Abstract: In this study, octreotide targeting doxorubicin liposome(Dox@Oct-L)was prepared by modifying cholesterol with azide group to prepare azide-modified doxorubicin liposome(Dox@N₃-L), followed by click reaction on the vehicle surface with alkyne-modified octreotide. HPLC chromatographic determination showed that octreotide was successfully attached to drug loaded liposome. No significant effect of click modification on the drug loaded within liposome was detected, and the entrapment efficiency of Dox@Oct-L was 99. 8%. Dox@Oct-L showed improved in vitro anti-tumor activity against HepG2 cell when compared with Dox@N₃-L, demonstrating that Dox@Oct-L possessed targeting ability against HepG2 cell. Therefore, the click chemistry in modification of drug-loading carrier surface is gentle and efficient, providing the possibility to functional modification in drug-loading carrier surface convieniently.