Drug nanocarriers have gained a considerable attention in the development of cancer disease treatment. The nanoscale size and the capability of poorly water-soluble drug encapsulation, make nanoparticles a promising material for anti-cancer therapy. Drug encapsulation provides several advantages: the protection of the molecule against biological conditions and the possibility to deliver the therapeutic agent in the target region, limiting the side effects and enhancing the specificity and the efficiency of the treatment. Particle size, surface characteristics and drug release profile are fundamental aspects when designing an effective nanocarrier, as they define the drug delivery system performance. Therefore, the importance to control these features represents an issue of primary concern.