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Type: Artigo
Title: Poloxamer-based binary hydrogels for delivering tramadol hydrochloride: sol-gel transition studies, dissolution-release kinetics, in vitro toxicity, and pharmacological evaluation
Author: Mendonca dos Santos, Ana Claudia
Santos Akkari, Alessandra Cristina
Silva Ferreira, Iasmin Rosanne
Maruyama, Cintia Rodrigues
Pascoli, Monica
Guilherme, Viviane Aparecida
de Paula, Eneida
Fraceto, Leonardo Fernandes
de Lima, Renata
Melo, Patricia da Silva
de Araujo, Daniele Ribeiro
Abstract: In 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
Subject: Copolímeros
Country: Reino Unido
Editor: Dove Medical
Rights: Fechado
Identifier DOI: 10.2147/IJN.S72337
Date Issue: 2015
Appears in Collections:IB - Artigos e Outros Documentos

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