Litcius/Paper detail

New Organic Salt from Levofloxacin-Citric Acid: What Is the Impact on the Stability and Antibiotic Potency?

Ilma Nugrahani, Agnesya Namira Laksana, Hidehiro Uekusa, Hironaga Oyama

2022Molecules16 citationsDOIOpen Access PDF

Abstract

This research dealt with the composition, structure determination, stability, and antibiotic potency of a novel organic salt composed of levofloxacin (LF) and citric acid (CA), named levofloxacin-citrate (LC). After a stoichiometric proportion screening, the antibiotic-antioxidant reaction was conducted by slow and fast evaporation methods. A series of characterizations using thermal analysis, powder X-ray diffractometry, vibrational spectroscopy, and nuclear magnetic resonance confirmed LC formation. The new organic salt showed a distinct thermogram and diffractogram. Next, Fourier transform infrared indicated the change in N-methylamine and carboxylic stretching, confirmed by 1H nuclear magnetic resonance spectra to elucidate the 2D structure. Finally, single-crystal diffractometry determined LC as a new salt structure three-dimensionally. The attributive improvements were demonstrated on the stability toward the humidity and lighting of LC compared to LF alone. Moreover, the antibiotic potency of LF against Staphylococcus aureus (Gram-positive) and Escherichia coli (Gram-negative) enhanced ~1.5–2-fold by LC. Hereafter, LC is a potential salt antibiotic-antioxidant combination for dosage formulas development.

Topics & Concepts

Citric acidChemistrySalt (chemistry)PotencyThermal stabilityNuclear chemistryLevofloxacinAntibioticsOrganic chemistryBiochemistryIn vitroCrystallography and molecular interactionsDrug Solubulity and Delivery SystemsCrystallization and Solubility Studies