Abstract Microfluidics has attracted considerable attention in various research areas of science and engineering. The precise manipulation of small amounts of liquid samples in microscale make it a valuable platform for the development of drug delivery systems. The microfluidic platforms have been used not only for the synthesis or assembly of nano- or microsized drug carriers, but also for controlled delivery of drug molecules into target tissues. This chapter presents the latest advances in microfluidics platforms for the fabrication of drug carriers and development of direct drug delivery devices. We discuss challenges and opportunities of advanced drug delivery systems as well as the potential roles of nano-/microfluidic technologies toward developing smart drug delivery systems.