In this era of nanoscience, advances of nanotechnology have led to the creation of new generations of nanostructures, each characterized by their explorative utilization in various types of applications in biomedicine and bio-engineering. These applications are expected to significantly improve the diagnosis and therapeutic aspects of many diseases. The materials have been explored and reported as components of biosensors and as very efficient drug delivery platform. Though, few nano-materials have been reported to be used in clinical medicine, but not coherently effective. This could be because of nano-toxicity which is a potential limitation for its use in biological system. A brief description on the development of nanostructure for biomedical application over the years in terms of new materials and understanding of their interaction with the body, may lead to better biocompatible nanostructures.