Low side-effect and heat-shock protein-inhibited chemo-phototherapy nanoplatform via co-assembling strategy of biotin-tailored IR780 and quercetin

Abstract The side effects of anticancer drugs and tumor tolerance from heat shock protein expression are still a bottleneck for the current chemo-phototherapy. Although quercetin (Qu) is a naturally low-side effect anticancer drug and heat shock protein inhibitor for tailoring phototherapy, it is largely restricted by poor water solubility. Moreover, the near-infrared dye IR780-iodide (IR780), as a promising phototherapy agent, is also restricted from clinical applications due to its poor water solubility. Herein, we rationally designed a robust low side-effect and heat-shock protein-inhibited chemo-phototherapy nanoplatform via co-assembly of biotin-tailored IR780 (B780) and quercetin, defined as B780/Qu nanoparticles (B780/Qu NPs), which efficiently solved the poor water solubility of both IR780 and Qu. Moreover, the B780 endowed B780/Qu NPs with superior active tumor-targeted property and pH-responsive drug delivery. Thanks to the combination of chemo-phototherapy, the B780/Qu NPs with near infrared (NIR) laser irradiation exhibited excellent anti-tumor efficacy. Therefore, our B780/Qu NPs are very promising as an efficient low side-effect and heat-shock protein-inhibited chemo-phototherapy nanoplatform against tumors.