Nanoscale drug delivery system (DDS) provides a new administration method in treatment of cardiovascular diseases. The system shows enormous advantages in solving current problems of oral medication, targeting, and long-term release, etc. New DDS formulation methods based on traditional forms of drug delivery nanoparticles are updated and reported. These methods include drug-loading fibers, drug-coated stent, cationic liposome, amphiphilic hyperbranched polymers and so on. In addition, DDS is improving towards multi-function by using magnetic resonance imaging, ultrasonic imaging and fluorescence to combine diagnosis and therapy in one device. However, the problems of  iocompatibility and cytotoxicity in DDS are to be resolved. This article reviews current developments of nanoscale drug delivery system specifically targeting cardiovascular diseases.