Objective: To investigate the feasibility and effectiveness of low density lipoprotein (LDL) particles as a carrier of a lipophilic anthracycline drug aclarubicin (ACR) for targeting delivery to an acute monocytic leukemia cell line THP-1.
Methods: LDL-ACR complex was prepared by incubating LDL with ACR. The intracellular ACR content was assayed fluorometrically. Cytotoxicity was studied by cell protein measurement and 3H-TdR incorporation test.
Results: Intracellular accumulation of LDL-ACR was reduced when THP-1 cells were incubated in the presence of native LDL, but methylated LDL had no effect on the cellular LDL-ACR accumulation. The LDL-ACR complex caused a greater inhibition of the growth of THP-1 cells than that of normal bone marrow nucleated cells. The cellular accumulation of LDL-ACR complex was much more than that of free ACR. The 3H-TdR incorporation test showed that the complex was more effective in the inhibition of DNA synthesis than that of the free drug.
Conclusion: The potency of ACR to tumor cells increased and its toxicity to normal cells decreased when LDL was used as a carrier.