Background: The drug delivery system is revolutionized by nanoparticles, an essential component of nanotechnology, exhibiting an ultra-small size, large surface area to mass ratio, and high reactivity, different from bulk materials having the same composition. Various types of nanoparticles include liposomes, neosomes, micelles, carbon-based, etc. The most useful among them are carbon nanotubes because of their distinct optical, electrical, thermal, and mechanical properties and their architectures. Furthermore, the carbon nanotubes could either be single-walled or multiple-walled, based on the number of graphene sheets rolled. Like any other technique, these come with many limitations, including their tendency of hydrophobicity, insolubility, bundling together, low dispersibility, and, majorly toxicity. Objective: In this review, the main objective is to update the applications of functionalized carbon nanotubes as drug delivery systems in various therapies. Methods: Functionalization came into being to solve the mentioned disabilities. Functionalization could be covalent as well as non-covalent. As a result, functionalized carbon nanotubes have shown improvement in mentioned drawbacks. Conclusion: Now, the above-said functionalized carbon nanotubes have achieved bigger objectives with a better approach than conventional carbon nanotubes in the field of drug delivery systems.