The construction of nanosized drug delivery systems possesses tremendous potential due to their ability to improve the solubility of poorly soluble drugs and to reduce metabolism by dissolving them in their hydrophobic or hydrophilic compartment. In addition, nanomedicine holds the advantages of passive targeting ability due to an enhanced permeability and retention (EPR) effect, a large surface-to-volume ratio for drug loading, a tunable size for modification, a prolonged plasma half-life and a different biodistribution profile compared to conventional chemotherapy. Typical nano-based delivery vehicles include liposome, micelle, dendrimer, inorganic vector, nanogel and nanoemulsion, while novel nanocarriers also contain biomimetic reconstituted high-density lipoprotein (rHDL), exosome and the hybrid nanoparticle, which come from the mixture of nanomaterials. Each of these nanotools displays its unique physiochemical properties and possesses the ability for further modification of active targeting ligands.