Improved Activity of Rifampicin Against Biofilms of Staphylococcus aureus by Multicomponent Complexation

DAN CÓRDOBA, ANTONELLA V.; AIASSA, VIRGINIA; LONGHI, MARCELA R.; QUEVEDO, MARIO A.; ZOPPI, ARIANA

AAPS PHARMSCITECH

SPRINGER

Año: 2020 vol. 21

1530-9932

he aim of this study was to evaluate a multicomponent complex (MC) between rifampicin (RIF), β-cyclodextrin (β-CD), and selected amino acids to enhance the solubility and antibiofilm activity of RIF. After performing phase-solubility studies that demonstrated a considerable increase in the solubility of RIF for the MC, the corresponding solid system was prepared by a freeze-drying method. Characterization of the MC was performed by Fourier transform-infrared spectroscopy, thermal analysis, powder X-ray diffraction, and scanning electron microscopy. Structural analyses evidenced molecular interactions between the components, resulting in a MC with amorphous solid features. Structural studies involving both experimental (i.e., 1H NMR) and theoretical (i.e., molecular modeling) methodologies demonstrated the inclusion of the RIF piperazine ring in the β-CD cavity. The bioactivity of the MC measured against biofilms of Staphylococcus aureus showed a significant reduction in