Poloxamer-based Binary Hydrogels For Delivering Tramadol Hydrochloride: Sol-gel Transition Studies, Dissolution-release Kinetics, In Vitro Toxicity, And Pharmacological Evaluation.

dc.creatordos Santos, Ana Claudia Mendonça
dc.creatorAkkari, Alessandra Cristina Santos
dc.creatorFerreira, Iasmin Rosanne Silva
dc.creatorMaruyama, Cintia Rodrigues
dc.creatorPascoli, Monica
dc.creatorGuilherme, Viviane Aparecida
dc.creatorde Paula, Eneida
dc.creatorFraceto, Leonardo Fernandes
dc.creatorde Lima, Renata
dc.creatorMelo, Patrícia da Silva
dc.creatorde Araujo, Daniele Ribeiro
dc.date2015
dc.date2016-05-23T19:43:19Z
dc.date2016-05-23T19:43:19Z
dc.date.accessioned2018-03-29T01:30:30Z
dc.date.available2018-03-29T01:30:30Z
dc.identifierInternational Journal Of Nanomedicine. v. 10, p. 2391-2401, 2015.
dc.identifier1178-2013
dc.identifier10.2147/IJN.S72337
dc.identifierhttp://www.ncbi.nlm.nih.gov/pubmed/25848258
dc.identifierhttp://repositorio.unicamp.br/jspui/handle/REPOSIP/235946
dc.identifier25848258
dc.identifier.urihttp://repositorioslatinoamericanos.uchile.cl/handle/2250/1304189
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 ~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 μg · 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 μg · h(-1/2), respectively) in relation to TR solution (K(rel) =417.9 ± 47.5 μg · 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.description10
dc.description2391-2401
dc.languageeng
dc.relationInternational Journal Of Nanomedicine
dc.relationInt J Nanomedicine
dc.rightsaberto
dc.sourcePubMed
dc.subjectAnalgesia
dc.subjectCytotoxicity
dc.subjectGenotoxicity
dc.subjectMicelle
dc.titlePoloxamer-based Binary Hydrogels For Delivering Tramadol Hydrochloride: Sol-gel Transition Studies, Dissolution-release Kinetics, In Vitro Toxicity, And Pharmacological Evaluation.
dc.typeArtículos de revistas


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