A carrier-free anti-inflammatory platinum (II) self-delivered nanoprodrug for enhanced breast cancer therapy

Cisplatin is one of the most used first-line anticancer drugs for various solid tumor therapies. However, cisplatin-based chemotherapy can induce cells to secrete excessive prostaglandin E2 (PGE2) catalyzed by cyclooxygenase-2 (COX-2), which, in turn, counteracts its chemotherapeutic effect and further accelerates metastasis. Here, we report a carrier-free self-delivered nanoprodrug based on platinum (II) coordination bonding coupled with tolfenamic acid (Tolf) (named Tolfplatin). Tolfplatin spontaneously assemble into uniformly sized nanoparticles (NPs) high drug-loading capacity. Compared cisplatin, NPs facilitate cellular uptake, significantly decrease PGE2 secretion COX-2 inhibition, which downregulate tumorous anti-apoptotic metastasis-associated proteins, thereby efficiently inducing apoptotic cell death inhibit metastasis vitro vivo. Therefore, as nanoprodrug, are promising anti-tumoral agents proliferation enriching function promoting anti-tumor activity cisplatin.