A HEPATOCYTE TARGETING POLYETHYLENE GLYCO-GRAFTED POLY-L-LYSINE POLYMERIC GENE CARRIER.

摘要

A compound for polymeric targeted gene delivery carrier consisting of polyethylene glycol (PEG) grafted poly(L-lysine) (PLL) and a targeting moiety (TM), wherein at least one free amino function of the PLL is substituted with said PEG, at least one free amino function of the PLL is substituted with the TM, and the grafted PLL contains at least 50 % unsubstituted free amino function groups. TM is preferably lactose or galactose which are capable of specifically targeting a hepatoma cell or a liver cell. The new synthetic carriers with various substitution ratios of TM-PEG were characterized using NMR spectroscopy. The new polymeric gene carriers of this invention are capable of forming stable and soluble complexes with nucleic acids, which in turn are able to efficiently transform cells. PEG attached to the PLL gives better solubility properties to the gene/carrier complex and improved transfection efficiency without considerable cytotoxicity. Methods of preparing and using the TM-PEG-PLL as polymeric gene carriers to efficiently transfect cells are disclosed.