Otro
Polymeric alginate nanoparticles containing the local anesthetic bupivacaine
Registro en:
Journal of Drug Targeting. London: Informa Healthcare, v. 18, n. 9, p. 688-699, 2010.
1061-186X
10.3109/10611861003649738
WOS:000282516600005
0000-0002-2042-018X
Autor
Grillo, Renato
de Melo, Nathalie F. S.
de Araujo, Daniele Ribeiro
de Paula, Eneida
Rosa, Andre Henrique
Fraceto, Leonardo Fernandes
Resumen
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.</. Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)