A
solid phase synthesis method for preparing
peptide-spacer-lipid conjugates, the
peptide-spacer-lipid conjugates synthesized by the method, and liposomes containing the
peptide-spacer-lipid conjugates. The present invention provides a convenient
solid phase synthesis method for preparing peptide-spacer-lipid conjugates and provides various linkage groups (such as
amide group) for conjugating peptide, spacer and lipid, wherein the spacer may comprise PEG. Several advantages can be achieved, such as the synthetic procedure can be simplified, the synthesis process can be set to
automation, the purification is easier in each
reaction step, and the product losses can be reduced to minimal during synthesis. The present synthesis method is suitable for preparing a wide range of peptide-spacer-lipid conjugates, provides
a peptide-spacer-lipid conjugate prepared by the
solid phase synthesis method of the present invention, which can be incorporated into a
liposome as the targeting
moiety for liposomal
drug delivery to specific cells, and provides a targeting
liposome containing the present peptide-spacer-lipid conjugate.