Pharmacokinetic and local toxicity studies of liposome-encapsulated and plain mepivacaine solutions in rats.
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.
Tofoli
Giovana Radomille
GR
Department of Biochemistry, Institute of Biology, State University of Campinas, Campinas, SP, Brazil.
Cereda
Cíntia Maria Saia
CM
de Araujo
Daniele Ribeiro
DR
de Paula
Eneida
E
Brito
Rui Barbosa
RB
Pedrazzoli
José
J
Meurer
Eduardo
E
Barros
Fábio Alessandro Proença
FA
Groppo
Francisco Carlos
FC
Volpato
Maria Cristina
MC
Ranali
José
J
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
D000779:Anesthetics, Local; D004304:Dosage Forms; D008051:Lipid Bilayers; D008081:Liposomes; D012996:Solutions; D008619:Mepivacaine; D004837:Epinephrine