Improving the antimycobacterial drug Clofazimine through formation of organic salts by combination with fluoroquinolones

This work reports the synthesis, structural and thermal analysis, and in vitro evaluation of the antimicrobial activity of two new organic salts (OSs) derived from the antimycobacterial drug clofazimine and the fluoroquinolones ofloxacin or norfloxacin. Organic salts derived from active pharmaceutic...

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Bibliographic Details
Published in:International journal of molecular sciences 2023-01, Vol.24(2) (2), p.1-11
Main Authors: Bento, Clara M., Silva, Ana Teresa, Mansano, Bruno, Aguiar, Luísa, Teixeira, Cátia, Gomes, Maria Salomé, Gomes, Paula, Silva, Tânia, Ferraz, Ricardo
Format: Article
Language:English
Subjects:
Anti-Bacterial Agents - chemistry
Anti-Bacterial Agents - pharmacology
Antibiotics
Antiinfectives and antibacterials
Antimicrobial activity
Bacteria
Bioavailability
Biological activity
Clofazimine
Clofazimine - chemistry
Clofazimine - pharmacology
Disease
Fluoroquinolones
Fluoroquinolones - pharmacology
Formulations
GUMBOS
Ionic liquids
Mycobacterium
Norfloxacin
Ofloxacin
Organic salts
Pharmaceuticals
Repurposing
Rescuing
Salts
Solubility
Thermal analysis
Thermal stability
Tuberculosis
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Summary:This work reports the synthesis, structural and thermal analysis, and in vitro evaluation of the antimicrobial activity of two new organic salts (OSs) derived from the antimycobacterial drug clofazimine and the fluoroquinolones ofloxacin or norfloxacin. Organic salts derived from active pharmaceutical ingredients (API-OSs), as those herein disclosed, hold promise as cost-effective formulations with improved features over their parent drugs, thus enabling the mitigation of some of their shortcomings. For instance, in the specific case of clofazimine, its poor solubility severely limits its bioavailability. As compared to clofazimine, the clofazimine-derived OSs now reported have improved solubility and thermostability, without any major deleterious effects on the drug’s bioactivity profile.
ISSN:1422-0067
1661-6596
1422-0067
DOI:10.3390/ijms24021402