Enrique Vacas Córdoba1, Eduardo Arnáiz, Francisco J De La Mata, Rafael Gómez, Manuel Leal, Marjorie Pion, Ma Angeles Muñoz-Fernández. 1. aLaboratorio InmunoBiología Molecular, Hospital General Universitario Gregorio Marañón bInstituto de Investigación Sanitaria del Gregorio Marañón cInorganic Chemistry Department, University of Alcalá, Alcalá de Henares dCentro Investigación Biomédica en Red, Bioingeniería, Biomateriales y Nanomedicina; CIBER-BNN, Madrid eLaboratory of Immunovirology, Clinic Unit of Infectious Diseases, Microbiology and Preventive Medicine, Institute of Biomedicine of Seville, IBiS, Virgen del Rocío University Hospital/CSIC/University of Seville, Spain.
Abstract
OBJECTIVE: Dendrimers have been shown as effective and safe anti-HIV compounds with great potential as topical microbicides. Currently, the most advanced microbicides are based on antiretrovirals. However, nowadays none of them has shown any success in clinical trials. DESIGN: Antiviral activity and combinatorial profile of different combinations between CCR5 co-receptor antagonist, maraviroc (MRV), and polyanionic carbosilane dendrimers against HIV-1 strains were evaluated. METHODS: Cellular in-vitro models were used to evaluate the antiviral action of combinations of carbosilane dendrimers/MRV against CCR5 and dual tropic viral strains in TZM.bl cells and peripheral blood mononuclear cells. Combinatorial analysis was performed using Calcusyn software. RESULTS: In the majority of combinations tested, dendrimers showed synergistic profile with MRV against CCR5 and dual tropic HIV-1. CONCLUSION: The evaluated two-drug combinations increase their antiviral potency supporting further clinical investigations to develop combinatorial formulated topical microbicides to fight against the worldwide HIV spread.
OBJECTIVE: Dendrimers have been shown as effective and safe anti-HIV compounds with great potential as topical microbicides. Currently, the most advanced microbicides are based on antiretrovirals. However, nowadays none of them has shown any success in clinical trials. DESIGN: Antiviral activity and combinatorial profile of different combinations between CCR5 co-receptor antagonist, maraviroc (MRV), and polyanionic carbosilane dendrimers against HIV-1 strains were evaluated. METHODS: Cellular in-vitro models were used to evaluate the antiviral action of combinations of carbosilane dendrimers/MRV against CCR5 and dual tropic viral strains in TZM.bl cells and peripheral blood mononuclear cells. Combinatorial analysis was performed using Calcusyn software. RESULTS: In the majority of combinations tested, dendrimers showed synergistic profile with MRV against CCR5 and dual tropic HIV-1. CONCLUSION: The evaluated two-drug combinations increase their antiviral potency supporting further clinical investigations to develop combinatorial formulated topical microbicides to fight against the worldwide HIV spread.
Authors: Michel D Wissing; Janet Mendonca; Madeleine S Q Kortenhorst; Nadine S Kaelber; Matthew Gonzalez; Eunice Kim; Hans Hammers; Paul J van Diest; Michael A Carducci; Sushant K Kachhap Journal: FASEB J Date: 2013-07-24 Impact factor: 5.191
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Authors: Enrique Vacas-Córdoba; Marek Maly; Francisco J De la Mata; Rafael Gómez; Marjorie Pion; M Ángeles Muñoz-Fernández Journal: Int J Nanomedicine Date: 2016-04-05
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Authors: Rafael Ceña-Diez; Enrique Vacas-Córdoba; Pilar García-Broncano; F J de la Mata; Rafael Gómez; Marek Maly; M Ángeles Muñoz-Fernández Journal: Int J Nanomedicine Date: 2016-05-19