The application of nanotechnology to medical purposes is termed as nanomedicine. Nanomedicine involves the use of nanomaterials for the diagnosis, monitoring, control, prevention & treatment of the diseases. Nanomaterials are either natural, incidental, or manufactured material comprising particles, either in an unbound state or as an aggregate wherein one or more external dimensions is in the size range of 1–100 nm for ≥50% of the particles, according to the number size distribution. The pharmaceutical manufacturing of nanomaterials involves two different approaches: Top down and bottom down. The top-down approach involves the breakdown of a bulk material into a smaller one or smaller pieces by mechanical or chemical energy. On the contrary, the bottom down approach starts with atomic or molecular species allowing the precursor particles to increase in size through chemical reaction. Nanomaterials can be applied in nanomedicine for medical purposes in three different areas: diagnosis (nanodiagnosis), controlled drug delivery (nano therapy), & regenerative medicine. Nanomedicine is holding promising changes in clinical practice by the introduction of novel medicines for both diagnosis & treatment, having enabled to address unmet medical needs, by (a) integrating effective molecules that otherwise could not be used because of their high toxicity, (b) exploiting multiple mechanisms of action, (c) maximizing efficacy by increasing bioavailability & reducing dose and toxicity, (d) providing drug targeting, controlled & site specific release, favoring a preferential distribution within the body, e.g., in areas with cancer lesions & improved transport across biological barriers. This is a result of intrinsic properties of nanomaterials that have brought many advantages in the pharmaceutical development. Due to their small size, nanomaterials have a high specific surface area in relation to the volume. Consequently, the particle surface energy is increased, making the nanomaterials much more reactive. Nanomaterials tend to adsorb biomolecules, e.g., proteins, lipids etc. when in contact with the biological fluids. One of the most important interactions with the living matter relies on the plasma/serum biomolecule adsorption layer, known as “corona,” that forms on the surface of colloidal nanoparticles. Its composition depends upon the on the point of entry into the body and on the fluid that the nanoparticles come across with (e.g., blood, lung fluid, gastro-intestinal fluid, etc.). In addition, nanomaterials can be engineered to have different size, shape, chemical composition, and surface, making them able to interact with specific biological targets.