Cardiovascular disease (CVD) is one of the most important diseases threatening human health worldwide. Atherosclerosis (AS) is the common pathological change of a broad spectrum of lethal CVDs such as myocardial infarction and stroke. Pharmaceutical treatment based on early diagnosis of vulnerable plaques is the most effective strategy for the management of AS. Unfortunately

accurate diagnosis and effective therapy of AS by traditional reagents have been largely limited due to critical issues such as low resolution/sensitivity

low drug concentration at diseased sites

and severe side effects. Rapid development in nanomedicine has offered great promise for the targeted therapy of AS. This review summarized the state-of-the-art of nanosystems for molecular imaging and targeted therapy of AS. Future development in this field was also discussed.