DESIGN OF QUATERNARY CHITOSAN CONJUGATE HAVING ANTENNARY GALACTOSE RESIDUES AS A GENE DELIVERY TOOL

It is well-known that some kinds of saccharide play the important role s in biological recognition on cellular surface. So, they are expected to be applied for cellular recognition devices. Recently, it was repo rted that cluster glycosides were effective in the specific interactio n between oligosaccharide chains and receptors. Since chitosan is a ca tionic natural polysaccharide, having formation ability of polyelectro lyte complex with DNA, it is expected to be used as a carrier of DNA i n gene delivery systems. So, in order to achieve an efficient gene del ivery via receptor-mediated endocytosis, the synthesis of novel polyca tionic polysaccharide derivative having recognizable branched sacchari de residues, N,N,N-trimethyl(TM)-chitosan/tetragalactose antenna conju gate (TC-Ga14A20), was carried out. The cellular recognition ability o f TC-Ga14A20 conjugate were tested, and then the possibility of its ap plication as a gene delivery tool was investigated. TC-Ga14A20 conjuga te showed high affinity to RCA(120) lectin and its polycation-DNA comp lex had the ability of specific gene delivery to hepatocyte. (C) 1997 Elsevier Science Ltd.