Co-delivery of Cu(I) chelator and chemotherapeutics as a new strategy for tumor theranostic.

Chelating Cu from tumors has been verified as an effective and promising strategy for cancer therapy through antiangiogenesis. However, systematic removal Cu by injecting with Cu chelators will result unavoidable side effects, since Cu is indispensable to the body. In this work, a micelle targeting to tumors' newborn vessels based on a polypeptide was developed to co-load DOX and Probe X, which can go through an "OFF-to-ON" procedure to report the Cu+-capture events in vivo in a real-time way by giving near infrared (NIR) fluorescence and photoacoustic signal. By co-delivering antiangiogenesis and chemotherapeutic reagents, the tumor can be significantly suppressed, meanwhile with a low systematic toxicity. Hopefully, this work can offer new insights in designing sophisticated antitumor strategy. Unlabelled Image • A theranostic specific Cu+ chelator was proposed. • Targeting micelle co-loaded with Cu+-chelator and chemotherapeutic reagents was fabricated. • Antiangiogenesis and tumor's oxygen saturation reduction were reduced. • Fine antitumor efficacy was achieved with low side effect. [ABSTRACT FROM AUTHOR]