Preparation and evaluation of enrofloxacin microspheres and tissue distribution in rats

Abstract

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 ∞ (AUC0-∞) 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.

<p>An Efficient, Lung-Targeted, Drug-Delivery System To Treat Asthma Via Microparticles</p>

“…These microspheres are obtained from spray-drying techniques, and the results of this study are also supported by other researchers. 61,62 Both drug-distribution schemes (ie, with SPP and conventional approaches) indicate that the organ/tissue is exposed to the drug to a greater extent if the Re (drug exposure) value is >1. The lungtargeting efficacy (Te) of the SPP formulation and the conventional formulation are shown in Table 4.…”

<p>Solid lipid nanoparticles with enteric coating for improving stability, palatability, and oral bioavailability of enrofloxacin</p>

“…1 It has been widely used in veterinary clinic because of its broad antibacterial spectrum, strong bactericidal activity, low adverse reactions, and high postantibacterial effect. 2 However, ENR has a bitter taste. 3,4 The poor palatability limits its oral administration since the animals with keen sense tastes, especially for pigs and cows, exhibit more possibility to refuse the bitter drugs.…”

Pharmacokinetic/pharmacodynamic relationship of enrofloxacin against Aeromonas hydrophila in crucian carp (Carassius auratus gibelio)

“…Enrofloxacin (ENR) is a third‐generation fluorinated quinolone which is extensively used in veterinary medicine (della Rocca, Di Salvo, Malvisi & Sello, ). It has broad spectrum activity, especially against gram‐negative bacteria, such as A. hydrophila (Guz & Kozińska, ; Yang et al., ). The drug has been demonstrated to be effective in the treatment of various bacterial fish infections, including Aeromonas hydrophila, Vibrio anguillarum, Yersinia spp., Pasteurella spp ., and Aeromonas salmonicida, and Renibacterium salmoninarum (Akhlaghi & Sharifi Yazdi, ; Guz & Kozińska, ; Hsu, Wooster & Bowser, ; Maluping et al., ).…”