Liposomal lidocaine gel for topical use at the oral mucosa: characterization, in vitro assays and in vivo anesthetic efficacy in humans

Author(s):Show less -

Franz-Montan, Michelle ^[1] ; Baroni, Daniela ^[1] ; Brunetto, Giovana ^[2] ; Vieira Sobral, Viviane Roberta ^[2] ; Goncalves da Silva, Camila Morais ^[2] ; Venancio, Paulo ^[1] ; Zago, Patricia Wiziack ^[1] ; Saia Cereda, Cintia Maria ^[2] ; Volpato, Maria Cristina ^[1] ; de Araujo, Daniele Ribeiro ^[3] ; de Paula, Eneida ^[2] ; Groppo, Francisco Carlos ^[1]

Affiliation

^[1] Univ Campinas UNICAMP, Piracicaba Dent Sch, Dept Physiol Sci, Sao Paulo - Brazil

^[2] Univ Campinas UNICAMP, Inst Biol, Dept Biochem, Sao Paulo - Brazil

^[3] Fed Univ ABC, Human & Nat Sci Ctr, Sao Paulo - Brazil

• Document type: Journal article
• Source: Journal of Liposome Research; v. 25, n. 1, p. 11-19, MAR 2015.
• Web of Science Citations: 21

Abstract

Objective: To characterize liposomal-lidocaine formulations for topical use on oral mucosa and to compare their in vitro permeation and in vivo anesthetic efficacy with commercially available lidocaine formulations. Materials and methods: Large unilamellar liposomes (400 nm) containing lidocaine were prepared using phosphatidylcholine, cholesterol, and alpha-tocoferol (4:3:0.07, w:w:w) and were characterized in terms of membrane/water partition coefficient, encapsulation efficiency, size, polydispersity, zeta potential, and in vitro release. In vitro permeation across pig palatal mucosa and in vivo topical anesthetic efficacy on the palatal mucosa in healthy volunteers (doubleblinded cross-over, placebo controlled study) were performed. The following formulations were tested: liposome-encapsulated 5% lidocaine (Liposome-Lido5); liposome-encapsulated 2.5% lidocaine (Liposome-Lido2.5); 5% lidocaine ointment (Xylocaina (R)), and eutectic mixture of lidocaine and prilocaine 2.5% (EMLA (R)). Results: The Liposome-Lido5 and EMLA showed the best in vitro permeation parameters (flux and permeability coefficient) in comparison with Xylocaina and placebo groups, as well as the best in vivo topical anesthetic efficacy. Conclusion: We successfully developed and characterized a liposome encapsulated 5% lidocaine gel. It could be considered an option to other topical anesthetic agents for oral mucosa. (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 type: Research Projects - Thematic Grants
• FAPESP's process: 07/05734-1 - Efficacy of a liposomal articaine hydrocloride formulation in rats.
• Grantee: Luciana Aranha Berto
• Support type: Scholarships in Brazil - Master
• FAPESP's process: 09/08860-3 - Transdermal permeation and biocompatibility studies on gel formulations of benzocaine encapsulated in elastic and conventional liposomes
• Grantee: Michelle Franz Montan Braga Leite
• Support type: Scholarships in Brazil - Post-Doctorate