Gp. Yan et al., Study on the anticancer drug 5-fluorouracil-conjugated polyaspartamide containing hepatocyte-targeting group, J BIOACT C, 16(4), 2001, pp. 277-293
Anticancer conjugates of 5-fluorouracil (5-Fu) and polyaspartamide, contain
ing pyridoxamine as the hepatocyte-targeting group, were synthesized and ch
aracterized. Their sustained release properties and biodistribution were ev
aluated. The 5-Fu was targeted to specific organs, such as the liver, and h
ad a sustained in vitro release rate in PBS. In vitro cytotoxicity assay sh
owed that the polymeric drugs exhibited low cytotoxicity to the human liver
cells (L-02). These polymeric drugs possess high anticancer efficiencies a
nd induced apoptosis in the human hepatic tumor cells (Bel-7204).