In the foreseeable future, the pharmaceuticals market, nanomedicine, and healthcare systems will largely depend on the drug nanoparticle formulation technology. Perceiving this, scientists around the world are reporting each day a significant amount of research work focusing on the fundamentals of nanocrystallization and performance enhancement. The nanocrystallization strategies' industrial applications mainly depend on the ability of the technique to produce nanoparticles of active pharmaceutical ingredients (APIs) with controlled particle size, narrow size distribution, stability, reproducibility, high solid loading, scale-up feasibility, suitabilty for a range of APIs, and cost-effectiveness. There are plenty of reports witnessing performance improvements of nanodrugs. The harmony between the nanocrystallization strategies, performance of nanodrugs, scale-up producibility, and industrial challenges remains an untold and unsummarized story in the field of pharmaceutical nanotechnology. This review is devoted to comprehensively discussing the promising nanocrystallization strategies, fundamental concepts, and promising results of nanodrugs. We have also reviewed the progress toward commercialization and market based on nanodrugs, further challenges toward industrial application, and the future direction of pharmaceutical technologies and their impact on the future of the healthcare system.