Preparation of tegafur magnetic long-circulating thermosensitive liposomes and its pharmacokinetics in rats.
- Author:
Zhao-wu ZENG
1
;
Xiao-li WANG
;
Wei-hua ZHOU
;
Yang-de ZHANG
Author Information
- Publication Type:Journal Article
- MeSH: Animals; Drug Delivery Systems; Female; Liposomes; pharmacokinetics; Liver; metabolism; Magnetics; Male; Nanoparticles; Random Allocation; Rats; Rats, Wistar; Tegafur; pharmacokinetics; Tissue Distribution
- From: Journal of Southern Medical University 2008;28(10):1864-1868
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVETo prepare tegafur magnetic long-circulating thermosensitive liposomes and study its pharmacokinetics and targeting properties in rats.
METHODSTegafur 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.
RESULTSThe 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.
CONCLUSIONTegafur complex liposome can obviously increase the drug concentration in the liver and decrease the nephrotoxicity of the drug in rats.
