Chromatography of functionalized liposomes and their components.
The antitumour drug 1-beta-D-arabinofuranosylcytosine (ara C) was acylated by means of oleic acid anhydride, resulting in the prodrug N4-oleoyl-ara C. Together with a lipophilic biotin derivative, this lipophilic prodrug was incorporated into the bilayer membrane of unilamellar liposomes prepared by means of the detergent dialysis method. On addition of these biotinylated prodrug-liposomes to an excess of avidin, biotin residues were complexed with avidin. The unreacted avidin was removed by chromatography on the Ultrogel AcA-22 column. The prodrug-liposome-avidin complex was coupled to biotinylated monoclonal antibodies through the free binding sites of the immobilized avidin. Unreacted antibodies were removed by chromatography on an Ultrogel AcA-22 column. In vitro, the liposome-antibody complexes selectively bound to cells which were recognized by the monoclonal antibodies linked to the liposomes. For this reason, a promising strategy towards a specific chemotherapy of cancer is expected.
Schott
H
H
Institut für Organische Chemie, Universität Tübingen, F.R.G.
Leitner
B
B
Schwendener
R A
RA
Hengartner
H
H
D001360:Avidin / Q000032:analysis; D001710:Biotin / Q000032:analysis; D002460:Cell Line; D003561:Cytarabine / Q000032:analysis* / Q000627:therapeutic use; D006801:Humans; D007074:Immunoglobulin G / Q000032:analysis; D008081:Liposomes / Q000008:administration & dosage / Q000032:analysis*; D011355:Prodrugs / Q000032:analysis; D011863:Radioimmunoassay
D007074:Immunoglobulin G; D008081:Liposomes; D011355:Prodrugs; D003561:Cytarabine; D001360:Avidin; D001710:Biotin