The present application belongs to the technical field of
medicine, and mainly relates to a conjugate of an ApoA1 short
peptide and a
tubulin inhibitor and a self-assembled nano preparation thereof, wherein the ApoA1 short
peptide and the
tubulin inhibitor are coupled through a
linker. The self-assembled nano preparation comprises the following components: 1-100 parts of the conjugate of the ApoA1 short
peptide and the
tubulin inhibitor; 1-100 parts of
phospholipid; 1-100 parts of
cholesteryl ester; and 1-100 parts of water for injection or
phosphate buffer. The conjugate of the ApoA1 short peptide and the tubulin inhibitor improves the targeting of the tubulin inhibitor on
tumor cells and reduces the toxic side effects of the tubulin inhibitor; the self-assembled nano preparation has the advantages of low cost, few operation steps, simple process, good
repeatability, can realize efficient
mass production at low cost, and is conducive to storage and
drug administration.