Abstract: Nowadays significant progress has been made in the study of nanoparticulate drug delivery systems which hold great potentials for the diagnosis and therapy of many diseases. However, the rate of industrial and clinical translation of these systems is slow, mainly due to the limitations of conventional preparation methods such as high batch-to-batch variations in physicochemical properties and poor feasibility in process scale-up. With good controllability and reproducibility in fluid mixing, microfluidic technology has been utilized to overcome the limitations of conventional precipitation methods and accelerate the industrial and clinical translation of nanoparticulate drug preparations. This article reviewed the advances of microfluidic technology in the preparation of nanoparticulate drug delivery systems from the perspectives of principles and characteristics of microfluidic precipitation, the engineering of microfluidic devices, and the prepared nanoparticulate drugs.