Polymeric alginate nanoparticles containing the local anesthetic bupivacaine
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Data
2010-11-01
Autores
Grillo, Renato [UNESP]
de Melo, Nathalie F. S. [UNESP]
de Araujo, Daniele Ribeiro
de Paula, Eneida
Rosa, Andre Henrique [UNESP]
Fraceto, Leonardo Fernandes [UNESP]
Título da Revista
ISSN da Revista
Título de Volume
Editor
Informa Healthcare
Resumo
Bupivacaine (BVC; S75-R25, NovaBupi<SU (R)</SU) is an amide-type local anesthetic. Sodium alginate is a water-soluble linear polysaccharide. The present study reports the development of alginate/bis(2-ethylhexyl) sulfosuccinate (AOT) and alginate/chitosan nanoparticle formulations containing BVC (0.5%). The amounts of BVC associated in the alginate/AOT and alginate/chitosan nanoparticles were 87 +/- 1.5 and 76 +/- 0.9%, respectively. The average diameters and zeta potentials of the nanoparticles were measured for 30 days, and the results demonstrated the good stability of these particles in solution. The in vitro release kinetics showed a different behavior for the release profile of BVC in solution, compared with BVC-loaded alginate nanoparticles. In vitro and in vivo assays showed that alginate-chitosan BVC (BVC(ALG-CHIT)) and alginate-AOT BVC (BVC(ALG-AOT)) presented low cytotoxicity in 3T3-fibroblasts, enhanced the intensity, and prolonged the duration of motor and sensory blockades in a sciatic nerve blockade model.</.
Descrição
Palavras-chave
Bupivacaine, polymeric nanoparticles, alginate, in vivo, in vitro
Como citar
Journal of Drug Targeting. London: Informa Healthcare, v. 18, n. 9, p. 688-699, 2010.