J Vet Sci.  2015 Jun;16(2):157-164. 10.4142/jvs.2015.16.2.157.

Preparation and evaluation of enrofloxacin microspheres and tissue distribution in rats

• Yang F
• Kang J
• Yang F
• Zhao Z
• Kong T
• Zeng Z

• KMID: 2164524
• DOI: http://doi.org/10.4142/jvs.2015.16.2.157

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 microm, and the diameter of 89.93% of all microspheres ranged from 7.0 microm to 30.0 microm. 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 (t(1/2beta)) 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 infinity (AUC(0-infinity)) was increased from 11.66 h.microg/g to 508.00 h.microg/g. The peak concentration (Cmax) in lung was increased from 5.95 microg/g to 93.36 microg/g. Three lung-targeting parameters were further assessed and showed that the microspheres had remarkable lung-targeting capabilities.

Keyword

enrofloxacin; lung-targeting; microsphere; preparation; tissue distribution

MeSH Terms

Animals
Anti-Bacterial Agents/*adverse effects
Drug Delivery Systems/instrumentation/*methods
Female
Fluoroquinolones/*adverse effects
Half-Life
Humans
Injections, Intravenous
Lung/*drug effects
Male
*Microspheres
Rats
Rats, Sprague-Dawley
Tissue Distribution
Anti-Bacterial Agents
Fluoroquinolones

Figure

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  Fig. 1 (A) Optical photomicrograph of the enrofloxacin microspheres (ENR-MICs). (B) Scanning electron microscopy micrograph of the ENR raw material. (C) Scanning electron microscopy micrograph of an ENR-MIC. Scale bar = 50 µm. Magnification: 100× (A), 150× (B), 3000× (C).

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  Fig. 2 Particle size distribution of the ENR-MICs. Size distribution was determined using 800 particles chosen randomly.

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  Fig. 3 In vitro drug release results for the ENR-MICs and ENR raw material (mean ± SD, n = 3).

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  Fig. 4 Semilogarithmic plots showing the mean ± SD plasma and tissue concentrations of ENR vs. time in rats (n = 6) after intravenous administration of the ENR-MICs (7.5 mg/kg bw).

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  Fig. 5 Semilogarithmic plots showing the mean ± SD plasma and tissue concentrations of ENR vs. time in rats (n = 6) after intravenous administration of the ENR-INJ (7.5 mg/kg bw).

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