Noninvasive monitoring/quantification of drug delivery to tumors is an ideal goal of chemotherapy treatment. However, the ability to overcome the barriers to the developing of targeted therapies—along with the physiological barriers that the tumor presents—is still needed. Recent advances demonstrate that targeted therapies can be used for diagnostic and therapeutic applications. The most mature of these technologies are liposomes that encapsulate a therapeutic drug in conjunction with a contrast agent. Through selective manipulation of the liposome composition, modification of the tumor microphysiology, and temporal sequencing of liposome administration with tumor microphysiology modification improvement in efficacy can be achieved. The future application of these targeted therapies will allow the radiologist to become a more central member of the cancer treatment team, further expanding the field and the radiologist’s unique skills.