Preparation of tegafur magnetic long-circulating thermosensitive liposomes and its pharmacokinetics in rats / 南方医科大学学报

ABSTRACT

<p><b>OBJECTIVE</b>To prepare tegafur magnetic long-circulating thermosensitive liposomes and study its pharmacokinetics and targeting properties in rats.</p><p><b>METHODS</b>Tegafur magnetic long-circulating thermosensitive liposomes were prepared by reversed phase-ultrasound method and its concentration in various organs of rats were detected with high-performance liquid chromatography.</p><p><b>RESULTS</b>The average size of tegafur magnetic long-circulating thermosensitive liposomes was about 126 nm, which showed strong ferromagnetism and superparamagnetism. Eight hours after administration in rats, the AUC value of tegafur magnetic long-circulating thermosensitive liposome in the liver was 17.4 times of that of the free drug, and 3.9 times of that of tegafur long-circulating liposome. The concentrations of the thermosensitive liposome in the serum and kidney were lower than those of the free drug, with a liver-targeting ratio reaching 73.9% and obviously prolonged half-life than the free drug.</p><p><b>CONCLUSION</b>Tegafur complex liposome can obviously increase the drug concentration in the liver and decrease the nephrotoxicity of the drug in rats.</p>