Antinociceptive effects of bupivacaine and its sulfobutylether-β-cyclodextrin inclusion complex in orofacial pain

Autor: Juliana Souza de Freitas Domingues, Silmara Martins Dias dos Santos, Julia das Neves Rodrigues Ferreira, Bianca Miguel Monti, Darciane Favero Baggio, Wagner Hummig, Erika Ivanna Araya, Eneida de Paula, Juliana Geremias Chichorro, Luiz Eduardo Nunes Ferreira
Rok vydání: 2022
Předmět:
Zdroj: Naunyn-Schmiedeberg's Archives of Pharmacology. 395:1405-1417
ISSN: 1432-1912
0028-1298
Popis: Bupivacaine hydrochloride (BVC) represents an option to produce long-lasting analgesia, and complexation in cyclodextrins has shown improvements in biopharmaceutical properties. This study aimed to characterize and test the cytotoxicity and antinociceptive effects of BVC complexed in sulfobutylether-β-cyclodextrin (SBEβCD). The kinetics and stoichiometry of complexation and BVC-SBEβCD association constant were evaluated by phase solubility study and Job's plot. Evidence of the BVC-SBEβCD complex formation was obtained from scanning electron microscopy (SEM), infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC). The cytotoxicity was evaluated in keratinocyte (HaCaT) and neuroblastoma (SH-SY5Y). Antinociceptive effects were registered via orofacial pain models: the formalin test, carrageenan-induced hyperalgesia, and postoperative pain (intraoral incision). The complex formation occurred at a 1:1 BVC-SBEβCD molar ratio, with a low association constant (13.2 M
Databáze: OpenAIRE
Externí odkaz: