Selective drug delivery at the potential target with mapping for health therapy of every individual is becoming biggest challenges over traditional drug delivery. With the advent of nanotechnology fabrication of nanomaterials of suitable shape and size, solubility, material compositions and surface chemistry offer increased effectiveness in target specific drug supply while decreasing nonspecific side effects. Fullerenes (parent and derivatives of C60, higher C70, C74, C76, C78, C84, etc.,) have been investigated in biomedical fields. In delivery of drug fullerenes show huge potential as nano-vehicles due to diverse exterior chemical characteristics (covalent and non-covalent), endohedral atoms/ions encapsulation within the closed carbon cages and lower nanoscale dimensions, along with the reproducible chemistry of molecules. In the present chapter the possibilities, challenges and limitations of fullerene derived materials for delivery of nucleic acid and peptide delivery, as well as topical drug, infectious diseases drug, anticancer drug, lung-specific drug, brain drug and ocular drug are discussed.