AbstractTaxanes have been recognized as a family of very efficient anticancer drugs, but the formulation in use for the two main taxanes—Taxol for paclitaxel and Taxotere for docetaxel—have shown dramatic side effects. Whereas several new formulations for paclitaxel have recently appeared, such as Abraxane and others currently in various phases of clinical trials, there is no new formulation in clinical trials for the other main taxane, docetaxel, except BIND‐014, a polymeric nanoparticle, which recently entered phase I clinical testing. Therefore, we review herein the state of the art and recent abundance in published results of academic approaches toward nanotechnology‐based drug‐delivery systems containing nanocarriers and targeting agents for docetaxel formulations. These efforts will certainly enrich the spectrum of docetaxel treatments in the near future. Taxotere′s systemic toxicity, low water solubility, and other side effects are significant problems that must be overcome. To avoid the limitations of docetaxel in clinical use, researchers have developed efficient drug‐delivery assemblies that consist of a nanocarrier, a targeting agent, and the drug. A wide variety of such engineered nanosystems have been shown to transport and eventually vectorize docetaxel more efficiently than Taxotere in vitro, in vivo, and in pre‐clinical administration. Recent progress in drug vectorization has involved a combined therapy and diagnostic (“theranostic”) approach in a single drug‐delivery vector and could significantly improve the efficiency of such an anticancer drug as well as other drug types.