Antitumor activity of high-density lipoproteins and their use for targeted drug delivery.

Blood levels of high-density lipoprotein (HDL) are significantly inversely correlated with the risk of numerous malignancies and overall mortality in most tumor types. This review focuses on the antitumor role of HDL and its main protein component, apolipoprotein A-I (apoA-I). The association of HDL/apoA-I with various cancer types and the probable mechanisms of their antitumor action, including cholesterol removal from tumor cells, modulation of the tumor microenvironment, and involvement in the regulation of oncogenic signaling pathways, are discussed. The identified high expression of the SR-B1 receptor in tumor cells supports the use of HDL and its synthetic analogs (apoA-I mimetics) as a platform for the targeted delivery of antitumor agents. Using various tumor models, it has been demonstrated that the use of these plasma components for targeted drug delivery enhanced their antitumor effect and reduced side effects.