Polymeric alginate nanoparticles containing the local anesthetic bupivacaine

Author(s)

Grillo, Renato ^[1] ; de Melo, Nathalie F. S. ^{[2, 1]} ; de Araujo, Daniele Ribeiro ^[3] ; de Paula, Eneida ^[2] ; Rosa, Andre Henrique ^[1] ; Fraceto, Leonardo Fernandes ^[1]

Affiliation

^[1] Unesp Sao Paulo State Univ, Dept Environm Engn, BR-18087180 Sorocaba, SP - Brazil

^[2] Univ Estadual Campinas, Inst Biol, Dept Biochem, Campinas, SP - Brazil

^[3] Fed Univ ABC, Human & Nat Sci Ctr, Santo Andre, SP - Brazil

• Document type: Journal article
• Source: Journal of Drug Targeting; v. 18, n. 9, p. 688-699, NOV 2010.
• Web of Science Citations: 44

Abstract

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.</. (AU)

• FAPESP's process: 06/00121-9 - New formulations for the controlled release of local anesthetics in dentistry: from development to clinical tests
• Grantee: Eneida de Paula
• Support Opportunities: Research Projects - Thematic Grants
• FAPESP's process: 08/01222-9 - Preparation and characterization of alginate nanoparticle with bupivacaine
• Grantee: Renato Grillo
• Support Opportunities: Scholarships in Brazil - Scientific Initiation