Levofloxacin-Ketoprofen Multicomponent Salt Development as A Strategy to Improve the Antibiotic Potency and Anti-Inflammatory Performance

Authors

• Ilma Nugrahani, Department of Pharmacochemistry, School of Pharmacy, Bandung Institute of Technology, Bandung 40132, IndonesiaFollow
• Nadhira Dzaky Naushafira, Department of Pharmacochemistry, School of Pharmacy, Bandung Institute of Technology, Bandung 40132, IndonesiaFollow
• Nova Suliska, Department of Pharmacology and Clinical Pharmacy, School of Pharmacy, Bandung Institute of Technology, Bandung 40132, IndonesiaFollow
• Marlia Singgih Wibowo, Department of Pharmacochemistry, School of Pharmacy, Bandung Institute of Technology, Bandung 40132, IndonesiaFollow
• Hana Fauziah, Department of Pharmacochemistry, School of Pharmacy, Bandung Institute of Technology, Bandung 40132, Indonesia

Abstract

Levofloxacin is a fluoroquinolone antibiotic with higher solubility than those from previous generations, but it is light-sensitive. Antibiotics, including levofloxacin, are generally prescribed in combination with nonsteroidal anti-inflamma-tory drugs (NSAIDs) to treat inflammatory infections. Furthermore, NSAIDs have poor water solubility, which can be improved by forming salts or multicomponent systems. This study aimed to develop a multicomponent system from levofloxacin with ketoprofen, an NSAID, and to evaluate its physicochemical characteristics; antibiotic potency; in vivo anti-inflammatory activity; absorption, distribution, metabolism, and excretion (ADME); and in silico toxicity risk. First, a phase diagram was created to predict the interaction type in the resulting multicomponent system and determine the appropriate stoichiometric molar ratio. Next, the multicomponent system was prepared by solvent-drop grinding and analyzed using thermal analysis and powder X-ray diffractometry. The next stage involved structure determination, per-formed using Fourier transform infrared and nuclear magnetic resonance, which revealed the formation of a multicom-ponent salt. The salt was further shown to increase the stability of levofloxacin and the solubility of ketoprofen, thereby increasing antibiotic potency against gram-positive (Staphylococcus aureus) and gram-negative (Escherichia coli) bacte-ria, as well as inducing anti-inflammatory activity in Wistar rats. Complementing this study, in silico tests were conducted using SwissADME and ProTox 3.0, yielding data indicating that the formation of the levofloxacin-ketoprofen salt may reduce the risk of nerve, kidney, and respiratory toxicity, as well as mutagenic toxicity, and may lower blood-brain barrier penetration. Thus, the levofloxacin-ketoprofen salt has the potential to be further developed into various formulations and would require additional testing, including in vivo toxicity studies and clinical trials.

Recommended Citation

Nugrahani, Ilma; Naushafira, Nadhira Dzaky; Suliska, Nova; Wibowo, Marlia Singgih; and Fauziah, Hana (2026) "Levofloxacin-Ketoprofen Multicomponent Salt Development as A Strategy to Improve the Antibiotic Potency and Anti-Inflammatory Performance," Makara Journal of Science: Vol. 30: Iss. 3, Article 6.
DOI: 10.7454/mss.v30i3.3276
Available at: https://scholarhub.ui.ac.id/science/vol30/iss3/6