In cancer treatment, one of the approaches is targeting of the drug to tumor cells via receptor specific ligands. Transferrin (molecular weight 80,000) has been used as a ligand for delivering anticancer drugs or drug containing liposomes mostly due to the increased number of transferrin (trf) receptors found on tumor cells as compared to normal cells. Transferrin was linked to methotrexate (MTX) containing small unilamellar liposomes and its activity was compared to antitransferrin receptor antibody (7D-3) linked to MTX liposomes. In each of these conjugates, the method of coupling was the same and a disulphide linkage was formed between the ligand and MTX liposomes. No significant differences in the potency of 7D-3 conjugate or trf conjugate with MTX liposomes were observed in studies performed in vitro against various human tumor cell lines (Hela, KB and Colon). Trf was also linked to adriamycin via a schiff base which was formed by using glutaraldehyde. This conjugate was found to be effective in vitro against various human tumors (Lovo, HL-60, SW 403 and Hep2) and also in vivo against H-mesothelioma tumors. Transferrin receptor has also been used for gene delivery. Gene delivery to K562 haematopoietic leukaemic cells was achieved by using a transferrin-polycation (poly-L-lysine or protamine) conjugate. This review will cover the various important applications of transferrin based drug delivery formulations in the chemotherapy of cancer and the related work performed in our and other laboratories.