AbstractThe currently used drug carriers for vascular drug delivery are reviewed. The human vascular system possesses unique physiological features that can be exploited for enhanced and effective targeted drug delivery. Although the thin layer of endothelial cells (EC) lines the interior surface of blood vessels forming an interface between circulating blood in the lumen and the tissue beyond the vessel wall, it can also function as a target for drugs to EC in different vascular areas. ECs overexpress specific cell‐surface molecules under various pathological conditions (tumor neovasculature, inflammation, oxidative stress, and thrombosis), which are absent or barely detectable in established normal blood vessels. By coupling unique endothelial surface markers, such as antibodies, specific peptides, and growth factors to a variety of drug carriers, effective active vascular‐targeted drug delivery systems can be achieved. This review focuses on the recent advances and strategies for effective targeted vascular drug delivery using a variety of drug‐loaded carriers along with new targeting approaches that can be used in the design and optimization of such carriers. © 2011 IUBMB IUBMB Life, 2011