Cardiovascular diseases, principally atherosclerosis, stroke or myocardial infarction, are a significant public health problem worldwide. Attempts to prevent cardiovascular diseases often imply modifications and improvement of causative risk factors such as obesity, elevated blood pressure, an unfavorable lipid profile or insulin resistance. Chitosan and its derivatives are considered to promote diverse activities, including antihypertensive, antioxidant, antiinflammatory, anticoagulant, antitumor and anticancer, applications in drug delivery and acceleration of calcium and iron absorption, antimicrobial, hypocholesterolemic and antidiabetic effects. By modulating and improving physiological functions, chitosan and its derivatives may provide novel therapeutic applications for the prevention or treatment of chronic diseases. This review focuses on chitosan and its derivatives with biological activities relevant to cardiovascular health.