A HEPATOCYTE TARGETING POLYETHYLENE GLYCO-GRAFTED POLY-L-LYSINE POLYMERIC GENE CARRIER
    9.
    发明公开
    A HEPATOCYTE TARGETING POLYETHYLENE GLYCO-GRAFTED POLY-L-LYSINE POLYMERIC GENE CARRIER 有权
    肝细胞LOOKING聚乙烯糖接枝的聚L-赖氨酸POLYMERS基因携带者

    公开(公告)号:EP1083882A4

    公开(公告)日:2004-08-18

    申请号:EP99925694

    申请日:1999-05-20

    CPC分类号: C12N15/87 A61K47/645

    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.

    A NOVEL CATIONIC LIPOPOLYMER AS BIOCOMPATIBLE GENE DELIVERY AGENT
    10.
    发明公开
    A NOVEL CATIONIC LIPOPOLYMER AS BIOCOMPATIBLE GENE DELIVERY AGENT 有权
    新的阳离子脂质ALS基因生物相容的转会资金

    公开(公告)号:EP1320386A1

    公开(公告)日:2003-06-25

    申请号:EP01968346.5

    申请日:2001-08-31

    CPC分类号: A61K9/1272 A61K47/645

    摘要: A biodegradable, novel cationic lipopolymer comprising a branched polyethylenimine(PEI), a cholesterol derived lipid anchor, and a biodegradable linker which covalently links the branched PEI and cholesterol derived lipid anchor. One example of such a novel lipolymer is poly{(ethylene imine)-co-[N-2-aminoethyl) ethylene imine]-co-[N-(N-cholesteryloxycarbonyl-(2-aminoethyl)ethylene imine]}('PEACE'). The cationic lipopolymers in the present invention can be used in drug delivery and are especially useful for delivery of a nucleic acid or any anionic bioactive agent to various organs and tissues after local or systemic administration. Methods of preparing and using the cationic lipopolymer gene carriers of the present invention to efficiently transfect cells, both in vitro and in vivo, are disclosed.