Study On Synthesis, Hepatic Targeting Action And Antitumor Activity Of Gal-HSA-5-Fu

Hepatic diseases, such as hepatoma and hepatitis, which need to be focused on prevention and treatment, are difficult to be charmed away as there is neither effective drug nor drugs which cannot to be delivered to hepatic pathological site in efficiency, that is known as no hepatic targeting effect. The hepatic targeting delivery system, a new style drug preparation, could play an activated role of preventing and curing liver disease as it can specifically transport the medicaments to liver, reduce delivery dose and times, elevate the therapeutic exponent and play down the side effects.There are two ways which can be used to achieve initiative hepatic targeting drug delivery. The first is asialoglycoprotein receptor which resides only at the cell surface of mammalian hepatocyte membrane. The second is mannose receptor and low density lipoprotein receptor in hepatic nonparenchyma membrane. With modifying the drug base on different receptors, it is possble to achieve hepatic targeting effect on receptor-ligand mediated.After comparing several hepatic targeting approaches, it is considered that the route mediated by asialoglycoprotein receptor may be the most suitable and the asialoglycoprotein receptor system is of both a high-affinity and a quick assimilation. Great attention has been payed to molecule modified with galactose to simulateasialoglycoprotein can be used as a drug carrier to achieve hepatic targeting effect. 5-Fluorouracil(5-FU), an analogue of uracil, which inhibits thymidylate...