Antibody or ligand-mediated targeting of liposomal anticancer drugs to antigens expressed selectively or over-expressed on tumor cells is increasingly being recognized as an effective strategy for increasing the therapeutic indices of anticancer drugs. This review summarizes some recent advances in the field of ligand-targeted liposomes (LTLs) for the delivery of anticancer drugs. New approaches used in the design and optimization of LTLs is discussed and the advantages and potential problems associated with their therapeutic applications are described. New technologies are widening the spectrum of ligands available for targeting and are allowing choices to be made regarding affinity, internalization and size. The time is rapidly approaching where we will see translation of anticancer drugs entrapped in LTLs to the clinic.