Owing to faulty DNA damage repair system, triple negative breast cancer (TNBC) exhibits high susceptibility towards DNA damaging drugs such as platinum compounds e.g., oxaliplatin. Nevertheless, the clinical utility of oxaliplatin (OXA) has been constrained due to chemoresistance and chronic toxicities. Hence, to confer systemic inertness, tumor specific delivery, and multifaceted action, a octahedral OXA-CBL prodrug was synthesized using chlorambucil (CBL) as an axial ligand. The combination of OXA and CBL exhibited synergistic anti-cancer action in TNBC cell lines. Further, to potentiate the cellular internalization, targeting efficiency, and in-vivo performance, the synthesized prodrug was loaded into bovine serum albumin nanoparticles (OXA-CBL/BSA-NPs). The prepared nanoparticles had optimal particle size <
200 nm and high drug loading (∼ 5.863 ± 0.16%). As relative to free conjugate, the nanoparticles exhibited amplified cellular internalization and reduced the IC