SACCHARIDE-ASSISTED DELIVERY OF CYTOTOXIC LIPOSOMES TO HUMAN-MALIGNANT CELLS

The overexpression of lectins by malignant cells was applied for in vi tro targeting of liposomes equipped with a saccharide vector and loade d in the lipid phase with a lipid derivative of anticancer agent sarco lysine. The lectin specificity of human leukemia HL-60 and human lung adenocarcinoma ACL cells was revealed by tests with fluorescein-labele d sugar probes. With the help of fluorescent lipid dye it was shown th at active saccharide ligands increased the level of the vectored lipos ome binding to malignant cells by 50-80% as compared to liposomes with out vector or with inactive one. The degree of liposome/cell membrane fusion was monitored fluorometrically and was shown to be complete and independent of the vectors. The targeted drug-loaded liposomes had th e cytotoxic activity 2-4 times higher as compared to the vector-free o nes.