Improved Activity of Rifampicin Against Biofilms of Staphylococcus aureus by Multicomponent Complexation
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, Seite 163 |
Sprache: |
Englisch |
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Beteiligte Personen: |
Dan Córdoba, Antonella V [VerfasserIn] |
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Links: |
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Themen: |
β-cyclodextrin |
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Anmerkungen: |
Date Completed 21.09.2020 Date Revised 21.09.2020 published: Electronic Citation Status MEDLINE |
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doi: |
10.1208/s12249-020-01706-z |
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funding: |
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Förderinstitution / Projekttitel: |
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PPN (Katalog-ID): |
NLM310689635 |
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