Improved Activity of Rifampicin Against Biofilms of Staphylococcus aureus by Multicomponent Complexation
Abstract The 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 the metabolic activity of the bacterium. Overall, the studied MC exhibited promising properties for the development of pharmaceutical formulations to treat bacterial infections..
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2020 |
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| Erschienen: |
2020 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:21 |
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| Enthalten in: |
AAPS PharmSciTech - 21(2020), 5 vom: 02. Juni |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Dan Córdoba, Antonella V. [VerfasserIn] |
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| Links: |
Volltext [lizenzpflichtig] |
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| BKL: |
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| doi: |
10.1208/s12249-020-01706-z |
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| 520 | |a Abstract The 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 the metabolic activity of the bacterium. Overall, the studied MC exhibited promising properties for the development of pharmaceutical formulations to treat bacterial infections. | ||
| 700 | 1 | |a Aiassa, Virginia |e verfasserin |4 aut | |
| 700 | 1 | |a Longhi, Marcela R. |e verfasserin |4 aut | |
| 700 | 1 | |a Quevedo, Mario A. |e verfasserin |4 aut | |
| 700 | 1 | |a Zoppi, Ariana |e verfasserin |4 aut | |
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