Low-density lipoprotein (LDL) is a small lipoprotein that plays a vital role in controlling lipid metabolism. LDL has a delicate nanostructure with unique physicochemical properties: superior payload capacity, long residence time in circulation, excellent biocompatibility, smaller size, and natural targeting. In recent decades, the superiority and feasibility of LDL particles as targeted delivery carriers have attracted much attention. In this review, we introduce the structure, composition, advantages, defects, and reconstruction of LDL delivery systems, summarize their research status and progress in targeted diagnosis and therapy, and finally look forward to the clinical application of LDL as an effective delivery vehicle.