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

Autor(es):Mostrar menos -

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]

Afiliação do(s) autor(es)

^[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

• Tipo de documento: Artigo Científico
• Fonte: Journal of Liposome Research; v. 25, n. 1, p. 11-19, MAR 2015.
• Citações Web of Science: 21

Resumo

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)

• Processo FAPESP: 06/00121-9 - Novas formulações de anestésicos locais de liberação controlada: do desenvolvimento ao teste clínico odontológico
• Beneficiário: Eneida de Paula
• Modalidade de apoio: Auxílio à Pesquisa - Temático
• Processo FAPESP: 09/08860-3 - Estudos de permeação cutânea e biocompatibilidade de formulações em gel de benzocaína encapsulada em lipossomas elásticos e convencionais
• Beneficiário: Michelle Franz Montan Braga Leite
• Modalidade de apoio: Bolsas no Brasil - Pós-Doutorado
• Processo FAPESP: 07/05734-1 - Estudo da eficácia da preparação anestésica local lipossomal de articaína em ratos.
• Beneficiário: Luciana Aranha Berto
• Modalidade de apoio: Bolsas no Brasil - Mestrado