High-density lipoproteins (HDLs) are the smallest lipoprotein with the highest level of protein in their surface. The main role of HDLs are reverse transport of cholesterol from peripheral tissues to the liver. More recently, HDLs have been considered as a new drug delivery system because of their small size, proper surface properties, long circulation time, biocompatibility, biodegradability, and low immune stimulation. Delivery of anticancer drug to the tumor tissue is a major obstacle against successful chemotherapy, which is because of the toxicity and poor aqueous solubility of these drugs. Loading chemotherapeutic drugs in the lipid core of HDLs can overcome the aforementioned problems and increase the efficiency of drug delivery. In this review, we discuss the use of HDLs particles in drug delivery to the tumor tissue and explain some barriers and limitations that exist in the use of HDLs as an ideal delivery vehicle.
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