There is a growing interest in nano-formulations of medicinal drugs for anti-bacterial, antiviral, antifungal, antiphrastic, and antioxidant drug delivery applications by researchers. Using nano-formulations, conventional drugs have enhanced properties and are targeted to specific sites of distribution. Some of the Nano-formulations gaining prominence in the pharmaceutical industry are hydrogels, Nanocrystals, polymeric nanoparticles, liposomes, nanoemulsions, and micelles. These metal nanoparticles (silver, gold, iron oxide, and others) and nanoemulsions cause protein damage and DNA damage and produce ROS (reactive oxygen species). Nanomaterials have found utilization in biomedical applications, spanning across metals, nonmetallic/inorganic materials, and biodegradable materials. Human cells exhibit toxicity (Titanium dioxide (TiO2) towards nanoparticles (NPs) due to the presence of synthetic chemicals as surface functional agents. Consequently, isolated nanoparticles alone can induce hepatotoxicity, skin sensitization, and damage. A focus on strategies such as coupling agents has been used in recent advancements aimed at reducing the toxicity of nano-formulations. These modified nanostructures provide safer and more efficient biomedical applications by reducing toxicity and enhancing effectiveness.