A lot of efforts have been devoted to engineering the delivery of hydrophobic drugs due to the high demand of chemotherapy against cancer. While early developed liposomes and polymeric nanoparticles did not meet the requirements of high drug loading efficiency, pure drug nanoparticles appeared to meet these together with high stability. Current drug delivery systems demand an improved performance over the whole aspects of stability, loading capacity, and therapeutic effects. As a result, both new techniques based on traditional methods and totally new procedures are under investigation. In this review, we focus on the evaluation of pure drug nanolloids fabricated by different engineering protocols with emphasis on the size and morphology, delivery and controlled release, and therapeutic effects of these drug nanocolloids.