Producción científica2020· Acta Scientific Dental Sciences
Hyaluronic Acid: Intraoral Application
AutoresAlbert-López MJ, Pallarés-Serrano AI, Bardají JA
Por qué importa
El presente estudio investiga el uso de polímeros tiolados (thiomers) quimicamente preactivados para la administración de fármacos a través de las mucosas. Específicamente, se sintetizaron conjugados de ácido hialurónico con cisteína y mercaptonicotinamida (HA-CYS-MNA) y se evaluaron sus propiedades de hinchamiento, cohesión y, crucialmente, su capacidad de adhesión a la mucosa oral. Los resultados indican una mejora significativa en la adhesión a la mucosa en comparación con polímeros tiolados no modificados, además de una mayor estabilidad y ausencia de toxicidad celular. Estos hallazgos sugieren que estos conjugados de ácido hialurónico preactivado representan una nueva generación de polímeros bioadhesivos, seguros para aplicaciones intraorales que requieren una prolongada permanencia en el sitio de acción.
This study was aimed to investigate chemical preactivated thiomers for their potential use in mucosal drug delivery. Thiomers--thiolated polymers--are mucoadhesive polymers with sulfhydryl group-bearing side chains. Thiomers are synthesized by covalent attachment of low molecular mass compounds bearing sulfhydryl group to the polymeric backbone of well-established polymers. Hyaluronic acid-cysteine ethyl ester-mercaptonicotinamide conjugates (HA-CYS-MNA) were synthesized by the oxidative S-S coupling of HA-CYS with 6-MNA. Conjugates were compressed into test discs to investigate cohesive properties, cytotoxicity assays, and mucoadhesion studies. Because of the immobilization of MNA, the HA-CYS-MNA conjugates exhibit comparatively higher swelling properties and cohesive properties corresponding unmodified HA. On the rotating cylinder, discs based on HA-CYS-MNA conjugates displayed fourfold improved mucoadhesion time compared with thiolated polymers. Tensile study results were found in good agreement with rotating cylinder results. Moreover, preactivated thiomers showed higher stability. All polymers were found nontoxic over Caco-2 cells. On the basis of achieved results, the preactivated thiomeric therapeutic agent seems to represent a promising generation of mucoadhesive polymers that are safe to use for a prolonged residence time to target the mucosa requested for intraoral application.
