Photodynamic therapy (PDT) has been used to treat several types of cancer, and comprises intravascular administration of photosensitizer, uptake by cancer cells, and followed by irradiation of light of appropriate wavelength. Although PDT takes advantage of relative retention of photosensitizer by cancer cells, effective delivery of photosensitizing drugs is of great concern. Several delivery strategies have been employed in PDT. Photosensitizers can be delivered either by passive carriers such as liposomes, micelles, and polymeric particles, or by active targeting using cancer cell-directed ligands or antibodies. Although well-studied colloidal carriers effectively deliver photosensitizer to tumor cells, they are taken up by mononuclear phagocytic system. Delivery system using polymers is an attractive alternative to colloidal carriers, in which hydrophobic drugs are chemically or physically loaded to polymers. Though there are several steps to be solved, targeted delivery system utilizing receptors or antigens abundantly expressed on cancer cell theoretically provides a great deal of advantages over passive system. Selective uptake of photosensitizers by cancer cells may greatly enhance therapeutic efficacy as well as minimizing adverse effects resulting from accumulation in normal tissue. This review discusses various strategies for photosensitizer delivery that have been investigated to date.