Arsonoliposomes (ARSL) constitute a particular class of liposomes that incorporate arsonolipids (ARS) in their membranes. ARSL realize selective toxicity to cancer cells, thus being an important tool in the treatment of cancer. Folic Acid (FA) is widely used in targeted drug delivery, due to its high affinity for the folate receptors that are overexpressed in cancer cell membranes. The aim of our studies was to develop novel TNBC-targeted ARSL, by incorporating folic acid-conjugated PEG-lipid in their membrane and loading them with anticancer drug doxorubicin (DOX). ARSL incorporating 0.1 mol% of FA-PEG-lipid (folate-PEG-DSPE) were prepared and loaded with DOX, using the active loading protocol. They were characterized for their size distribution, zeta potential and drug entrapment efficiency (%). Their cytotoxic activity towards TNBC cell lines, particularly MDA-MB-231 (epithelial human breast cancer cells) and 4T1 (murine mammary carcinoma cells) was evaluated by the MTT-assay. Additionally MCF7 (Human breast cancer cells), and HEK-293 (Human embryonic kidney cells) were evaluated as control cells. The first results demonstrated enhanced toxicity of this novel type of ARSL towards cancer cells, which is particularly interesting and deserves further exploitation.