This review throws light upon the functionalization of DNA amphiphiles which upon self‐assembly give rise to nanostructures of varied morphology and novelty. Such nanostructures comprising of micelles, vesicles, sheets or ribbons find a multitude of applications in medical field, specially in drug delivery. Emphasis has been laid upon the self‐assembly process of DNA based amphiphiles which prove excellent drug carriers by making use of the unique structural features of DNA. Further insights may also aid in developing modified nanostructures based on DNA out of subsequent derivatization. [ABSTRACT FROM AUTHOR]