Abstract To prolong the biological half-life of levofloxacin (LVFX) and increase the drug accumulation in the target site, an antibacterial agent, levofloxacin loaded liposomes with distearolyphos phatidyl ethanolamine-N-poly (ethylene glycol) 2000 (DSPE-PEG 2000) (LVFX-PEG-Lips) were prepared and evaluated. LVFX-PEG-Lips were prepared with the ammonium sulfate gradients method. The formulated liposomes were found to be relatively uniform in size 224.9±24.5 nm with a negative zeta potential –30.11±1.08 mV. The entrapment efficiency and drug loading ranged from 78.49% to 81.23% and 6.53% to 6.77%, respectively. In vitro drug release was monitored for up to 3 days, and the release behavior was in accordance with the Weibull equation. Pharmacokinetic parameters of LVFX-PEG-Lips were compared with those of levofloxacin solution (LVFX-Sol). The AUC and MRT of LVFX-PEG-Lips increased 5.7 and 9.2 fold, respectively. The encapsulation of LVFX in PEG-liposomes also changed its biodistribution in mice after intravenous injection in caudal vein. Compared with LVFX-Sol, the biodistribution of liposomal formulation in organs decreased, and can potentially reduce the side effects of free drugs and improve the treatment efficiency.
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2011, Vol. 6 
