Biopharmaceutical profile of pranoprofen-loaded PLGA nanoparticles containing hydrogels for ocular administration.
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.
['Abrego|Guadalupe|G|', 'Alvarado|Helen|H|', 'Souto|Eliana B|EB|', 'Guevara|Bessy|B|', 'Bellowa|Lyda Halbaut|LH|', 'Parra|Alexander|A|', 'Calpena|Ana|A|', 'Garcia|María Luisa|ML|']
D000180:Acrylic Resins D060433:Administration, Ophthalmic D000818:Animals D000894:Anti-Inflammatory Agents, Non-Steroidal D001381:Azepines D001578:Benzopyrans D003315:Cornea D003692:Delayed-Action Preparations D004337:Drug Carriers D065546:Drug Liberation D020100:Hydrogels D019344:Lactic Acid D008297:Male D053758:Nanoparticles D010539:Permeability D011100:Polyglycolic Acid D000077182:Polylactic Acid-Polyglycolic Acid Copolymer D011422:Propionates D011817:Rabbits
Nanoparticles Hydrogel Azone Non-steroidal anti-inflammatory drug Pranoprofen Corneal permeation Anti-inflammatory efficacy Ocular tolerance Physical stability Pranoprofen (PubChem CID:4888)