Bio‐inspired Coordination‐Assembled Nanoparticles for Enhanced Drug Delivery of Tumor Chemotherapeutics

Owing to low drug delivery efficiency (<1%), nanoparticle-based drug delivery system remains great challenge for efficient tumor chemotherapeutics. In this study, bioinspired coordination-assembled nanoparticles (CuET@HR-Pro) are fabricated by programming the assembly of three types of functional biomolecules (heparin, cRGD, and protamine) and the anti-cancer drug (CuET). The nanoparticles enhanced the drug delivery efficiency of an intravenous injective dose to up to 6.9%, and thereby significantly improving the anti-tumor efficacy of the drug. The CuET@HR-Pro is fabricated by patching coordination-assembled CuET@heparin-cRGD (CuET@HR) nanoparticles onto the surface of protamine (Pro) nanoparticles in 10% fetal bovine serum. The enhanced drug delivery capacity of the obtained CuET@HR-Pro nanoparticles is due to their improved stability (anti-complement activation, anti-protein adhesion), targeting capacity, and cell penetration ability. As expected, CuET@HR-Pro exhibited a superior inhibitory effect on orthotopic ovarian cancer in nude mice. The proposed strategy provides an alternative for achieving highly efficient drug delivery and tumor therapy.