The invention discloses a nano aggregate as well as a preparation method and anti-
breast cancer application thereof. The nano aggregate comprises a
drug-
drug conjugate AI (formed by
dehydration condensation of ATRA and IRI), an anoxic
response type prodrug PAC (formed by
coupling of CPUL119 and PEG through an
azobenzene connecting bond), and a targeting molecule DT (DSPE-PEG2000-Try), wherein the
drug-drug conjugate AI is formed by
dehydration condensation of ATRA and IRI; the anoxic
response type prodrug PAC is formed by
coupling of CPUL119 and PEG through an
azobenzene connecting bond; the preparation method comprises the following steps: respectively dissolving AI, PAC and DT in an
organic solvent, dropwise adding an AI solution into deionized water, stirring for the first time, adding a PAC solution and a DT solution, and stirring again to obtain the nano aggregate. The nano aggregate disclosed by the invention has a uniform particle size of 90-130 nm and a high drug loading capacity (greater than 80%), stably exists in a physiological environment, and shows excellent
tumor targeted accumulation capacity; the
medicine is released through hypoxia / pH /
esterase triple response,
chemotherapy (IRI), differentiation therapy (ATRA) and
ferroptosis therapy (CPUL119) are coordinated, and the killing effect on
breast cancer cells and stem cells is remarkably enhanced.