For treating cancer in particular, therapeutic agents have evolved in complexity in an effort to enhance targeting efficacy. So far, efforts towards the synthesis alone of new therapeutics have attracted most attention. However, present cancer treatments frequently fail because of severe side effects related to the fact that the drug accumulates in insufficient concentration at the tumor site, while being distributed over healthy tissues and organs. More recently, advanced engineering principles have been considered for the development of platforms and drug-loaded vehicles to deliver payloads to the area to be treated by navigating them using the most direct route in order to improve tumor killing effects while minimizing toxic side effects caused by drug activity in nontargeted regions. If the introduction of engineering and principles of robotics to provide complementary techniques in targeted cancer therapy prove to be beneficial, it could influence future delivery methods and the synthesis of therapeutic carriers.