Conventional pharmaceuticals generally display the inability to transport active ingredients directly to specific regions of the body, amongst some of their main limitations. The distribution of the drugs in the circulatory system may lead to undesired toxicity, and therefore, adverse reactions. To address this situation, a selective transport of drugs is required, that is, releasing drugs specifically to the site of action in appropriate concentrations and in the right time. To achieve this goal, it is necessary to develop delivery systems that respond to several features, such as low toxicity, optimum properties for the transport and release of the drug, as well as a long half-life in the body. This feature paper critically provides an overview of different strategies of controlled drug release for two model antineoplasic drugs, i.e. doxorubicin (DOX) and 5-fluorouracil (5-FU). Any of the presented strategies for drug release possess advantages and disadvantages, and the selection of the strategy used will depend on the targeted tissue and nature of the drug.