Synergy between surfactants and mucoadhesive polymers enhances the transbuccal permeation of local anesthetics from freeze-dried tablets

Autor(es)

Silva Favacho, Hugo Alexandre ^[1] ; do Couto, Rene Oliveira ^[2] ; Ferreira Duarte, Maira Peres ^[3] ; Garofo Peixoto, Maria Paula ^[3] ; Vianna Lopez, Renata Fonseca ^[3] ; Pedrazzi, Vinicius ^[4] ; de Gaitani, Cristiane Masetto ^[3] ; de Freitas, Osvaldo ^[3]

Afiliação do(s) autor(es)

^[1] Univ Fed Amapa, BR-68903419 Macapa, AP - Brazil

^[2] Univ Fed Sao Joao del Rei, Campus Ctr Oeste Dona Lindu, BR-35501296 Divinopolis, MG - Brazil

^[3] Univ Sao Paulo, Sch Pharmaceut Sci Ribeirao Preto, Ribeirao Preto, SP - Brazil

^[4] Univ Sao Paulo, Sch Odontol Ribeirao Preto, Ribeirao Preto, SP - Brazil

• Tipo de documento: Artigo Científico
• Fonte: Materials Science & Engineering C-Materials for Biological Applications; v. 108, MAR 2020.
• Citações Web of Science: 0

Resumo

We report on the advance of freeze-dried mucoadhesive orodispersible tablets (ODTs) loaded with prilocaine (PRC) and lidocaine (LDC) hydrochlorides, aiming to promote noninvasive buccal anesthesia. The influences of combining biocompatible polymers (pullulan and HPMC K100 LV) and a blend of surfactants (oleic acid, polysorbate 80 and propylene glycol) acting as chemical enhancers on the permeation of such drugs through the esophageal porcine epithelium and in vitro mucoadhesion were investigated. The ODTs were also characterized in terms of average weight, thickness, pH, drug content, in vitro release, thermal behavior and scanning electronic microscopy. A dissolution test showed fast drug release within one hour. The drug release data for all ODTs fitted first order. No significant influence of the type of mucoadhesive polymer on release was observed, while the drug release from ODTs decreased in the presence of chemical enhancers. For the ODT containing pullulan the drug release mechanism was anomalous transport, whist for all others it was case-II transport. A remarkable synergic effect between pullulan and chemical enhancers on the permeation flux, lag time, and permeability coefficient of both drugs, but mainly for PRC was observed. Pullulan together with permeation enhancers also substantially improved the work of mucoadhesion as compared to HPMC. In contrast, HPMC improved drug retention in the epithelium. The novel drug delivery platform achieved by combining a freezedrying technique, mucoadhesive biocompatible polymers, and chemical permeation enhancers displayed an effective strategy for the transbuccal delivery of PRC and LDC that can be used to improve needle-free buccal anesthesia. (AU)

• Processo FAPESP: 12/05644-0 - Desenvolvimento de sistemas semi-sólidos mucoadesivos para liberação de anestésico e aplicação de iontoforese na cavidade bucal
• Beneficiário: Camila Cubayachi
• Modalidade de apoio: Bolsas no Brasil - Mestrado
• Processo FAPESP: 12/06167-1 - Desenvolvimento de filmes mucoadesivos para liberação de fármacos anestésicos na cavidade bucal
• Beneficiário: Renê Oliveira Do Couto
• Modalidade de apoio: Bolsas no Brasil - Doutorado
• Processo FAPESP: 12/07251-6 - Desenvolvimento de plataforma com sistemas mucoadesivos para liberação de fármacos na cavidade bucal
• Beneficiário: Osvaldo de Freitas
• Modalidade de apoio: Auxílio à Pesquisa - Regular
• Processo FAPESP: 13/12174-3 - Estudo de polímeros reabsorvíveis: efeito da degradação e erosão na liberação de corantes
• Beneficiário: Renê Oliveira Do Couto
• Modalidade de apoio: Bolsas no Exterior - Estágio de Pesquisa - Doutorado
• Processo FAPESP: 14/22451-7 - Sistemas de liberação sustentada e direcionada de fármacos para o tecido epitelial
• Beneficiário: Renata Fonseca Vianna Lopez
• Modalidade de apoio: Auxílio à Pesquisa - Temático