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Biomed Res Int ; 2021: 7300098, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34568494

RESUMEN

This study reports the development of thermosensitive hydrogels for delivering ropivacaine (RVC), a wide clinically used local anesthetic. For this purpose, poloxamer- (PL-) based hydrogels were synthesized for evaluating the influence of polymer concentration, hydrophilic-lipophilic balances, and binary system formation on biopharmaceutical properties and pharmacological performance. Transition temperatures were shifted, and rheological analysis revealed a viscoelastic behavior with enhanced elastic/viscous modulus relationship (G'/G " = 1.8 to 22 times), according to hydrogel composition and RVC incorporation. The RVC release from PL407 and PL407/338 systems followed the Higuchi model (R 2 = 0.923-0.989), indicating the drug diffusion from hydrogels to the medium. RVC-PL hydrogels were potentially biocompatible evoking low cytotoxic effects (in fibroblasts and Schwann cells) and mild/moderate inflammation signs on sciatic nerve nearby histological evaluation. In vivo pharmacological assays demonstrated that PL407 and PL407/338 evoked differential analgesic effects, by prolonging the sensory blockade duration up to ~340 and 250 min., respectively. All those results highlighted PL407 and PL407/338 as promising new strategies for sustaining analgesic effects during the postoperative period.


Asunto(s)
Anestesia Local , Materiales Biocompatibles/química , Hidrogeles/química , Poloxámero/química , Ropivacaína/farmacología , Células 3T3 , Analgesia , Animales , Área Bajo la Curva , Rastreo Diferencial de Calorimetría , Muerte Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Liberación de Fármacos , Elasticidad , Masculino , Ratones , Micelas , Ratas Wistar , Reología , Nervio Ciático/efectos de los fármacos , Sensación/efectos de los fármacos , Viscosidad
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