The invention belongs to the technical field of high-
molecular medicine, and particularly relates to an antitumor
medicine conjugate with
folic acid receptor-mediated and photoresponsive functions and a preparation method thereof. The preparation method comprises the following steps: firstly, performing amidation reaction on
folic acid and amino polyethyleneglycol; then performing amidation reaction on a product obtained in the former step and 7-ethyloic-4-
hydroxymethyl coumarin to obtain a polyethyleneglycol flexible chain with a
folic acid receptor targeting function and a photoresponse group; finally enabling the polyethyleneglycol flexible chain to be coupled with an antitumor
medicine containing amino with an ester
activation method to obtain the antitumor
medicine conjugate with the folic acid
receptor-mediated and photoresponsive functions. The conjugate prepared by the invention can target a tumor
cell through a folic acid receptor-mediated function, and enters the
cell via the
endocytosis to accelerate the accumulation speed of the medicine in the tumor
cell; when being irradiated by
ultraviolet light with a specific
wavelength or near-
infrared light, the conjugate is photolyzed to release original medicine, and the medicine quickly reaches the effective concentration, so that controllable 'time / space' treatment is realized; in addition, the method provides a simple and effective manner for preparing target-controllable photoresponsive high-
molecular medicine conjugates.