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

Author(s)

de Freitas, Eduardo Sinesio ^[1] ; da Silva, Patricia Bento ^[2] ; Chorilli, Marlus ^[2] ; Batista, Alzir Azevedo ^[3] ; Lopes, Erica de Oliveira ^[1] ; da Silva, Monize Martins ^[3] ; Fujimura Leite, Clarice Queico ^[1] ; Pavan, Fernando Rogerio ^[1]

Affiliation

^[1] Univ Estadual Paulista, Fac Ciencias Farmaceut, Dept Ciencias Biol, BR-14801902 Sao Paulo - Brazil

^[2] Univ Estadual Paulista, Fac Ciencias Farmaceut, Dept Farmacos & Medicamentos, BR-14801902 Sao Paulo - Brazil

^[3] Univ Fed Sao Carlos, Dept Quim, BR-13565905 Sao Paulo - Brazil

• Document type: Journal article
• Source: Molecules; v. 19, n. 5, p. 5999-6008, MAY 2014.
• Web of Science Citations: 11

Abstract

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. (AU)

• FAPESP's process: 13/09265-7 - Evaluation of the potential nanostructured lipid systems for administration of Cu(II) compounds applicable in optimizing the treatment of tuberculosis
• Grantee: Patrícia Bento da Silva
• Support Opportunities: Scholarships in Brazil - Post-Doctoral
• FAPESP's process: 13/14957-5 - Research potential against tuberculosis of a new class of furoxan compounds and nanostructured compounds of the ruthenium(II) and copper (II)
• Grantee: Fernando Rogério Pavan
• Support Opportunities: Research Grants - Young Investigators Grants