Specific Delivery To Liver Cells By Asialoglycoprotein Modified Antisence Oligodeo Ynucleotides In Vitro And In Vivo

Two kinds of galactose-terminal glyco-poly-L-lysine which could bind ASODNS electrostatic were synthesized.The ASODNS specificallly complementary to the polyadenylation signals of HBV mRNA were labelled with fluorescence.The specifically uptake of these two asialoglycoprotein modified ASODNS to Hep-G2 cells transfected with HBV genomes(2.2.15 cells)were detected by cell smear and flow cytometric analysis.The cells fluorescence staining rates were 75.3% and 83.8% in 3days cell incubation,while the non-modified ASODN group only 24.3%,the controlled group,1.8%.These asialoplycoprotein modified ASODN complex were injected into mice by intraperitoneal injection.After 8 hours,fluorescence of the ASODNS were observed predominantly ccumulated in liver tissue;while the non-tagrgeted ASODNS were distributied evenly in every organ in frozen sections of heart、lung、liver、spleen and kidney. The data indicated that these two kinds of asialoglycoprotein could deliver ASODNS specifically to liver cells in vitro and in vivo.