Cytotoxic effect of a lipophilic alkylating agent after incorporation into low density lipoprotein or emulsions: studies in human leukemic cells.

The use of low density lipoprotein (LDL) as drug carrier in acute myeloblastic leukemia chemotherapy is attractive due to high LDL uptake by leukemic cells. Lipid-based formulations, such as liposomes or microemulsions are promising alternatives. In the current study, we incorporated N-trifluoroacetyl-adriamycin-14-valerate (AD32), a lipophilic derivative of daunorubicin (DNR), and WB4291, a lipophilic alkylating agent, into LDL or lipid microemulsions and evaluated their cytotoxic activities towards leukemic cell lines using as references DNR and melphalan.

Cellular association and cytotoxicity of anti-CD74-targeted lipid drug-carriers in B lymphoma cells.

The ability to selectively target anti-cancer drugs via specific ligands against antigens expressed on malignant cells could greatly improve the therapeutic indices of the drugs. In this paper an anti-CD74 antibody (Ab), LL1, was covalently attached to the surface of sterically stabilized lipid drug-carriers (emulsions and liposomes) by use of a PEG-based heterobifunctional coupling agent. Target cells internalize LL1 very fast and that was found to be true for the LL1-lipid drug-carrier complexes as well.