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Drug Deliv. 2016;23(3):992-8. doi: 10.3109/10717544.2014.926429. Epub 2014 Jun 17.

Preparation oral levofloxacin colon-specific microspheres delivery: in vitro and in vivo studies.

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  • 1a Department of Gastroenterology , Putuo Hospital, Shanghai University of Traditional Chinese Medicine , Shanghai , China.


The aim of this study was to prepare levofloxacin-loaded chitosan microspheres and to evaluate their in vitro and in vivo characteristics. Glutaraldehyde-crosslinked microspheres were prepared using a spray-drying method, and characterized in terms of the morphological examination, particle size distribution, entrapment efficiency, drug loading and in vitro release. Pharmacokinetics and colon biodistribution studies were used to evaluate that microspheres have more advantage than the conventional formulations. The surface morphology of the freeze-dried microspheres were smooth, discrete with a regular spherical to near-spherical shape. Size of the microspheres after freeze-drying was 4.96 ± 0.76 μm and well-distributed. The zeta potential of microspheres was -29.3 ± 2.1 mV. An average drug loading of 9.3 ± 0.4% and encapsulation efficiency of 81.1 ± 4.7% of levofloxacin microspheres were obtained with the optimized preparation parameters. The cumulative release rate of levofloxacin microspheres was followed by a sustained release and fitted for classic Higuchi kinetic model. In vivo studies showed that chitosan microspheres are thought to have the potential to maintain levofloxacin concentration within target ranges for a long time, decreasing side effects caused by concentration fluctuation, ensuring the efficiency of treatment and improving patient compliance by reducing dosing frequency. It also does not cause any harmful or toxic effect in colon and rectum as evaluated by histopathologic studies.


Chitosan; colon target; levofloxacin; microspheres; pharmacokinetics; release

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