title: Biopharmaceutical profile of pranoprofen-loaded PLGA nanoparticles containing hydrogels for ocular administration.
abstract: 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.
authors: Department of Physical Chemistry, Faculty of Pharmacy, University of Barcelona, Barcelona, Spain; Department of Biopharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Barcelona, Barcelona, Spain.
authors: Guadalupe
authors: G
authors: Abrego
authors: Department of Physical Chemistry, Faculty of Pharmacy, University of Barcelona, Barcelona, Spain; Department of Biopharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Barcelona, Barcelona, Spain.
authors: Helen
authors: H
authors: Alvarado
authors: Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Coimbra (FFUC), Pólo das Ciências da Saúde, Coimbra, Portugal; Center for Neuroscience and Cell Biology & Institute for Biomedical Imaging and Life Sciences (CNC-IBILI), University of Coimbra, Pólo das Ciências da Saúde, Coimbra, Portugal. Electronic address: ebsouto@ff.uc.pt.
authors: Eliana B
authors: EB
authors: Souto
authors: Department of Biopharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Barcelona, Barcelona, Spain.
authors: Bessy
authors: B
authors: Guevara
authors: Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Barcelona, Barcelona, Spain.
authors: Lyda Halbaut
authors: LH
authors: Bellowa
authors: Department of Physical Chemistry, Faculty of Pharmacy, University of Barcelona, Barcelona, Spain; Department of Biopharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Barcelona, Barcelona, Spain.
authors: Alexander
authors: A
authors: Parra
authors: Department of Biopharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Barcelona, Barcelona, Spain.
authors: Ana
authors: A
authors: Calpena
authors: Department of Physical Chemistry, Faculty of Pharmacy, University of Barcelona, Barcelona, Spain. Electronic address: marisagarcia@ub.edu.
authors: María Luisa
authors: ML
authors: Garcia
mesh_terms: D000180:Acrylic Resins / Q000737:chemistry; D060433:Administration, Ophthalmic; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D001381:Azepines / Q000737:chemistry; D001578:Benzopyrans / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D003315:Cornea / Q000378:metabolism; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000737:chemistry; D065546:Drug Liberation; D020100:Hydrogels; D019344:Lactic Acid / Q000737:chemistry*; D008297:Male; D053758:Nanoparticles; D010539:Permeability; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011422:Propionates / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D011817:Rabbits
chemical_list: D000180:Acrylic Resins; D000894:Anti-Inflammatory Agents, Non-Steroidal; D001381:Azepines; D001578:Benzopyrans; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D020100:Hydrogels; D011422:Propionates; C035229:laurocapram; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; C043940:pyranoprofen; D019344:Lactic Acid; C006903:carbopol 940
keywords: Anti-inflammatory efficacy; Azone; Corneal permeation; Hydrogel; Nanoparticles; Non-steroidal anti-inflammatory drug; Ocular tolerance; Physical stability; Pranoprofen; Pranoprofen (PubChem CID:4888)