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

Nenhuma Miniatura disponível

Data

2015-01-01

Orientador

Coorientador

Pós-graduação

Curso de graduação

Título da Revista

ISSN da Revista

Título de Volume

Editor

Dove Medical Press Ltd

Tipo

Artigo

Direito de acesso

Acesso restrito

Resumo

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.

Descrição

Idioma

Inglês

Como citar

International Journal Of Nanomedicine, v. 10, p. 2391-2401, 2015.

Itens relacionados