Nanotechnology can be defined as the science and engineering involved in the design, synthesis, characterization, and application of materials and devices whose smallest functional organization in at least one dimension is on the nanometer scale or one billionth of a meter. One of the great promises of nanotechnology is the application to biology and medicine. In medicine, the cardiovascular field is one of the most technically advanced disciplines. Engineering achievements have helped us develop novel diagnostic and therapeutic technologies that provide safe and efficient solutions for cardiovascular patients. In spite of such progress, cardiovascular disease remains a major cause of death, morbidity, and disability in Occidental and Oriental societies. To address this formidable public health issue, substantial advances will be needed, and in particular, some important technological hurdles need to be overcome. The burgeoning new field of nanotechnology might open up a brand new approach in addressing some of these technical challenges. In fact, recent rapid advances in nanotechnology and nanoscience offer a wealth of new opportunities for diagnosis, prevention, and therapy of cardiovascular diseases, especially atherosclerosis. The aim of this article is to provide a brief survey at promising, important targets for nanotechnology in atherosclerosis. We review some of the main advances in the field of nanotechnology over the past few years, explore the prospects of clinical application in atherosclerosis, and discuss the concepts, issues, approaches, and challenges, with the goal of triggering the interest of biomedical scientists in the field of extremely tiny world.