The invention discloses a pH-responsive
polyethylene glycol-
anticarcinogen conjugate, and a synthetic method and application thereof. After
anticarcinogen molecules and
polyethylene glycol are covalently linked through pH-sensitive phenylimide linkage, the conjugate is formed, wherein,
anticarcinogen can be
doxorubicin,
epirubicin,
daunorubicin, demethoxydaunorubicin or hydrochlorides of the above-mentioned anticarcinogens. The phenylimide linkage is stable under the condition of a normal physiological pH value but undergoes
hydrolysis under the condition of a slightly acidic pH value, e.g., a
solid tumor
cell external pH value and a
cell endosome and
lysosome pH value; that is, the phenylimide linkage is sensitive to changes of pH values in a range of 7.4 to 4.5 or to below 4.5. The
polyethylene glycol-anticarcinogen conjugate has amphiphilic nature and can form nanometer-scale
micelle in a
saline solution through self-
assembly; the
micelle can be used as a
drug carrier to carry hydrophobic drugs and form a nanometer
micelle preparation cladded with drugs, thereby realizing
synergy therapy of a plurality of drugs.