Syntheses of Novel Galactosyl Ligands for Liposomes and Their Accumulation in the Rat Liver

抄録

The effects of liposomes, bearing galactosyl ligands on their surface, on their clearance from circulation and on tissue distribution were studied in rats. The ligands were obtained through coupling 2, 3, 4, 6-tetraacetyl-{2-[2-(2-aminoethoxy) ethoxy] ethyl}-β-D-galactoside p-toluenesulfonate with hydrophobic anchors, followed by deprotection. We introduced mid-chain or long, branched or non-branched aliphatic chains, and cholesterol as anchors. Among various anchors tested, that with a dihexadecyl branch caused the greatest accumulation of liposomes in the liver. On the other hand, liposome bearing these ligands were aggregated by Ricinus communis agglutin. This showed that these ligands were similarly incorporated to liposomes. These results show the importance of the balance between lipophilicity and the structure of ligands.