Abstract

Doxorubicin (DOX) has been extensively used in the clinic to treat malignant tumors such as leukemias and Hodgkin’s lymphoma. However, the severe cardiotoxicity associated with the use of DOX requests the development of alternative and efficient pharmaceutical formulations. The PEGylated liposome of DOX can significantly reduce the cardiotoxicity but still lacks the active targeting towards cancer cells. Modification of liposomal DOX with active ligands would then be a rational approach to enhance the transportation of the toxin into tumor cells. Currently used targeting ligands include antibodies, proteins, small molecules, and peptides. By virtue of the advantages such as easy preparation, lower cost, and elevated resistance to enzymatic degradation, peptides are attracting a significant amount of interest as active targeting ligands for pharmaceutics. In this paper, we will briefly discuss the application of peptide ligands for the improvement of the therapeutic efficacy of liposomal DOX.

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