Anticancer conjugates of 5-fluorouracil (5-Fu) and polyaspartamide, containing pyridoxamine as the hepatocyte-targeting group, were synthesized and characterized. Their sustained release properties and biodistribution were evaluated. The 5-Fu was targeted to specific organs, such as the liver, and had a sustained in vitro release rate in PBS. In vitro cytotoxicity assay showed that the polymeric drugs exhibited low cytotoxicity to the human liver cells (L-02). These polymeric drugs possess high anticancer efficiencies and induced apoptosis in the human hepatic tumor cells (Bel-7204).
INTRODUCTIONP olymer-based drug delivery systems are used to optimize the therapeutic properties of drugs and render them safer, effective and reliable [1]. Moreover, polymeric drugs and macromolecules used as drug carriers can be easily synthesized at low cost, freely water-soluble, non-toxic, non-immunogenic and well characterized from the physico-chemical point of view [2,3].