Biopharmaceutical profile of pranoprofen-loaded PLGA nanoparticles containing hydrogels for ocular administration

[Display omitted] •Pranoprofen-PLGA nanoparticles dispersed in Carbomer 934 hydrogels were produced.•Azone showed an optimal ocular tolerance in vitro and in vivo.•PLGA nanoparticles exhibited sustained release behavior of pranoprofen.•Pranoprofen-PLGA nanoparticles significantly reduced the ocular...

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Bibliographic Details
Published in:European journal of pharmaceutics and biopharmaceutics 2015-09, Vol.95 (Pt B), p.261-270
Main Authors: Abrego, Guadalupe, Alvarado, Helen, Souto, Eliana B., Guevara, Bessy, Bellowa, Lyda Halbaut, Parra, Alexander, Calpena, Ana, Garcia, María Luisa
Format: Article
Language:English
Subjects:
Acrylic Resins - chemistry
Administració de medicaments
Administration of drugs
Administration, Ophthalmic
Animals
Anti-Inflammatory Agents, Non-Steroidal - administration & dosage
Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics
Anti-Inflammatory Agents, Non-Steroidal - pharmacology
Anti-inflammatory efficacy
Antiinflamatoris no esteroïdals
Azepines - chemistry
Azone
Benzopyrans - administration & dosage
Benzopyrans - pharmacokinetics
Benzopyrans - pharmacology
Cornea - metabolism
Corneal permeation
Delayed-Action Preparations
Drug Carriers - chemistry
Drug Liberation
Hydrogel
Hydrogels
Lactic Acid - chemistry
Male
Nanoparticles
Nanopartícules
Non-steroidal anti-inflammatory drug
Nonsteroidal anti-inflammatory agents
Ocular tolerance
Ophthalmological therapeutics
Permeability
Physical stability
Polyglycolic Acid - chemistry
Pranoprofen
Propionates - administration & dosage
Propionates - pharmacokinetics
Propionates - pharmacology
Rabbits
Terapèutica oftalmològica
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Summary:[Display omitted] •Pranoprofen-PLGA nanoparticles dispersed in Carbomer 934 hydrogels were produced.•Azone showed an optimal ocular tolerance in vitro and in vivo.•PLGA nanoparticles exhibited sustained release behavior of pranoprofen.•Pranoprofen-PLGA nanoparticles significantly reduced the ocular edema. Two optimized pranoprofen-loaded poly-l-lactic-co glycolic acid (PLGA) nanoparticles (PF-F1NPs; PF-F2NPs) have been developed and further dispersed into hydrogels for the production of semi-solid formulations intended for ocular administration. The optimized PF-NP suspensions were dispersed in freshly prepared carbomer hydrogels (HG_PF-F1NPs and HG_PF-F2NPs) or in hydrogels containing 1% azone (HG_PF-F1NPs-Azone and HG_PF-F2NPs-Azone) in order to improve the ocular biopharmaceutical profile of the selected non-steroidal anti-inflammatory drug (NSAID), by prolonging the contact of the pranoprofen with the eye, increasing the drug retention in the organ and enhancing its anti-inflammatory and analgesic efficiency. Carbomer 934 has been selected as gel-forming polymer. The hydrogel formulations with or without azone showed a non-Newtonian behavior and adequate physicochemical properties for ocular instillation. The release study of pranoprofen from the semi-solid formulations exhibited a sustained release behavior. The results obtained from ex vivo corneal permeation and in vivo anti-inflammatory efficacy studies suggest that the ocular application of the hydrogels containing azone was more effective over the azone-free formulations in the treatment of edema on the ocular surface. No signs of ocular irritancy have been detected for the produced hydrogels.
ISSN:0939-6411
1873-3441
DOI:10.1016/j.ejpb.2015.01.026