Improved efficiency of ibuprofen by cationic carbosilane dendritic conjugates
Autores
Perise-Barrios, A.J.; Fuentes Paniagua, María Elena; Sánchez-Nieves Fernández, Javier; Serramía Lobera, Mª Jesús; Alonso, Ester; [et al.]Identificadores
Enlace permanente (URI): http://hdl.handle.net/10017/34041DOI: 10.1021/acs.molpharmaceut.6b00420
ISSN: 1543-8384
Editor
American Chemical Society
Fecha de publicación
2016-08-17Patrocinadores
Ministerio de Economía y Empresa
Cita bibliográfica
Molecular Pharmaceutics, 2016, v. 13 , n. 10 , p. 3427-3438
Palabras clave
Anti-inflammatory
Carbosilane dendrimers,
Dendrons
Ibuprofen
Drug release and macrophages.
Proyectos
info:eu-repo/grantAgreement/MINECO//CTQ-2014-54004-P/ES/DISEÑO DE SISTEMAS DENDRÍTICOS AVANZADOS PARA SU USO EN BIOMEDICINA, OBTENIDOS A TRAVÉS DE PROCESOS DE DENDRONIZACIÓN
Tipo de documento
info:eu-repo/semantics/article
Versión
info:eu-repo/semantics/acceptedVersion
Derechos
Attribution-NonCommercial-NoDerivatives 4.0 International (CC BY-NC-ND 4.0)
(c) American Chemical Society, 2016
Derechos de acceso
info:eu-repo/semantics/openAccess
Resumen
In order to improve the efficiency of the anti-inflammatory drug ibuprofen, cationic carbosilanedendrimers and dendrons with ibuprofen at their periphery or at their focal point, respectively, havebeen synthesized and the release of the drug was studied using HPLC. Macrophages were used toevaluate the anti-inflammatory effect of the ibuprofen-conjugated dendritic systems and comparedwith mixtures of non-ibuprofen dendritic systems in the presence of the drug. The cationic ibuprofenconjugateddendron was the compound that showed higher anti-inflammatory properties. It reduces the LPS-induced COX-2 expression, decreases the release of several inflammatory cytokines such as TNFalfa, IL-1beta, IL-6 and CCL3. These results open new perspectives in the use of these compounds asdrug carriers.
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