Nanocrystals are used as a drug-delivery platform for poorly water-soluble drugs and have had commercial success in oral drug delivery. We assert that the future of this technique is with cancer treatment and in the development of parenteral preparations. Advances in techniques for uniform and high-quality nanocrystals as well as deciphering the in vivo fate of nanocrystals are critical. The bottom-up technique allows for better control of particle properties, while the hybrid nanocrystal technique provides a novel approach to explore the in vivo fate of nanocrystals. Breakthroughs in these two techniques to further the development of nanocrystals are also discussed.