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Assessing α-Bisabolol as a Transmucosal Permeation Enhancer of Buccal Local Anesthetics

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Autor(es):
do Couto, Rene Oliveira ; Thomaz, Douglas Vieira ; Duarte, Maira Perez Ferreira ; Lopez, Renata Fonseca Vianna ; Pedrazzi, Vinicius ; de Freitas, Osvaldo ; Tartaglia, Gianluca Martino
Número total de Autores: 7
Tipo de documento: Artigo Científico
Fonte: PHARMACEUTICS; v. 16, n. 9, p. 13-pg., 2024-09-01.
Resumo

Needle-free buccal anesthesia improves dental treatment outcomes for both patients and dentists. In this study, we report on an assessment of the enhancement effects of alpha-bisabolol on the in vitro transmucosal permeation of prilocaine hydrochloride (PCl) and lidocaine hydrochloride (LCl) from needleless buccal films. We also evaluated the mechanical properties of the film, which consisted of Methocel (TM) K100 LV as the film-forming polymer (3% m<middle dot>m-1), PEG 400 as a cosolvent (15% m<middle dot>m-1 based on drug loading), alpha-bisabolol (15 and 30% m<middle dot>m-1 based on drug loading), and the drugs combined at a 1:1 ratio (15 mg<middle dot>unit-1). The porcine esophageal epithelium was used as a membrane barrier, and artificial saliva was the release medium. After a 1 h experiment at 25 +/- 2 degrees C, alpha-bisabolol significantly decreased, rather than enhanced, the permeation fluxes (five-fold), permeability coefficients (seven-fold), and retentions (two-fold) of both PCl and LCl through the epithelium, regardless of the concentration. Moreover, the resistance and flexibility of the films markedly decreased compared to those without alpha-bisabolol. Therefore, under the experimental conditions, using alpha-bisabolol as a buccal permeation enhancer for the hydrophilic local anesthetics PCl and LCl from buccal films is not feasible. (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 Tambellini Cubayachi
Modalidade de apoio: Bolsas no Brasil - Mestrado
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
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