Pharmacokinetic study of liposome-encapsulated and plain mepivacaine formulations injected intra-orally in volunteers

Author(s)

Tofoli, Giovana Radomille ^[1] ; Cereda, Cintia M. S. ^[2] ; Araujo, Daniele Ribeiro ^[3] ; Franz-Montan, Michelle ^[2] ; Groppo, Francisco Carlos ^[4] ; Quaglio, Daiane ^[5] ; Pedrazzoli Junior, Jose ^[1] ; Calafatti, Silvana Aparecida ^[1] ; Proenca Barros, Fabio Alessandro ^[5] ; de Paula, Eneida ^[2]

Affiliation

^[1] Univ Sao Francisco, BR-12916900 Braganca Paulista, SP - Brazil

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

^[3] Fed Univ ABC, Santo Andre, SP - Brazil

^[4] Univ Estadual Campinas, Piracicaba Dent Sch, Dept Physiol Sci, Sao Paulo - Brazil

^[5] CORE, Lab Clin Anal, Braganca Paulista, SP - Brazil

• Document type: Journal article
• Source: Journal of Pharmacy and Pharmacology; v. 64, n. 3, p. 397-403, MAR 2012.
• Web of Science Citations: 7

Abstract

Objectives The pharmacokinetics of commercial and liposome-encapsulated mepivacaine (MVC) injected intra-orally in healthy volunteers was studied. Methods In this double blind, randomized cross-over study, 15 volunteers received, at four different sessions, 1.8 ml of the following formulations: 2% MVC with 1 : 100 000 epinephrine (MVC2%EPI), 3% MVC (MVC3%), 2% and 3% liposomeen-capsulated MVC (MVC2%LUV and MVC3%LUV). Blood samples were collected pre dose (0 min) and at 15, 30, 45, 60, 90, 120, 180, 240, 300, 360 min after injections. Liquid chromatography-tandem mass spectrometry was used to quantify plasma MVC concentrations. Results Pharmacokinetic analysis showed that the maximum plasma concentration (Cmax) and the areas under the curves (AUC(0-360) and AUC(0-infinity)) after MVC2%LUV and MVC2%EPI injections were smaller (P < 0.05) than the equivalent figures for MVC3% and MVC3%LUV. The time to maximum plasma concentration (Tmax) and the half-life of elimination (t1/2beta) obtained after the treatment with MVC2%LUV, MVC2%EPI, MVC3% and MVC3%LUV presented no statistically significant differences (P > 0.05). Cmax, AUC(0-360) and AUC(0-infinity) after injection of the 2% formulations (MVC2%LUV and MVC2%EPI) did not exhibit statistically significant differences (P > 0.05). The pharmacokinetics of MVC2%LUV were comparable to the pharmacokinetics of MVC2%EPI. Conclusion The liposomal formulation of 2% MVC exhibits similar systemic absorption to the local anesthetic with vasoconstrictor. (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