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

Autor(es)

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]}

Afiliação do(s) autor(es)

^[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

• Tipo de documento: Artigo Científico
• Fonte: Journal of Pharmaceutical Sciences; v. 102, n. 1, p. 215-226, JAN 2013.
• Citações Web of Science: 24

Resumo

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)

• Processo FAPESP: 06/00121-9 - Novas formulações de anestésicos locais de liberação controlada: do desenvolvimento ao teste clínico odontológico
• Beneficiário: Eneida de Paula
• Linha de fomento: Auxílio à Pesquisa - Temático
• Processo FAPESP: 07/00127-0 - Preparo e caracterização de nanoesferas de poli-láctico-co-glicólico contendo bupivacaína como sistema de liberação para anestesia local
• Beneficiário: Leonardo Fernandes Fraceto
• Linha de fomento: Auxílio à Pesquisa - Regular
• Processo FAPESP: 10/11097-7 - Preparo e caracterização de micropartículas poliméricas contendo lidocaína, desenvolvidas para o tratamento da dor
• Beneficiário: Estefânia Vangelie Ramos Campos
• Linha de fomento: Bolsas no Brasil - Iniciação Científica