The invention provides a simple and rapid preparation method of a novel HER2 targeted nano-
drug maytansine (DM1). The preparation of the nano-
drug is realized by using carboxyl on a
side chain of
azide-terminated poly (L-
glutamic acid) (PLG) as a load
binding site. The preparation method comprises the following steps: firstly,
grafting N-(2-aminoethyl)
maleimide hydrochloride (Mal-C2H4-NH2-HCL) to carboxyl of PLG (Poly L-Glycol), and introducing a
maleimide group to form PLG-Mal; the preparation method comprises the following steps: preparing Fc-III-4
C peptide-PLG-Mal (Fc-PLG-Mal) by virtue of an amidation reaction between carboxyl and amino of the Fc-III-4
C peptide, and then carrying out
thiol-
maleimide click
chemical reaction on a maleimide group and sulfydryl of DM1, so as to obtain the Fc-PLG-DM1. Finally, the HER2
antibody and the Fc-PLG-DM1 are mixed in water by utilizing the high affinity effect between the Fc-III-4
C peptide and the Fc segment of the HER2
antibody, so that the HER2-PLG-DM1 can be obtained, and the HER2-PLG-DM1 has a remarkable
tumor inhibition effect in animal experiments. The successful development of the HER2-PLG-DM1 proves the potential of the method in the design and development of functional nano-drugs in the future.