The application discloses a method for accelerating bio-orthogonal
catalysis in situ of tumors by using acid / reduction-sensitive
polymer vesicles, and the method comprises the following steps: introducing hydrophilic / hydrophobic precursors and Cu 2+ into the
polymer vesicles, and then injecting the
polymer vesicles into the body of a patient. The polymer vesicles are separated into an inner aqueous phase, a hydrophobic layer and a hydrophilic surface, so that side reactions and early reactions between the precursors and the
divalent copper can be effectively avoided. The polymer vesicles are composed of linear copolymers of
hyaluronic acid-bisulfur bond-poly-
caprolactone with specific molecular weights, and the structure of the polymer vesicles is stable under normal physiological environment; under the acid / reduction environment in
tumor cells, the membrane of the vesicles is degraded to cause perforation, so that the hydrophilic precursors are preferentially released from the inner aqueous phase to the outside of the membrane, chelate with the Cu + on the
surface layer, and stabilize the structure of the Cu + and shorten the distance between the
azide group and the catalytic center, so as to improve the
catalytic efficiency. The co-delivery of the three substances (
Azide,
Alkyne and Cu 2+ ) and the improved
catalytic efficiency after the
chelation of the precursors and
copper significantly reduce the dosage of intravenous injection, so that the nano-
vesicle therapy has high efficiency and
biological safety.