Poloxamer-based binary hydrogels for delivering tramadol hydrochloride: sol-gel transition studies, dissolution-release kinetics, in vitro toxicity, and pharmacological evaluation

dc.contributorUniversidade Estadual Paulista (UNESP)
dc.creatorMendonca dos Santos, Ana Claudia
dc.creatorSantos Akkari, Alessandra Cristina
dc.creatorSilva Ferreira, Iasmin Rosanne
dc.creatorMaruyama, Cintia Rodrigues
dc.creatorPascoli, Monica
dc.creatorGuilherme, Viviane Aparecida
dc.creatorPaula, Eneida de
dc.creatorFraceto, Leonardo Fernandes
dc.creatorLima, Renata de
dc.creatorMelo, Patricia da Silva
dc.creatorAraujo, Daniele Ribeiro de
dc.date2015-10-21T21:19:54Z
dc.date2016-10-25T21:09:25Z
dc.date2015-10-21T21:19:54Z
dc.date2016-10-25T21:09:25Z
dc.date2015-01-01
dc.date.accessioned2017-04-06T09:10:44Z
dc.date.available2017-04-06T09:10:44Z
dc.identifierInternational Journal Of Nanomedicine, v. 10, p. 2391-2401, 2015.
dc.identifier1178-2013
dc.identifierhttp://hdl.handle.net/11449/129545
dc.identifierhttp://acervodigital.unesp.br/handle/11449/129545
dc.identifierhttp://dx.doi.org/10.2147/IJN.S72337
dc.identifierWOS:000351616800001
dc.identifier.urihttp://repositorioslatinoamericanos.uchile.cl/handle/2250/940100
dc.descriptionIn this work, poloxamer (PL)-based binary hydrogels, composed of PL 407 and PL 188, were studied with regard to the physicochemical aspects of sol-gel transition and pharmaceutical formulation issues such as dissolution-release profiles. In particular, we evaluated the cytotoxicity, genotoxicity, and in vivo pharmacological performance of PL 407 and PL 407-PL 188 hydrogels containing tramadol (TR) to analyze its potential treatment of acute pain. Drug-micelle interaction studies showed the formation of PL 407-PL 188 binary systems and the drug partitioning into the micelles. Characterization of the sol-gel transition phase showed an increase on enthalpy variation values that were induced by the presence of TR hydrochloride within the PL 407 or PL 407-PL 188 systems. Hydrogel dissolution occurred rapidly, with approximately 30%-45% of the gel dissolved, reaching similar to 80%-90% up to 24 hours. For in vitro release assays, formulations followed the diffusion Higuchi model and lower K-rel values were observed for PL 407 (20%, K-rel = 112.9 +/- 10.6 mu g . h(-1/2)) and its binary systems PL 407-PL 188 (25%-5% and 25%-10%, K-rel = 80.8 +/- 6.1 and 103.4 +/- 8.3 mu g.h(-1/2), respectively) in relation to TR solution (K-rel = 417.9 +/- 47.5 mu g.h(-1/2), P<0.001). In addition, the reduced cytotoxicity (V79 fibroblasts and hepatocytes) and genotoxicity (V79 fibroblasts), as well as the prolonged analgesic effects (>72 hours) pointed to PL-based hydrogels as a potential treatment, by subcutaneous injection, for acute pain.
dc.descriptionFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.descriptionConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.languageeng
dc.publisherDove Medical Press Ltd
dc.relationInternational Journal Of Nanomedicine
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.subjectmicelle
dc.subjectcytotoxicity
dc.subjectgenotoxicity
dc.subjectanalgesia
dc.titlePoloxamer-based binary hydrogels for delivering tramadol hydrochloride: sol-gel transition studies, dissolution-release kinetics, in vitro toxicity, and pharmacological evaluation
dc.typeOtro


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