Cardiovascular Diseases (CVDs) pose a significant global health threat, with rising mortality rates attributed to factors like diabetes, obesity, and an aging population. This paper explores the evolving landscape of micro and nanoscale Drug Delivery Systems (DDSs) to enhance cardiovascular treatment efficacy. Various nanoagents, both organic (e.g., liposomes, dendrimers, polymeric nanoparticles) and inorganic (e.g., carbon nanotubes, silver nanoparticles, iron oxide nanoparticles), are classified and examined. The advantages, limitations, and preparation techniques of nanoagents are discussed, emphasizing their potential in targeted delivery, multifunctionality, minimal side effects, and enhanced efficiency. The anatomical details of the heart, layers of heart walls, and heart functions are presented for contextual understanding. The application of nanoagents in treating specific cardiovascular conditions, such as atherosclerosis, hypertension, myocardial infarction, and coronary artery disease, is thoroughly explored. Evaluation methods for nanoagents, including size and morphology analysis, surface charge determination, and molecular weight evaluation, are outlined. This paper concludes by emphasizing the promising role of nano-drug delivery systems in addressing CVD challenges, urging collaborative efforts for successful translational medicine implementation. Future research directions are proposed, highlighting the potential of peptides, antibodies, and selective nanodelivery systems in advancing cardiovascular care. Challenges like pharmaceutical scale-up, regulatory requirements, and patient preparation are acknowledged, underscoring the need for interdisciplinary collaboration to propel nanocardio medicine into clinical practice.