoparticles performance was assessed with biopharmaceutical behavior studies, ocular tolerance, anti-inflammatory efficacy and bioavailability. The biopharmaceutical behavior of the drug from nanoparticles was adjusted to hyperbola order showing a significantly greater permeation in the cornea than in the sclera. The optimized formulation had significantly greater anti-inflammatory effects than the commercial formulation. In addition, nanoparticles increased drug penetration toward the vitreous. Polymeric nanoparticles of fluorometholone could provide a suitable alternative for the treatment of inflammatory disorders of the anterior and posterior segments of the eye against of conventional topical formulations. KEYWORDS: Drug delivery; Fluorometholone; Nanoparticles; Ocular anti-inflammatory; PLGA; Permeation
publishDate 2018
dc.date.none.fl_str_mv 2018
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/acceptedVersion
format article
status_str acceptedVersion
dc.identifier.none.fl_str_mv https://hdl.handle.net/2445/146039
url https://hdl.handle.net/2445/146039
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv Versió postprint del document publicat a: https://doi.org/10.1016/j.ijpharm.2018.05.050
International Journal of Pharmaceutics, 2018, vol. 547, num. 1-2, p. 338-346
https://doi.org/10.1016/j.ijpharm.2018.05.050
dc.rights.none.fl_str_mv cc-by-nc-nd (c) Elsevier B.V., 2018
http://creativecommons.org/licenses/by-nc-nd/3.0/es
info:eu-repo/semantics/openAccess
rights_invalid_str_mv cc-by-nc-nd (c) Elsevier B.V., 2018
http://creativecommons.org/licenses/by-nc-nd/3.0/es
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv Elsevier B.V.
publisher.none.fl_str_mv Elsevier B.V.
dc.source.none.fl_str_mv Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica)
reponame:Dipòsit Digital de la UB
instname:Universidad de Barcelona
instname_str Universidad de Barcelona
reponame_str Dipòsit Digital de la UB
collection Dipòsit Digital de la UB
repository.name.fl_str_mv
repository.mail.fl_str_mv
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