Introduction: Docetaxel (DTX) has been proven as one of the most important cytotoxic agents, and its clinical efficacy against many cancers is superior to paclitaxel. DTX in commercial formulation contains the non-ionic surfactant Tween 80 (polysorbate 80) and 13% ethanol; the side effects caused by DTX and the solvent have considerably limited its clinical use. In recent decades, the emergence of nanoformulations provides new modes of actions in DTX. Many nano-sized carriers can help DTX transport through leaky tumor capillary fenestrations into the tumor cells. Moreover, these particles can be modified for binding to specific sites such as cancer cell membranes, cytoplasmic or nuclear receptors.
Areas covered: The authors focus on nanoformulations related to DTX delivery, covering their preparation, physicochemical properties and the in vitro and in vivo actions against tumor cells. The challenges involved in the development of nanoformulations for DTX are also discussed.
Expert opinion: Although nanoformulations such as liposome, micelle, nanoparticle, nanoemulsion greatly improve the solubility, activity and distribution of DTX in vivo, significant hurdles remain concerning aspects of nanoformulations such as quality control, physicochemical stability, storage conditions, large-scale production and controlled manufacture technology, in vivo metabolism, excretion, acute and chronic toxicity, etc. In-depth studies in these areas are essential to making DTX nanoformulations applicable in clinic and commercially available viable.