Lack of selectivity, toxic side effects and multidrug resistance represent major limitations for chemotherapy treatment against cancer. The non-specific targeting of the chemotherapeutic agents leads to the rapid damage of normal cells. This could be significantly reduced through folate mediated nano-therapeutics which aimed to target cancerous cells. In this study, a folate decorated carboplatin loaded albumin nanoparticles was prepared aiming to successful active targeting of folate receptor overexpressing cancer cells which inconsequence decrease side effects and increase efficacy of carboplatin. The formulation was prepared using desolvation technique, glutaraldehyde as a cross linker, bovine serum albumin as a nanocarrier and folic acid as a targeting ligand. Physical characterization of the formulation was carried out as per of particle size, zeta potential and poly dispersity index (PDI). Results showed (267.29 nm) particles with (- 30.4 mV) potential and (0.069) PDI which confirmed a successful preparation of the formulation. For evaluation of the cytotoxic effect of the suggested formulation against the free form of the Carboplatin, an MTT cytotoxic assay was performed on folate receptor overexpressing cell lines (Caco2, PC3) a human colon cancer cell line and a prostate cancer cell line respectively. Results revealed higher significant efficacy represented by lower the half maximal Inhibitory concentration (IC50) values which gives a new hope for using carboplatin in a more effective and safe way in treatment after further clinical investigations.