El. Vodovozova et al., The transport of cytotoxic liposomes to malignant cells by means of carbohydrate determinants, BIOORG KHIM, 24(10), 1998, pp. 760-767
A method of the synthesis of lipophilic glycoconjugates (vectors) on the ba
sis of polyethyleneglycol-containing detergent was proposed. It has been sh
own by flow cytofluorometry that fluorescent labeled liposomes equipped wit
h beta-galactosyl conjugate are bound human leukosis HL-60 cells more effec
tively than liposomes embedded with the beta-glucosyl conjugate or vector-f
ree liposomes. A new lipid derivative of antitumor drug rubomycin (daunorub
icin). N-(rac-1,2-dioleoylglycero-3-oxalyl)rubomycin (RubDG) has been synth
esized. Liposomes loaded with RubDG and equipped with galactosyl vector sho
wed higher cytotoxic activity in vitro against HL-60 cells than analogous u
nvectored liposomes or liposomes bearing glycosyl conjugate.