Improved efficiency of ibuprofen by cationic carbosilane dendritic conjugates

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 t...

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Bibliographic Details
Authors: Perise-Barrios, A.J., Fuentes Paniagua, María Elena, Sánchez-Nieves Fernández, Javier|||0000-0003-0410-2285, Serramía Lobera, María Jesús, Alonso, Ester, Reguera, Rosa, Gómez Ramírez, Rafael|||0000-0001-6448-2414, Mata de la Mata, Francisco Javier de la|||0000-0003-0418-3935, Muñoz Fernández, María Ángeles
Format: article
Publication Date:2016
Country:España
Institution:Universidad de Alcalá (UAH)
Repository:e_Buah Biblioteca Digital Universidad de Alcalá
Language:English
OAI Identifier:oai:ebuah.uah.es:10017/34041
Online Access:http://hdl.handle.net/10017/34041
https://dx.doi.org/10.1021/acs.molpharmaceut.6b00420
Access Level:Open access
Keyword:Anti-inflammatory
Carbosilane dendrimers,
Dendrons
Ibuprofen
Drug release and macrophages.
Química
Chemistry
Description
Summary: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.