A. Sasaki et al., SYNTHESES OF NOVEL GALACTOSYL LIGANDS FOR LIPOSOMES AND THE INFLUENCEOF THE SPACER ON ACCUMULATION IN THE RAT-LIVER, Biological & pharmaceutical bulletin, 18(5), 1995, pp. 740-746
We modified the surface of liposomes with galactosyl ligands, At first
we determined whether or not the galactosyl moiety was exposed on the
liposomes, We then investigated the effect of the ligands on the hepa
tic accumulation of liposomes in rats, We introduced an oligoethylene
glycol moiety as a spacer. Among the various ligands tested, those wit
h a tri- or tetraethylene glycol moiety as a spacer caused the greates
t accumulation of liposomes in the liver, Liposomes bearing ligands wi
th a tri- or tetraethylene glycol moiety as a spacer, were aggregated
by Ricinus communis agglutinin. On the other hand, those modified with
ligands with a mono- or diethylene glycol spacer did not clearly aggl
utinate, These results show the importance of a spacer between the hom
ing device and the ligand anchor.