The invention discloses a preparation method and application of a dual-targeting
hepatocellular carcinoma nano-
drug, and belongs to the field of biological medicines. According to the invention, a double-targeting target molecule with
myeloperoxidase-
asialoglycoprotein receptor double-targeting property is synthesized, and the double-targeting target molecule is modified on a covalent organic nano molecule COF-366 through pi-pi stacking, wherein the covalent organic nano molecule COF-366 is coated with
chemotherapeutic drugs sorafenib and
chloroquine and has photodynamic characteristics. The obtained nano-
drug can be gradually delivered to hepatocytes under the guidance of double-targeting molecules,
drug release is started in acidity of a tumor acidic microenvironment, the synergistic
treatment effect of
photodynamic therapy and
chemotherapy can be played, and the synergistic effect causes tumor injury, so that the
inflammation targeting of the nano-drug is further enhanced. The nano-drug has good stability and
biological safety, in-vivo behavior tracing and
treatment efficacy evaluation are carried out in subcutaneous
solid tumor and in-situ tumor mouse models, and the nano-drug is expected to play a huge role in clinical application.