Anticancer platinum (Pt) complexes have long been pronounced as one of the biggest success stories in the history of medicinal inorganic chemistry. Yet there still remains the hunt for the “magic bullet” which can satiate the requisites of an effective chemotherapeutic drug formulation. Pt(IV) complexes are kinetically more inert that the Pt(II) congeners and offer the opportunity to append additional functional groups/ligands for prodrug activation, tumor targeting or drug delivery. The ultimate aim for functionalization is to enhance the tumor selective action and attenuate systemic toxicity of the drugs. Moreover, increase in cellular accumulation to surmount the resistance of the tumor against the drugs is also of paramount importance in drug development and discovery. In this review, we will address some of the attempts in our lab to develop Pt(IV) prodrugs that can be activated and their targeted delivery using robust nanotechnology platforms.