<p>Bioactive compounds have been utilised for their therapeutic effects in various biomedical applications for a long time. The growing global emphasis on health has driven a significant increase in demand for these compounds in recent years. However, using them in the conventional formats does not achieve the required bioavailability for the desired effects. Thus, there is a growing need for nanonizing bioactive compounds, as this significantly increases the surface area-to-volume ratio and enhances their pharmacological activities. This review aims to provide a comprehensive overview of the various techniques that can be used to prepare nanonized formulations of such compounds. This ranges from widely used techniques, such as wet-media milling and electrospinning, to relatively newer techniques, including supercritical fluid technology. Additionally, we have covered the various encapsulation layers that can be employed to protect these nanoformulations and facilitate the delivery of the nanomaterials. Delivery of such bioactive compounds can be achieved through invasive and non-invasive methods. After entering these compounds into the biological system, they are taken up by the cells via active or passive transport. However, despite these advancements, many challenges remain during the preparation of these formulations. During the preparation of nanomaterials, it thus becomes essential to address these challenges and carefully evaluate the different parameters before scaling up the manufacturing process.</p> Graphical Abstract <p></p>