Edelfosine lipid nanosystems overcome drug resistance in leukemic cell lines

Although current therapies have improved leukemia survival rates, adverse drug effects and relapse are frequent. Encapsulation of edelfosine (ET) in lipid nanoparticles (LNs) improves its oral bioavailability and decreases its toxicity. Here we evaluated the efficacy of ET-LN in myeloid leukemia cell lines. Drug-loaded LN were as effective as free ET in sensitive leukemia cell lines. Moreover, the encapsulated drug overcame the resistance of the K562 cell line to the drug. LN containing ET might be used as a promising drug delivery system in leukemia due to their capacity to overcome the in vivo pitfalls of the free drug and their efficacy in vitro in leukemia cell lines.

► The antitumor effect of free and encapsulated edelfosine is comparable in leukemia cells sensitive to the action of the drug.
► Edelfosine loaded lipid nanoparticles overcome the resistance of K562 cells to the free drug.
► Lipid nanoparticles might be triggering caspase-independent apoptotic pathways in resistant leukemia cells.