Preparation and characterization of poly(e-caprolactone) nanospheres containing the local anesthetic lidocaine

Author(s)

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

Affiliation

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

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

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

• Document type: Journal article
• Source: Journal of Pharmaceutical Sciences; v. 102, n. 1, p. 215-226, JAN 2013.
• Web of Science Citations: 24

Abstract

The objective of this work was to develop a modified release system for the local anesthetic lidocaine (LDC), using poly(e-caprolactone) (PCL) nanospheres (NSs), to improve the pharmacological properties of the drug when administered by the infiltration route. In vitro experiments were used to characterize the system and investigate the release mechanism. The NSs presented a polydispersion index of 0.072, an average diameter of 449.6?nm, a zeta potential of -20.1?mV, and an association efficiency of 93.3%. The release profiles showed that the release of associated LDC was slower than that of the free drug. Atomic force microscopy analyses showed that the spherical structure of the particles was preserved as a function of time, as well as after the release experiments. Cytotoxicity and pharmacological tests confirmed that association with the NSs reduced the toxicity of LDC, and prolonged its anesthetic action. This new formulation could potentially be used in applications requiring gradual anesthetic release, especially dental procedures. (c) 2012 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 102:215226, 2013 (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