Abstract
A synthesis of a lipophilic derivative of methotrexate was devised, this being suitable for insertion into the membranes of carrier liposomes. The conjugate consisted of a rac-1,2-dioleoylglycerol residue attached via an ester bond to methotrexate via the β-alanyl-N-carbonylmethylene linker. A liposomal formulation of the derivative showed cytotoxic activity in cultures of M3 melanoma cells; this activity depended on the structure of the carbohydrate ligands on the liposome surface. As compared with a control liposome preparation carrying a diglyceride derivative of methotrexate and bearing an inactive pentaol aminoglucitol ligand, the cytotoxicity of liposomes carrying trisaccharide A residues was 1.5 times greater and that of liposome carrying tetrasaccharide sialyl-Lewis X was three times greater.
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