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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Detalles Bibliográficos
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 recurso: artículo
Estado:Versión aceptada para publicación
Fecha de publicación:2018
País:España
Institución:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)
Repositorio:Recercat. Dipósit de la Recerca de Catalunya
OAI Identifier:oai:recercat.cat:2445/146039
Acceso en línea:https://hdl.handle.net/2445/146039
Access Level:acceso abierto
Palabra clave:Sistemes d'alliberament de medicaments
Nanopartícules
Farmacologia ocular
Agents antiinflamatoris
Drug delivery systems
Nanoparticles
Ocular pharmacology
Antiinflammatory agents
Descripción
Sumario: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