AIM: To research the synergistic activity by triple combinations of carbosilane dendrimers with tenofovir and maraviroc as topical microbicide. METHODS: Cytotoxicity, anti-HIV-1 activity, vaginal irritation and histological analysis of triple combinations were determined. Analysis of combined effects and the median effective concentration were performed using CalcuSyn software. RESULTS: Combinations showed a greater broad-spectrum anti-HIV-1 activity than the single-drug, and preserved this activity in acid environment or seminal fluid. The strongest combinations were G2-STE16/G2-S24P/tenofovir, G2-STE16/G2-S16/maraviroc and G2-STE16/tenofovir/maraviroc at 2:2:1, 10:10:1 10:5:1 ratios, respectively. They demonstrated strong synergistic activity profile due to the weighted average combination indices varied between 0.06 and 0.38. No irritation was detected in female BALB/c mice. CONCLUSION: The three-drug combination increases their antiviral potency and act synergistically as potential microbicide.
AIM: To research the synergistic activity by triple combinations of carbosilane dendrimers with tenofovir and maraviroc as topical microbicide. METHODS:Cytotoxicity, anti-HIV-1 activity, vaginal irritation and histological analysis of triple combinations were determined. Analysis of combined effects and the median effective concentration were performed using CalcuSyn software. RESULTS: Combinations showed a greater broad-spectrum anti-HIV-1 activity than the single-drug, and preserved this activity in acid environment or seminal fluid. The strongest combinations were G2-STE16/G2-S24P/tenofovir, G2-STE16/G2-S16/maraviroc and G2-STE16/tenofovir/maraviroc at 2:2:1, 10:10:1 10:5:1 ratios, respectively. They demonstrated strong synergistic activity profile due to the weighted average combination indices varied between 0.06 and 0.38. No irritation was detected in female BALB/c mice. CONCLUSION: The three-drug combination increases their antiviral potency and act synergistically as potential microbicide.
Authors: Ignacio Rodríguez-Izquierdo; Daniel Sepúlveda-Crespo; Jose María Lasso; Salvador Resino; Ma Ángeles Muñoz-Fernández Journal: Wiley Interdiscip Rev Nanomed Nanobiotechnol Date: 2022-01-12
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
Authors: Rodriguez-Izquierdo I; Serramia Mj; Gomez R; De La Mata Fj; Bullido Mj; Muñoz-Fernández Ma Journal: J Clin Med Date: 2020-01-07 Impact factor: 4.241