Stability and Local Toxicity Evaluation of a Liposomal Prilocaine Formulation

Autor(es)

Saia Cereda, Cintia M. ^[1] ; Tofoli, Giovana R. ^{[1, 2]} ; De Brito Junior, Rui B. ^[3] ; De Jesus, Marcelo B. ^[1] ; Fraceto, Leonardo F. ^{[1, 4]} ; Groppo, Francisco C. ^[2] ; De Araujo, Daniele R. ^[1] ; De Paula, Eneida ^[1]

Afiliação do(s) autor(es)

^[1] Univ Estadual Campinas, Inst Biol, Dept Biochem, Campinas, SP - Brazil

^[2] Univ Estadual Campinas, Piracicaba Dent Sch, Dept Physiol Sci, Piracicaba, SP - Brazil

^[3] Sao Leopoldo Mand Dent Res Inst, Dept Biol Mol, Campinas, SP - Brazil

^[4] State Univ Sao Paulo, Dept Environm Engn, Sorocaba, SP - Brazil

• Tipo de documento: Artigo Científico
• Fonte: Journal of Liposome Research; v. 18, n. 4, p. 329-339, 2008.
• Citações Web of Science: 18

Resumo

This study reports a physicochemical stability evaluation of a previously reported liposomal prilocaine (PLC(LUV)) formulation (Cereda el al. J. Pharm. Pharmaceut. Sci. 7:235, 2004) before and after steam sterilization as well as its local toxicity evaluation. Prilocaine (PLC) was encapsulated into extruded unilamellar liposomes (LUVs) composed by egg phosphatidylcholine:cholesterol:alfa-tocopherol (4:3:0.07, mole %). Laser light-scattering analysis (p > 0.05) and thiobarbituric acid reaction (p > 0.05) were used to evaluate the liposomes physical (size) and chemical (oxidation) stability, respectively. The prilocaine chemical stability was followed by (1)H-nuclear magnetic resonance. These tests detected no differences on the physicochemical stability of PLC or PLCLUV, sterilized or not, up to 30 days after preparation (p > 0.05). Finally, the paw edema test and histological analysis of rat oral mucosa were used to assess the possible inflammatory effects of PLC(LUV). PLC(LUV) did not evoke rat paw edema (p > 0.05), and no significant differences were found in histological analysis, when compared to the control groups (p > 0.05). The present work shows that PLC(LUV) is stable for a 30-day period and did not induce significant inflammatory effects both in the paw edema test and in histological analysis, giving supporting evidence for its safely and possible clinical use in dentistry. (AU)

• Processo FAPESP: 06/00121-9 - Novas formulações de anestésicos locais de liberação controlada: do desenvolvimento ao teste clínico odontológico
• Beneficiário: Eneida de Paula
• Modalidade de apoio: Auxílio à Pesquisa - Temático