Polymeric alginate nanoparticles containing the local anesthetic bupivacaine.
Bupivacaine (BVC; S75–R25, NovaBupi® 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.
Grillo
Renato
R
Department of Environmental Engineering, Unesp—São Paulo State University, Av. Três de Março, 511, 18087-180 Sorocaba, SP, Brazil.
de Melo
Nathalie F S
NF
de Araújo
Daniele Ribeiro
DR
de Paula
Eneida
E
Rosa
André Henrique
AH
Fraceto
Leonardo Fernandes
LF
D000464:Alginates; D000779:Anesthetics, Local / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D002045:Bupivacaine / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D048271:Chitosan; D004355:Drug Stability; D020723:Glucuronic Acid; D006603:Hexuronic Acids; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D053758:Nanoparticles; D010316:Particle Size; D013386:Succinates
D000464:Alginates; D000779:Anesthetics, Local; D006603:Hexuronic Acids; D013386:Succinates; C511925:bis(2-ethylhexyl)sulfosuccinate; D020723:Glucuronic Acid; D048271:Chitosan; D002045:Bupivacaine