Context: In recent years, nanotechnology has opened up several new avenues of extraordinary biomedical potential by modulating metals into their nanosize leading to significant improvement in their chemical, physical and optical properties. Introduction: The advanced fabrication techniques have been exploited to modify nanostructured materials. The functionalized nanoscaled fibers display various exclusive features like high surface area to volume ratio, tunable porosity and maneuverable surface with desired function. Additionally, surface modification stabilizes nanoparticles against agglomeration, provides compatibility with other phase and presents them in a highly self-organized structure with desired properties. This study gives an overview of nanoparticles which have been significantly improved by fabrication technology to make them suitable for extensive biomedical applications. The strategies involved introduction of functionalities like grafting of an already functionalized ligand on the surface of nanoparticle, exchanging part/whole of the existing ligands on its surface or grafting of a ligand on a nanoparticle followed by modification via organic chemical reactions have also been reviewed. Applications of various surface modified carbon nanotubes and silica based nanoparticles in biomedical/biotechnological sectors are also outlined. Conclusion: Since purity, dispersity and stability of multifunctional nanoparticles is highly important in a physiological environment for in vivo biomedical applications, the newly developed surface modified nanoconjugates can be used for cancer cell imaging, tumor ablation and drug delivery.