Poly(Lactide-co-Glycolide) Nanocapsules Containing Benzocaine: Influence of the Composition of the Oily Nucleus on Physico-Chemical Properties and Anesthetic Activity

Author(s)

Silva de Melo, Nathalie Ferreira ^{[1, 2]} ; Grillo, Renato ^{[1, 2]} ; Guilherme, Viviane Aparecida ^[2] ; de Araujo, Daniele Ribeiro ^{[2, 3]} ; de Paula, Eneida ^[2] ; Rosa, Andre Henrique ^[1] ; Fraceto, Leonardo Fernandes ^{[1, 2]}

Affiliation

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

^[2] State Univ Campinas UNICAMP, Dept Biochem, BR-13083970 Campinas, SP - Brazil

^[3] Fed Univ ABC UFABC, Human & Nat Sci Ctr, BR-09210170 Santo Andre, SP - Brazil

• Document type: Journal article
• Source: PHARMACEUTICAL RESEARCH; v. 28, n. 8, p. 1984-1994, AUG 2011.
• Web of Science Citations: 29

Abstract

The aim of this work was to investigate the influence of the oily nucleus composition on physico-chemical properties and anesthetic activity of poly (lactide-co-glycolide) nanocapsules with benzocaine. Nanocapsules containing benzocaine were prepared with three different oily nucleus composition and characterized by mean diameter, polydispersivity, zeta potential, pH and stability were investigated as a function of time. In vitro release kinetics were performed in a system with two compartments separated by a cellulose membrane. Intensity and duration of analgesia were evaluated in rats by sciatic nerve blockade. The greatest stability, slower release profile and improvement in the local anesthetic activity of BZC were obtained with the formulation using USP mineral oil as component. Results from our study provide useful perspectives on selection of the primary materials needed to produce suspensions of polymeric nanocapsules able to act as carriers of BZC, with potential future application in the treatment of pain. (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