Cocrystals Enhance Biopharmaceutical and Antimicrobial Properties of Norfloxacin

Cocrystals Enhance Biopharmaceutical and Antimicrobial Properties of Norfloxacin

A solvate cocrystal of the antimicrobial norfloxacin (NFX) was formed by using isonicotinamide (INA) as a coformer with the solvent evaporation technique. The cocrystal formation was confirmed by performing solid-state characterization techniques. We evaluated the dissolution under supersaturated co...

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Bibliographic Details
Published in:Pharmaceutics Vol. 15; no. 9; p. 2211
Main Authors: Gomes, Samantha Nascimento, Biscaia, Isabela Fanelli Barreto, Lopes, Diana Schon, Mengarda, Mariana, Murakami, Fábio Seigi, Oliveira, Paulo Renato, Bernardi, Larissa Sakis
Format: Journal Article
Language:English
Published: Basel MDPI AG 26-08-2023
MDPI
Subjects:
Acids
Analysis
Antibiotics
Antimicrobial agents
Bioavailability
cocrystal
colorimetric microdilution assay
Drugs
Microorganisms
Norfloxacin
Pharmaceutical industry
Physical properties
Sodium
Solvents
Spectrum analysis
Brazil
Japan
United States > US
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Summary:A solvate cocrystal of the antimicrobial norfloxacin (NFX) was formed by using isonicotinamide (INA) as a coformer with the solvent evaporation technique. The cocrystal formation was confirmed by performing solid-state characterization techniques. We evaluated the dissolution under supersaturated conditions and also the solubility at the vertex of triphasic domain of cocrystal and NFX in both water and Fasted-State Simulated Intestinal Fluid (FaSSIF). The antimicrobial activity was evaluated using the microdilution technique. The cocrystal showed 1.8 times higher dissolution than NFX in water at 60 min and 1.3 times higher in FaSSIF at 180 min in the kinetic study. The cocrystal also had an increase in solubility of 8.38 times in water and 6.41 times in FaSSIF. The biopharmaceutical properties of NFX with cocrystallization improved antimicrobial action, as shown in the results of minimum inhibitory concentration (MIC) and inhibitory concentrations of 50% (IC50%) and 90% (IC90%). This paper presents, for the first time, a more in-depth analysis of the cocrystal of NFX–INA concerning its dissolution, solubility, and antimicrobial activity. In all these criteria, the cocrystal obtained better results compared to the pure drug.
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ISSN:1999-4923
1999-4923
DOI:10.3390/pharmaceutics15092211