Mannose Liposomes for Liver NPC Targeting

Because Man-C4-Chol has a cationic charge, a cationic charge could also be induced on the surface of a Man-liposome. Therefore, Man-liposomes are also an attractive potential gene carrier because of this cationic charge that would allow electrical interaction with the gene. As far as in vivo gene transfection is concerned, the highest gene expression was observed in the liver after intravenous injection of pDNA/Man-liposome complexes (Man-lipoplex) in mice.66-68 In addition, gene transfer by a Man-liposome was mannose receptor-mediated because the gene expression with Man-lipoplex in the liver was significantly reduced by pre-dosing with manno-sylated bovine serum albumin. Because macrophages in the liver and spleen exist at the endothelial cells intervals and could make contact with the complex without passing through the sinusoid (100-200 nm), cell-selective gene transfection could be achieved by intravenous administration of Man-lipoplex. Therefore, a mannosylated gene carrier would be effective for the NPC-selective gene transfection system even after intravenous administration.94 As far as the application to cancer therapy using targeted gene delivery by mannosylated liposomes is concerned, DNA vaccine therapy is suitable because antigen encoded pDNA can be efficiently transfected into dendritic cells that expressed a large number of mannose receptors. Recently, Hattori et al.95 demonstrated that the targeted delivery of a DNA vaccine by Man-liposomes is a potent method for DNA vaccine therapy.

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