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Biopharmaceutical profile of pranoprofen-loaded PLGA nanoparticles containing hydrogels for ocular administration Abrego Escobar, Guadalupe Alvarado, Helen Souto, Eliana B. Guevara, Bessy Halbaut, Lyda Parra Coca, Alexander Calpena Campmany, Ana Cristina García López, María Luisa Antiinflamatoris no esteroïdals Nanopartícules Terapèutica oftalmològica Administració de medicaments Nonsteroidal anti-inflammatory agents Nanoparticles Ophthalmological therapeutics Administration of drugs Two optimized pranoprofen-loaded poly-L-lactic-co glycolic acid (PLGA) nanoparticles (PF-F1NPs; PF- 39 F2NPs) have been developed and further dispersed into hydrogels for the production of semi-solid formu- 40 lations intended for ocular administration. The optimized PF-NP suspensions were dispersed in freshly 41 prepared carbomer hydrogels (HG_PF-F1NPs and HG_PF-F2NPs) or in hydrogels containing 1% azone 42 (HG_PF-F1NPs-Azone and HG_PF-F2NPs-Azone) in order to improve the ocular biopharmaceutical profile 43 of the selected non-steroidal anti-inflammatory drug (NSAID), by prolonging the contact of the pranopro- 44 fen with the eye, increasing the drug retention in the organ and enhancing its anti-inflammatory and 45 analgesic efficiency. Carbomer 934 has been selected as gel-forming polymer. The hydrogel formulations 46 with or without azone showed a non-Newtonian behavior and adequate physicochemical properties for 47 ocular instillation. The release study of pranoprofen from the semi-solid formulations exhibited a sus- 48 tained release behavior. The results obtained from ex vivo corneal permeation and in vivo anti-inflamma- 49 tory efficacy studies suggest that the ocular application of the hydrogels containing azone was more 50 effective over the azone-free formulations in the treatment of edema on the ocular surface. No signs of 51 ocular irritancy have been detected for the produced hydrogels. 2015-07-29T08:44:46Z 2016-02-11T23:01:52Z 2015-02-11 2015-07-29T08:44:46Z info:eu-repo/semantics/article info:eu-repo/semantics/acceptedVersion 0939-6411 https://hdl.handle.net/2445/66632 647946 25681744 eng Versió postprint del document publicat a: http://dx.doi.org/10.1016/j.ejpb.2015.01.026 European Journal of Pharmaceutics and Biopharmaceutics, 2015 http://dx.doi.org/10.1016/j.ejpb.2015.01.026 cc-by-nc-nd (c) Elsevier B.V., 2015 http://creativecommons.org/licenses/by-nc-nd/3.0/es info:eu-repo/semantics/openAccess application/pdf Elsevier B.V. Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica)