In the face of a large number of insoluble drugs, the development of nanocrystals is effective in destroying the limits of poorly soluble drug applications and becoming an indispensable route of drug delivery in the pharmaceutical industry. In addition, the proposed delivery goal is to provide more convenience and benefits and the number of researchers who are developing a number of advanced technologies try to use improved nano-drugs to improve the bioavailability of drug, drug dissolution velocity and solubility. Previously, more mature study has been done, for example, preparation of nanocrystals, the problems of safety, the route of administration and so on. This review systematically dwells upon several of the current nanocrystals technologies for target delivery by different modification technologies, such as magnetic nanocrystals, PEG and PEGylated chitosan modified nanocrystals, cationic nanocrystals and pluronic modified nanocrystals. Subsequently, the effects of surface charge and particle size on the drug targeted administration was analyzed. This review will provide a new insight for improving stability and controllability of the nanocrystals, and promote the nanocrystals technology development in targeting drug delivery.