Triple combination of carbosilane dendrimers, tenofovir and maraviroc as potential microbicide to prevent HIV-1 sexual transmission
| Autor: | Jose L. Jimenez, Javier Sánchez-Rodríguez, Rafael Gómez, María Jesús Serramía, Ma Ángeles Muñoz-Fernández, Francisco Javier de la Mata, Daniel Sepúlveda-Crespo |
|---|---|
| Rok vydání: | 2015 |
| Předmět: |
Dendrimers
Sexual transmission Materials science Tenofovir Anti-HIV Agents Cell Survival Biomedical Engineering Organophosphonates Medicine (miscellaneous) Bioengineering HIV Infections Development Pharmacology medicine.disease_cause Antiviral Agents Maraviroc chemistry.chemical_compound Mice Anti-Infective Agents Cyclohexanes Microbicide Dendrimer medicine Potency Animals Humans General Materials Science Cytotoxicity Mice Inbred BALB C Mucous Membrane Adenine Silanes Triazoles Virology Drug Combinations chemistry Vagina HIV-1 Female Irritation Software medicine.drug |
| Zdroj: | Nanomedicine (London, England). 10(6) |
| ISSN: | 1748-6963 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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