Abstract: Monocytes/macrophages play an important role in the inflammatory process of cardiovascular disease (atherosclerosis, myocardial ischemia-reperfusion). When inflammation occurs, monocytes are recruited into the inflammatory tissue through the interaction of integrins and cell adhesion molecules (CAMs), targeting the inflammatory sites. Using macrophages directly as drug carriers, engineering biomimetic nanoparticles with macrophage cell membrane proteins, encapsulating nanoparticles with macrophage membranes, or using macrophage exosomes as drug carriers to simulate mononuclear/macrophage characteristics for targeted drug delivery, are all of great value in the diagnosis and treatment of cardiovascular diseases. This paper reviews the progress macrophage-based drug delivery system in cardiovascular disease.