Nanostructured Lipid Systems as a Strategy to Improve the in Vitro Cytotoxicity of Ruthenium(II) Compounds
Autor(a) principal: | |
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Data de Publicação: | 2014 |
Outros Autores: | , , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Institucional da UNESP |
Texto Completo: | http://dx.doi.org/10.3390/molecules19055999 http://hdl.handle.net/11449/113460 |
Resumo: | 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 (MIC90) and reducing the cytotoxicity (IC50). The nanostructured system was composed of 10% phase oil (cholesterol), 10% surfactant (soy oleate, soy phosphatidylcholine and Eumulgin (R)) 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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Nanostructured Lipid Systems as a Strategy to Improve the in Vitro Cytotoxicity of Ruthenium(II) Compoundsruthenium complexestuberculosisnanostructured lipid systemsTuberculosis 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 (MIC90) and reducing the cytotoxicity (IC50). The nanostructured system was composed of 10% phase oil (cholesterol), 10% surfactant (soy oleate, soy phosphatidylcholine and Eumulgin (R)) 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.Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)NPQ-GlaxoPROPEUniv Estadual Paulista, Fac Ciencias Farmaceut, Dept Ciencias Biol, BR-14801902 Sao Paulo, BrazilUniv Estadual Paulista, Fac Ciencias Farmaceut, Dept Farmacos & Medicamentos, BR-14801902 Sao Paulo, BrazilUniv Fed Sao Carlos, Dept Quim, BR-13565905 Sao Paulo, BrazilUniv Estadual Paulista, Fac Ciencias Farmaceut, Dept Ciencias Biol, BR-14801902 Sao Paulo, BrazilUniv Estadual Paulista, Fac Ciencias Farmaceut, Dept Farmacos & Medicamentos, BR-14801902 Sao Paulo, BrazilFAPESP: 13/09265-7FAPESP: 13/14957-5NPQ-Glaxo406827/2012-5PROPE0102/004/43Mdpi AgUniversidade Estadual Paulista (Unesp)Universidade Federal de São Carlos (UFSCar)Freitas, Eduardo Sinesio de [UNESP]Silva, Patricia Bento da [UNESP]Chorilli, Marlus [UNESP]Batista, Alzir AzevedoLopes, Erica de Oliveira [UNESP]Silva, Monize Martins daLeite, Clarice Queico Fujimura [UNESP]Pavan, Fernando Rogério [UNESP]2014-12-03T13:11:43Z2014-12-03T13:11:43Z2014-05-01info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/article5999-6008application/pdfhttp://dx.doi.org/10.3390/molecules19055999Molecules. Basel: Mdpi Ag, v. 19, n. 5, p. 5999-6008, 2014.1420-3049http://hdl.handle.net/11449/11346010.3390/molecules19055999WOS:000337113000034WOS000337113000034.pdf2114570774349859Web of Sciencereponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengMolecules3.0980,855info:eu-repo/semantics/openAccess2024-06-24T13:46:34Zoai:repositorio.unesp.br:11449/113460Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462024-08-05T23:52:22.741495Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false |
dc.title.none.fl_str_mv |
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 |
spellingShingle |
Nanostructured Lipid Systems as a Strategy to Improve the in Vitro Cytotoxicity of Ruthenium(II) Compounds Freitas, Eduardo Sinesio de [UNESP] ruthenium complexes tuberculosis nanostructured lipid systems |
title_short |
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_sort |
Nanostructured Lipid Systems as a Strategy to Improve the in Vitro Cytotoxicity of Ruthenium(II) Compounds |
author |
Freitas, Eduardo Sinesio de [UNESP] |
author_facet |
Freitas, Eduardo Sinesio de [UNESP] Silva, Patricia Bento da [UNESP] Chorilli, Marlus [UNESP] Batista, Alzir Azevedo Lopes, Erica de Oliveira [UNESP] Silva, Monize Martins da Leite, Clarice Queico Fujimura [UNESP] Pavan, Fernando Rogério [UNESP] |
author_role |
author |
author2 |
Silva, Patricia Bento da [UNESP] Chorilli, Marlus [UNESP] Batista, Alzir Azevedo Lopes, Erica de Oliveira [UNESP] Silva, Monize Martins da Leite, Clarice Queico Fujimura [UNESP] Pavan, Fernando Rogério [UNESP] |
author2_role |
author author author author author author author |
dc.contributor.none.fl_str_mv |
Universidade Estadual Paulista (Unesp) Universidade Federal de São Carlos (UFSCar) |
dc.contributor.author.fl_str_mv |
Freitas, Eduardo Sinesio de [UNESP] Silva, Patricia Bento da [UNESP] Chorilli, Marlus [UNESP] Batista, Alzir Azevedo Lopes, Erica de Oliveira [UNESP] Silva, Monize Martins da Leite, Clarice Queico Fujimura [UNESP] Pavan, Fernando Rogério [UNESP] |
dc.subject.por.fl_str_mv |
ruthenium complexes tuberculosis nanostructured lipid systems |
topic |
ruthenium complexes tuberculosis nanostructured lipid systems |
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 (MIC90) and reducing the cytotoxicity (IC50). The nanostructured system was composed of 10% phase oil (cholesterol), 10% surfactant (soy oleate, soy phosphatidylcholine and Eumulgin (R)) 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. |
publishDate |
2014 |
dc.date.none.fl_str_mv |
2014-12-03T13:11:43Z 2014-12-03T13:11:43Z 2014-05-01 |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://dx.doi.org/10.3390/molecules19055999 Molecules. Basel: Mdpi Ag, v. 19, n. 5, p. 5999-6008, 2014. 1420-3049 http://hdl.handle.net/11449/113460 10.3390/molecules19055999 WOS:000337113000034 WOS000337113000034.pdf 2114570774349859 |
url |
http://dx.doi.org/10.3390/molecules19055999 http://hdl.handle.net/11449/113460 |
identifier_str_mv |
Molecules. Basel: Mdpi Ag, v. 19, n. 5, p. 5999-6008, 2014. 1420-3049 10.3390/molecules19055999 WOS:000337113000034 WOS000337113000034.pdf 2114570774349859 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
Molecules 3.098 0,855 |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
5999-6008 application/pdf |
dc.publisher.none.fl_str_mv |
Mdpi Ag |
publisher.none.fl_str_mv |
Mdpi Ag |
dc.source.none.fl_str_mv |
Web of Science reponame:Repositório Institucional da UNESP instname:Universidade Estadual Paulista (UNESP) instacron:UNESP |
instname_str |
Universidade Estadual Paulista (UNESP) |
instacron_str |
UNESP |
institution |
UNESP |
reponame_str |
Repositório Institucional da UNESP |
collection |
Repositório Institucional da UNESP |
repository.name.fl_str_mv |
Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP) |
repository.mail.fl_str_mv |
|
_version_ |
1808129560231804928 |