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Synthesis, Characterization, and Pharmacodynamics Study of Enrofloxacin Mesylate
Lin-Lin Pei1, Wen-Zhu Yang1, Jing-Yuan Fu1
1Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, Sichuan, People's Republic of China.
Introduction:
Enrofloxacin is used in the treatment of a wide variety of bacterial infections in mammals. However, its poor solubility limits the clinical use.
Methods:
In order to improve the solubility of enrofloxacin, the enrofloxacin mesylate (EM) were obtained by a chemical synthesis method. The characterization of EM was carried out using ultraviolet scan (UV), synchronous thermal analysis (SDT), fourier transform infrared spectrometer (FTIR) and mass spectrometry (MS), nuclear magnetic resonance (NMR) and X-ray powder diffraction analysis (XRPD). Acute toxicity of EM in Kunming mice was studied. Besides, pharmacokinetic studies were performed in New Zealand rabbits at a single oral dose of 10 mg/kg, and the antibacterial activity of EM was also evaluated.
Results:
EM was successfully synthesized and purified. The stoichiometric ratio of mesylate to enrofloxacin was 1:1 and the aqueous solubility of EM was 483.01±4.06 mg/mL, the solubility of EM was about 2000 times higher than enrofloxacin. The oral lethal dose (LD50) of EM was 1168.364 mg/kg, and the pharmacokinetics indicated that the oral relative bioavailability of EM was about 1.79 times and 1.48 times higher than that of enrofloxacin and enrofloxacin hydrochloride, respectively. In addition, the in vitro antibacterial activity of EM was not significantly changed compared with enrofloxacin and enrofloxacin hydrochloride.
Conclusion:
EM has higher solubility, low toxicity for oral use, and increases the oral bioavailability in rabbit. This study may be of benefit for the development of new enrofloxacin drugs.
Insights
Enrofloxacin mesylate (EM) significantly improves enrofloxacin solubility and oral bioavailability in rabbits. This novel formulation shows promise for developing enhanced enrofloxacin antibacterial drugs with reduced toxicity.
Area of Science:
- Veterinary Pharmacology
- Drug Development
- Medicinal Chemistry
Background:
- Enrofloxacin is a widely used antibiotic for bacterial infections in mammals.
- Poor aqueous solubility of enrofloxacin limits its clinical application.
- Developing strategies to enhance enrofloxacin solubility is crucial for improving its therapeutic efficacy.
Purpose of the Study:
- To synthesize and characterize enrofloxacin mesylate (EM) to improve enrofloxacin's solubility.
- To evaluate the safety, pharmacokinetic profile, and antibacterial activity of EM.
- To assess the potential of EM as a superior alternative to existing enrofloxacin formulations.
Main Methods:
- Enrofloxacin mesylate (EM) was synthesized and characterized using spectroscopic (UV, FTIR, MS, NMR) and analytical (SDT, XRPD) techniques.
- Acute oral toxicity was assessed in Kunming mice, and pharmacokinetic studies were conducted in New Zealand rabbits.
- In vitro antibacterial activity of EM was compared against enrofloxacin and enrofloxacin hydrochloride.
Main Results:
- EM was successfully synthesized with a 1:1 stoichiometric ratio and exhibited a ~2000-fold increase in aqueous solubility compared to enrofloxacin.
- EM demonstrated low acute oral toxicity (LD50 = 1168.364 mg/kg) and significantly enhanced oral bioavailability in rabbits.
- The in vitro antibacterial efficacy of EM remained comparable to enrofloxacin and its hydrochloride salt.
Conclusions:
- Enrofloxacin mesylate (EM) offers superior aqueous solubility and enhanced oral bioavailability.
- EM exhibits favorable safety and pharmacokinetic properties, making it a promising candidate for new drug development.
- This study supports the development of novel enrofloxacin-based therapeutics with improved clinical utility.
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