Nanodrugs need a completely characterization by both chemically and biological point of view. As nanoparticles have evolved as multi-functional systems combining different custom anchorages, their pharmacological involvements require more comprehensive analysis. In this work, we present the design and synthesis of novel iron-NPs conjugated with a cisplatin derivate and their biological evaluation by quantitative proteomics approches. To decipher detailed insights related to the NP interactions with environment (as protein corona) and pharmacodynamics functionalities of the nanodrugs conjugates, LC-MS/MS analysis was perform to stablish protein profile. Biocompatibility and animal model provided complete insights of the potential of multifunctional iron NPs.