Pharmacokinetic and local toxicity studies of liposome-encapsulated and plain mepivacaine solutions in rats

Author(s):Show less -

Tofoli, Giovana Radomille ^{[1, 2]} ; Saia Cereda, Cintia Maria ^[1] ; de Araujo, Daniele Ribeiro ^{[3, 1]} ; de Paula, Eneida ^[1] ; Brito Junior, Rui Barbosa ^[4] ; Pedrazzoli Junior, Jose ^[2] ; Meurer, Eduardo ^[2] ; Proenca Barros, Fabio Alessandro ; Groppo, Francisco Carlos ^[5] ; Volpato, Maria Cristina ^[5] ; Ranali, Jose ^[5]

Affiliation

^[1] Univ Estadual Campinas, Dept Biochem, Inst Biol, BR-13083970 Campinas, SP - Brazil

^[2] Univ Sao Francisco, UNIFAG Clin Pharmacol & Gastroenterol Unit, BR-12900000 Braganca Paulista, SP - Brazil

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

^[4] Sao Leopoldo Mand Dent Res Inst, Dept Mol Biol, Campinas, SP - Brazil

^[5] Univ Estadual Campinas, Piracicaba Dent Sch, Dept Physiol Sci, Piracicaba, SP - Brazil

• Document type: Journal article
• Source: DRUG DELIVERY; v. 17, n. 2, p. 68-76, FEB 2010.
• Web of Science Citations: 6

Abstract

The pharmacokinetics and the local toxicity of commercial and liposome-encapsulated mepivacaine formulations injected intra-orally in rats were studied. Animals were divided in groups (n=4-6) and treated with 0.1 mL of the formulations: 2% mepivacaine with 1:100,000 epinephrine (MVC(2%EPI)), 3% mepivacaine (MVC(3%)), and 2% liposome-encapsulated mepivacaine (MVC(LUV)). The results showed that the 2% liposome-encapsulated mepivacaine reduced C(max), prolonged AUC(0-infinity) and t(1/2) compared with 3% plain and 2% vasoconstritor-associated mepivacaine, after intraoral injection. In addition, it was also observed that liposomal mepivacaine might protect the tissue against local inflammation evoked by plain or vasoconstrictors-associated mepivacaine, giving supporting evidence for its safety and possible clinical use in dentistry. (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