title: Pharmacokinetic and local toxicity studies of liposome-encapsulated and plain mepivacaine solutions in rats.
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.
authors.affiliation: Department of Biochemistry, Institute of Biology, State University of Campinas, Campinas, SP, Brazil.
authors.forename: Giovana Radomille
authors.initials: GR
authors.lastname: Tofoli
authors.forename: Cíntia Maria Saia
authors.initials: CM
authors.lastname: Cereda
authors.forename: Daniele Ribeiro
authors.initials: DR
authors.lastname: de Araujo
authors.forename: Eneida
authors.initials: E
authors.lastname: de Paula
authors.forename: Rui Barbosa
authors.initials: RB
authors.lastname: Brito
authors.forename: José
authors.initials: J
authors.lastname: Pedrazzoli
authors.forename: Eduardo
authors.initials: E
authors.lastname: Meurer
authors.forename: Fábio Alessandro Proença
authors.initials: FA
authors.lastname: Barros
authors.forename: Francisco Carlos
authors.initials: FC
authors.lastname: Groppo
authors.forename: Maria Cristina
authors.initials: MC
authors.lastname: Volpato
authors.forename: José
authors.initials: J
authors.lastname: Ranali
mesh_terms: D000779:Anesthetics, Local / Q000008:administration & dosage / Q000493:pharmacokinetics*; D000818:Animals; D002626:Chemistry, Pharmaceutical; D019411:Clinical Laboratory Techniques; D004304:Dosage Forms; D016503:Drug Delivery Systems; D004837:Epinephrine / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008051:Lipid Bilayers; D008081:Liposomes / Q000008:administration & dosage*; D008297:Male; D008619:Mepivacaine / Q000493:pharmacokinetics*; D009407:Nerve Block / Q000379:methods; D051381:Rats; D017208:Rats, Wistar; D012106:Research; D012996:Solutions
chemical_list: D000779:Anesthetics, Local; D004304:Dosage Forms; D008051:Lipid Bilayers; D008081:Liposomes; D012996:Solutions; D008619:Mepivacaine; D004837:Epinephrine