title: Improved Efficiency of Ibuprofen by Cationic Carbosilane Dendritic Conjugates.
abstract: In order to improve the efficiency of the anti-inflammatory drug ibuprofen, cationic carbosilane dendrimers and dendrons with ibuprofen at their periphery or at their focal point, respectively, have been synthesized, and the release of the drug was studied using HPLC. Macrophages were used to evaluate the anti-inflammatory effect of the ibuprofen-conjugated dendritic systems and compared with mixtures of non-ibuprofen dendritic systems in the presence of the drug. The cationic ibuprofen-conjugated dendron was the compound that showed higher anti-inflammatory properties. It reduces the LPS-induced COX-2 expression and decreases the release of several inflammatory cytokines such as TNFα, IL-1β, IL-6, and CCL3. These results open new perspectives in the use of these compounds as drug carriers.
authors.affiliation: Laboratorio Inmuno-Biología Molecular, Hospital General Universitario Gregorio Marañón, Spanish HIV HGM BioBank and Instituto de Investigación Sanitaria Gregorio Marañón , 28007 Madrid, Spain.|Networking Research Center on Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN) , Spain.
authors.forename: Ana Judith
authors.initials: AJ
authors.lastname: Perisé-Barrios
authors.affiliation: Departamento de Química Orgánica y Química Inorgánica, Campus Universitario, Universidad de Alcalá , Alcalá de Henares, Madrid, Spain.
authors.forename: Elena
authors.initials: E
authors.lastname: Fuentes-Paniagua
authors.affiliation: Networking Research Center on Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN) , Spain.|Departamento de Química Orgánica y Química Inorgánica, Campus Universitario, Universidad de Alcalá , Alcalá de Henares, Madrid, Spain.
authors.forename: Javier
authors.initials: J
authors.lastname: Sánchez-Nieves
authors.affiliation: Laboratorio Inmuno-Biología Molecular, Hospital General Universitario Gregorio Marañón, Spanish HIV HGM BioBank and Instituto de Investigación Sanitaria Gregorio Marañón , 28007 Madrid, Spain.
authors.forename: M Jesús
authors.initials: MJ
authors.lastname: Serramía
authors.affiliation: Laboratorio Inmuno-Biología Molecular, Hospital General Universitario Gregorio Marañón, Spanish HIV HGM BioBank and Instituto de Investigación Sanitaria Gregorio Marañón , 28007 Madrid, Spain.
authors.forename: Esther
authors.initials: E
authors.lastname: Alonso
authors.affiliation: Departamento de Ciencias Biomédicas, Universidad de León , Campus de Vegazana s/n, 24071 León, Spain.
authors.forename: Rosa M
authors.initials: RM
authors.lastname: Reguera
authors.affiliation: Networking Research Center on Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN) , Spain.|Departamento de Química Orgánica y Química Inorgánica, Campus Universitario, Universidad de Alcalá , Alcalá de Henares, Madrid, Spain.
authors.forename: Rafael
authors.initials: R
authors.lastname: Gómez
authors.affiliation: Networking Research Center on Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN) , Spain.|Departamento de Química Orgánica y Química Inorgánica, Campus Universitario, Universidad de Alcalá , Alcalá de Henares, Madrid, Spain.
authors.forename: F Javier
authors.initials: FJ
authors.lastname: de la Mata
authors.affiliation: Laboratorio Inmuno-Biología Molecular, Hospital General Universitario Gregorio Marañón, Spanish HIV HGM BioBank and Instituto de Investigación Sanitaria Gregorio Marañón , 28007 Madrid, Spain.|Networking Research Center on Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN) , Spain.
authors.forename: M Ángeles
authors.initials: MÁ
authors.lastname: Muñoz-Fernández
mesh_terms: D000893:Anti-Inflammatory Agents / Q000737:chemistry* / Q000494:pharmacology*; D002412:Cations / Q000737:chemistry*; D002454:Cell Differentiation; D002478:Cells, Cultured; D054405:Chemokine CCL3 / Q000378:metabolism; D050091:Dendrimers / Q000737:chemistry*; D006801:Humans; D007052:Ibuprofen / Q000737:chemistry* / Q000494:pharmacology*; D053583:Interleukin-1beta / Q000378:metabolism; D015850:Interleukin-6 / Q000378:metabolism; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism; D018124:Receptors, Tumor Necrosis Factor / Q000378:metabolism; D012821:Silanes / Q000737:chemistry*
chemical_list: D000893:Anti-Inflammatory Agents; D002412:Cations; D054405:Chemokine CCL3; D050091:Dendrimers; D053583:Interleukin-1beta; D015850:Interleukin-6; D018124:Receptors, Tumor Necrosis Factor; D012821:Silanes; C504072:carbosilane; D007052:Ibuprofen
keywords: anti-inflammatory; carbosilane dendrimers; dendrons; drug release; ibuprofen; macrophages