[Preparation of tegafur magnetic long-circulating thermosensitive liposomes and its pharmacokinetics in rats].
OBJECTIVE
To prepare tegafur magnetic long-circulating thermosensitive liposomes and study its pharmacokinetics and targeting properties in rats.


METHODS
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.


RESULTS
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.


CONCLUSIONS
Tegafur complex liposome can obviously increase the drug concentration in the liver and decrease the nephrotoxicity of the drug in rats.
Zeng
Zhao-wu
ZW
National Hepatobiliary and Enteric Surgery Research Center, Ministry of Health, Institute of Biomedical Engineering of Central South University, Changsha 410008, China. artgreenking@126.com
Wang
Xiao-li
XL
Zhou
Wei-hua
WH
Zhang
Yang-de
YD
D000818:Animals; D016503:Drug Delivery Systems; D005260:Female; D008081:Liposomes / Q000493:pharmacokinetics*; D008099:Liver / Q000378:metabolism*; D008280:Magnetics; D008297:Male; D053758:Nanoparticles; D011897:Random Allocation; D051381:Rats; D017208:Rats, Wistar; D005641:Tegafur / Q000493:pharmacokinetics*; D014018:Tissue Distribution
D008081:Liposomes; D005641:Tegafur