In the last two decades, dendrimers have proven their capabilities in drug delivery, physical stabilization of the drug, solubility enhancement of the poorly soluble drugs and gene delivery. Several key features of dendrimers such as excellent control over molecular structure, nanoscopic size, availability of multiple functional groups at the periphery and narrow polydispersity index distinguish them as a superior choice over available polymers. The diversity of bio-actives loaded in dendrimers due to covalent and non-covalent interactions, such as hydrogen bonding and hydrophobic interaction contribute to the physical forces for binding of bioactives. The key advantage of drug-loaded dendrimers is the delayed and sustained-release of bioactives because of the encapsulation of the drug in the hydrophobic cavities of the dendrimer that acts as a sink to retain the drug molecules for extended duration. Because of these features researchers are particularly excited about the potential application of dendrimers as a versatile carrier for drug delivery. Collectively, this review focuses on detailed note on the delivery and improved solubility of poorly soluble anti-cardiovascular bioactives, nitric oxide (NO) donor for anti-thrombosis, gene delivery and delivery of receptor agonists for cardio-protective action of the receptors using dendrimers.