title: Saccharide-assisted delivery of cytotoxic liposomes to human malignant cells.
abstract: The overexpression of lectins by malignant cells was applied for in vitro targeting of liposomes equipped with a saccharide vector and loaded in the lipid phase with a lipid derivative of anticancer agent sarcolysine. The lectin specificity of human leukemia HL-60 and human lung adenocarcinoma ACL cells was revealed by tests with fluorescein-labeled sugar probes. With the help of fluorescent lipid dye it was shown that active saccharide ligands increased the level of the vectored liposome binding to malignant cells by 50-80% as compared to liposomes without 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 the cytotoxic activity 2-4 times higher as compared to the vector-free ones.
authors.affiliation: Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Moscow.
authors.forename: E L
authors.initials: EL
authors.lastname: Vodovozova
authors.forename: G P
authors.initials: GP
authors.lastname: Gayenko
authors.forename: V I
authors.initials: VI
authors.lastname: Razinkov
authors.forename: E Y
authors.initials: EY
authors.lastname: Korchagina
authors.forename: N V
authors.initials: NV
authors.lastname: Bovin
authors.forename: J G
authors.initials: JG
authors.lastname: Molotkovsky
mesh_terms: D000180:Acrylic Resins / Q000494:pharmacology; D000230:Adenocarcinoma / Q000188:drug therapy / Q000378:metabolism; D015295:Antigens, Tumor-Associated, Carbohydrate / Q000378:metabolism; D002240:Carbohydrate Sequence; D002462:Cell Membrane / Q000378:metabolism; D004075:Diglycerides / Q000737:chemistry; D004337:Drug Carriers; D019793:Fluorescein / Q000737:chemistry; D018922:HL-60 Cells / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D008081:Liposomes / Q000378:metabolism* / Q000494:pharmacology*; D008558:Melphalan / Q000494:pharmacology; D008969:Molecular Sequence Data; D009844:Oligosaccharides / Q000494:pharmacology*; D012235:Rhodamines / Q000737:chemistry; D014407:Tumor Cells, Cultured; D000099166:Polyacrylamides
chemical_list: D000180:Acrylic Resins; D015295:Antigens, Tumor-Associated, Carbohydrate; D004075:Diglycerides; D004337:Drug Carriers; D019793:Fluorescein; D008081:Liposomes; D008558:Melphalan; D009844:Oligosaccharides; D012235:Rhodamines; D000099166:Polyacrylamides