Preparation and evaluation of enrofloxacin microspheres and tissue distribution in rats

作者：Fan Yang, Jijun Kang, Fang Yang, Zhensheng Zhao, Tao Kong, Zhenling Zeng · 发表于：Journal of Veterinary Science · 年份：2015 · DOI：10.4142/jvs.2015.16.2.157 · 被引用次数：20 · 研究领域：Antibiotics Pharmacokinetics and Efficacy、Advanced Drug Delivery Systems、Inhalation and Respiratory Drug Delivery

New enrofloxacin microspheres were formulated, and their physical properties, lung-targeting ability, and tissue distribution in rats were examined. The microspheres had a regular and round shape. The mean diameter was 10.06 µm, and the diameter of 89.93% of all microspheres ranged from 7.0 µm to 30.0 µm. Tissue distribution of the microspheres was evaluated along with a conventional enrofloxacin preparation after a single intravenous injection (7.5 mg of enrofloxacin/kg bw). The results showed that the elimination half-life (t1/2β) of enrofloxacin from lung was prolonged from 7.94 h for the conventional enrofloxacin to 13.28 h for the microspheres. Area under the lung concentration versus time curve from 0 h to ∞ (AUC00∞) was increased from 11.66 h·µg/g to 508.00 h·µg/g. The peak concentration (Cmax) in lung was increased from 5.95 µg/g to 93.36 µg/g. Three lung-targeting parameters were further assessed and showed that the microspheres had remarkable lung-targeting capabilities.