Improved nonclinical pharmacokinetics and biodistribution of a new PPAR pan-agonist and COX inhibitor in nanocapsule formulation.

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MetadadosDescriçãoIdioma
Autor(es): dc.creatorGarcia, Giani Martins-
Autor(es): dc.creatorOliveira, Liliam Teixeira-
Autor(es): dc.creatorPitta, Ivan da Rocha-
Autor(es): dc.creatorLima, Maria do Carmo Alves de-
Autor(es): dc.creatorVilela, José Mário Carneiro-
Autor(es): dc.creatorAndrade, Margareth Spangler-
Autor(es): dc.creatorAbdalla, Dulcinéia Saes Parra-
Autor(es): dc.creatorMosqueira, Carla Furtado-
Data de aceite: dc.date.accessioned2019-11-06T13:36:02Z-
Data de disponibilização: dc.date.available2019-11-06T13:36:02Z-
Data de envio: dc.date.issued2016-01-05-
Data de envio: dc.date.issued2016-01-05-
Data de envio: dc.date.issued2015-
Fonte completa do material: dc.identifierhttp://www.repositorio.ufop.br/handle/123456789/5988-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/capes/559091-
Descrição: dc.descriptionWereport the in vitro release profile and comparative pharmacokinetics and biodistribution of a newperoxisome proliferator-activated receptor-γ agonist and cyclooxygenase inhibitor (Lyso-7) free or associated to poly(D,Llactic acid) nanocapsules (NC) after intravenous administration in mice. Lyso-7 pertains to the class of insulinsensitizing agents that shows potential beneficial effects in diabetes therapy. Monodispersed Lyso-7 NC with a mean diameter of 273 nm with high encapsulation efficiency (83%) were obtained. Lyso-7 dissolution rate was reduced (2.6-fold) upon loading in NC. The pharmacokinetic parameters were determined using a noncompartmental approach. In comparison with Lyso-7 in solution, the plasma-AUC increased 14-fold, the mean residence time 2.6-fold and the mean half-life (t1/2) 1.5-fold for Lyso-7-NC; the Lyso-7 plasma clearance, distribution volume and elimination rate were reduced 13, 10 and 1.4 fold, respectively, which indicates higher retention of encapsulated Lyso-7 in the blood compartment. Upon association with NC, organ exposure to Lyso-7 was higher in the heart (3.6-fold), lung (2.8-fold), spleen (2.3-fold), kidney (2-fold) and liver (1.8-fold) compared to Lyso-7 in solution. The analysis of whole data clearly indicates that body exposure to Lyso-7 was enhanced and the general toxicity reduced upon nanoencapsulation, allowing further evaluation of Lyso-7 in nonclinical and clinical studies-
Idioma: dc.languageen-
Direitos: dc.rightsO Periódico Journal of Controlled Release concede permissão para depósito deste artigo no Repositório Institucional da UFOP. Número da licença: 3732420794007-
Palavras-chave: dc.subjectThiazolidinedione-
Palavras-chave: dc.subjectPharmacokinetics-
Título: dc.titleImproved nonclinical pharmacokinetics and biodistribution of a new PPAR pan-agonist and COX inhibitor in nanocapsule formulation.-
Aparece nas coleções:Repositório Institucional - UFOP

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