With the inherent merits of a low reagent consumption, the small amount of sample needed and easy integration, a wide variety of microfluidic platforms (continuous-flow, droplet, digital and paper) have been developed to address the challenges (e.g. throughput, single-cell isolation, cost and flexibility) of cell-based drug screening. This review essentially summarises the pros and cons of the platforms for different applications, so as to shed light on the road ahead for drug screening research and discovery via the advance of microfluidics.