Hence, this novel tumor targeting DDS may have several functions for prostate tumor therapy: first of all, the Chol–PEG–DUP1 micelles could provide prolonged drug effects because of their sustained release characteristic, and protect the encapsulated agent from enzymatic degradation; secondly, the nanoscale size of the micelles would improve the targeting efficiency and therapeutic activity of small molecular antitumor drug via EPR effect; finally, the DUP1 fragment could specifically target to the PSMA-negative tumor cells, resulting in special uptake of antitumor drugs. Here, FOLH1 is linked to prostate neoplasm.