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Nanostructured Lipid Systems as a Strategy to Improve the in Vitro Cytotoxicity of Ruthenium(II) Compounds

: Tuberculosis is an ancient disease that is still present as a global public health problem. Our group has been investigating new molecules with anti-TB activity. In this context, inorganic chemistry has been a quite promising source of such molecules, with excellent results seen with ruthenium com...

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Autores principales: de Freitas, Eduardo Sinesio, da Silva, Patricia Bento, Chorilli, Marlus, Batista, Alzir Azevedo, Lopes, Érica de Oliveira, da Silva, Monize Martins, Leite, Clarice Queico Fujimura, Pavan, Fernando Rogério
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2014
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271922/
https://www.ncbi.nlm.nih.gov/pubmed/24818578
http://dx.doi.org/10.3390/molecules19055999
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author de Freitas, Eduardo Sinesio
da Silva, Patricia Bento
Chorilli, Marlus
Batista, Alzir Azevedo
Lopes, Érica de Oliveira
da Silva, Monize Martins
Leite, Clarice Queico Fujimura
Pavan, Fernando Rogério
author_facet de Freitas, Eduardo Sinesio
da Silva, Patricia Bento
Chorilli, Marlus
Batista, Alzir Azevedo
Lopes, Érica de Oliveira
da Silva, Monize Martins
Leite, Clarice Queico Fujimura
Pavan, Fernando Rogério
author_sort de Freitas, Eduardo Sinesio
collection PubMed
description : Tuberculosis is an ancient disease that is still present as a global public health problem. Our group has been investigating new molecules with anti-TB activity. In this context, inorganic chemistry has been a quite promising source of such molecules, with excellent results seen with ruthenium compounds. Nanostructured lipid systems may potentiate the action of drugs by reducing the required dosage and side effects and improving the antimicrobial effects. The aim of this study was to develop a nanostructured lipid system and then characterize and apply these encapsulated compounds (SCARs 1, 2 and 4) with the goal of improving their activity by decreasing the Minimum Inhibitory Concentration (MIC(90)) and reducing the cytotoxicity (IC(50)). The nanostructured system was composed of 10% phase oil (cholesterol), 10% surfactant (soy oleate, soy phosphatidylcholine and Eumulgin(®)) and 80% aqueous phase (phosphate buffer pH = 7.4). Good activity against Mycobacterium tuberculosis was maintained after the incorporation of the compounds into the nanostructured lipid system, while the cytotoxicity decreased dramatically, in some cases up to 20 times less toxic than the unencapsulated drug.
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spelling pubmed-62719222018-12-21 Nanostructured Lipid Systems as a Strategy to Improve the in Vitro Cytotoxicity of Ruthenium(II) Compounds de Freitas, Eduardo Sinesio da Silva, Patricia Bento Chorilli, Marlus Batista, Alzir Azevedo Lopes, Érica de Oliveira da Silva, Monize Martins Leite, Clarice Queico Fujimura Pavan, Fernando Rogério Molecules Article : Tuberculosis is an ancient disease that is still present as a global public health problem. Our group has been investigating new molecules with anti-TB activity. In this context, inorganic chemistry has been a quite promising source of such molecules, with excellent results seen with ruthenium compounds. Nanostructured lipid systems may potentiate the action of drugs by reducing the required dosage and side effects and improving the antimicrobial effects. The aim of this study was to develop a nanostructured lipid system and then characterize and apply these encapsulated compounds (SCARs 1, 2 and 4) with the goal of improving their activity by decreasing the Minimum Inhibitory Concentration (MIC(90)) and reducing the cytotoxicity (IC(50)). The nanostructured system was composed of 10% phase oil (cholesterol), 10% surfactant (soy oleate, soy phosphatidylcholine and Eumulgin(®)) and 80% aqueous phase (phosphate buffer pH = 7.4). Good activity against Mycobacterium tuberculosis was maintained after the incorporation of the compounds into the nanostructured lipid system, while the cytotoxicity decreased dramatically, in some cases up to 20 times less toxic than the unencapsulated drug. MDPI 2014-05-09 /pmc/articles/PMC6271922/ /pubmed/24818578 http://dx.doi.org/10.3390/molecules19055999 Text en © 2014 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
de Freitas, Eduardo Sinesio
da Silva, Patricia Bento
Chorilli, Marlus
Batista, Alzir Azevedo
Lopes, Érica de Oliveira
da Silva, Monize Martins
Leite, Clarice Queico Fujimura
Pavan, Fernando Rogério
Nanostructured Lipid Systems as a Strategy to Improve the in Vitro Cytotoxicity of Ruthenium(II) Compounds
title Nanostructured Lipid Systems as a Strategy to Improve the in Vitro Cytotoxicity of Ruthenium(II) Compounds
title_full Nanostructured Lipid Systems as a Strategy to Improve the in Vitro Cytotoxicity of Ruthenium(II) Compounds
title_fullStr Nanostructured Lipid Systems as a Strategy to Improve the in Vitro Cytotoxicity of Ruthenium(II) Compounds
title_full_unstemmed Nanostructured Lipid Systems as a Strategy to Improve the in Vitro Cytotoxicity of Ruthenium(II) Compounds
title_short Nanostructured Lipid Systems as a Strategy to Improve the in Vitro Cytotoxicity of Ruthenium(II) Compounds
title_sort nanostructured lipid systems as a strategy to improve the in vitro cytotoxicity of ruthenium(ii) compounds
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271922/
https://www.ncbi.nlm.nih.gov/pubmed/24818578
http://dx.doi.org/10.3390/molecules19055999
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