Abstract: Microfluidics is a technology that involves the use of micro-nanoscale pipelines to manipulate fluid mixing. Precise control of the mixing process of laminar flows or liquid droplets by using microfluidics will contribute to the preparation of nanoparticles, which are difficult to be achieved by the conventional methods. Based on the progress in delivery systems of nanoparticulate drug, we provide a summary to introduce the applications of microfluidics in construction of nanoparticulate drug delivery system such as liposomes, polymer nanoparticles and hybrid nanoparticles, and analyze the assembling mechanisms of different nanostructures by using microfluidic precise control. This review will provide a reference in utilization of microfluidic technology more scientifically and reasonably.