Improved efficiency of ibuprofen by cationic carbosilane dendritic conjugates

Abstract

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.