| Autor: |
Silveira N; Universidade Federal do Rio de Janeiro, Faculdade de Farmácia, Departamento de Produtos Naturais e Alimentos, Rio de Janeiro, Brazil., Longuinho MM; Universidade Federal do Rio de Janeiro, Faculdade de Farmácia, Departamento de Produtos Naturais e Alimentos, Rio de Janeiro, Brazil., Leitão SG; Universidade Federal do Rio de Janeiro, Faculdade de Farmácia, Departamento de Produtos Naturais e Alimentos, Rio de Janeiro, Brazil., Silva RS; Núcleo de Ciências Químicas, Instituto de Educação, Ciência e Tecnologia do Rio de Janeiro, Campus Rio de Janeiro, Rio de Janeiro, Brazil., Lourenço MC; Instituto de Pesquisa Clínica Evandro Chagas, Laboratório de Bacteriologia e Bioensaios em Micobactérias, FIOCRUZ, Rio de Janeiro, Brazil., Silva PE; Universidade Federal do Rio Grande, FURG, Laboratório de Micobactérias, Rio Grande, RS, Brazil., Pinto Mdo C; Universidade Federal do Rio de Janeiro, Instituto de Pesquisa de Produtos Naturais, Rio de Janeiro, Brazil., Abraçado LG; Universidade Federal do Rio de Janeiro, Instituto de Ciências Biológicas, RJ, Brazil., Finotelli PV; Universidade Federal do Rio de Janeiro, Faculdade de Farmácia, Departamento de Produtos Naturais e Alimentos, Rio de Janeiro, Brazil. Electronic address: pfinotelli@gmail.com. |
| Abstrakt: |
The aim of this work was to develop and characterize nanoparticles as carriers of lapazine, a phenazine derived from β-lapachone; its antimycobacterial activity is described for the first time as a potential treatment for tuberculosis. The lapazine was synthesized, and by using gas chromatography coupled to a flame ionization detector, it was possible to evaluate its purity degree of almost 100%. For better elucidation of the molecular structure, mass spectroscopy and 1H NMR were carried out and compared to the literature values. Lapazine was assayed in vitro against H37Rv Mycobacterium tuberculosis and a rifampicin-resistant strain, with minimum inhibitory concentration values of 3.00 and 1.56 μg mL(-1), respectively. The nanoparticles showed a polydispersity index of 0.16,mean diameter of 188.5 ± 1.7 mm, zeta potential of -15.03 mV, and drug loading of 54.71 mg g(-1) for poly-ε-caprolactone (PCL) nanoparticles and a polydispersity index of 0.318,mean diameter of 197.4 ± 2.7 mm, zeta potential of -13.43 mV and drug loading of 137.07 mg g(-1) for poly(DL-lactide-co-glycolide) (PLGA) nanoparticles. These results indicate that both polymeric formulations have good characteristics as potential lapazine carriers in the treatment of tuberculosis. |
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