Drug delivery to the brain is crucial in the treatment for central nervous system disorders. While significant progress has been made in recent years, there are still major challenges in achieving controllable drug delivery to the brain. Unmet clinical needs arise from various factors, including controlled drug transport, handling large drug doses, methods for crossing biological barriers, the use of imaging guidance, and effective models for analyzing drug delivery. Recent advances in micro/nanosystems have shown promise in addressing some of these challenges. These include the utilization of microfluidic platforms to test and validate the drug delivery process in a controlled and biomimetic setting, the development of novel micro/nanocarriers for large drug loads across the blood-brain barrier, and the implementation of micro-intervention systems for delivering drugs through intraparenchymal or peripheral routes. In this article, we present a review of the latest developments in micro/nanosystems for controllable drug delivery to the brain. We also delve into the relevant diseases, biological barriers, and conventional methods. In addition, we discuss future prospects and the development of emerging robotic micro/nanosystems equipped with directed transportation, real-time image guidance, and closed-loop control.