Nanoscale materials (NSMs) are gaining attention due to their small size and unique physiochemical properties. Different approaches are used for the synthesis of NSMs. NSMs cannot be visualized by ordinary instruments. Instruments with high resolution are required for their characterisation. NSMs offer enhanced activity and specificity to encapsulate drugs. NSM are used as vehicles for site specific delivery of drugs inside the body. In this chapter, approaches for the synthesis of NSMs, and characterisation techniques for NSMs like SEM, TEM, AFM, DLS, XRD, and FTIR have been explained briefly. In addition, this chapter also covers zero dimensional one dimensional, two dimensional and three dimensional NSMs briefly. Detailed information about approaches of targeted delivery like passive and active have been covered in this chapter. NSMs like polymeric nanoparticles, metallic nanoparticles, liposomes, quantum dots, polymeric micelles, carbon nanotubes, dendrimers, and magnetic nanoparticles used in targeted drug delivery have also been explained in this chapter.