This paper reviews the optimization of antiproliferative drugs, the innovations in excipients, the improvements in coating methods, and the smart drug-coated balloons (DCB). Advantages, disadvantages, and future optimization of two commonly used antiproliferative drugs, paclitaxel (PTX) and sirolimus and its derivatives are presented. The mechanism of action and future application prospects of iopromide, polyethylene oxide (PEO), citrate, and keratose (KOS) as excipients are described. Then, coating methods, such as the micropipette method, the dip coating method, the brush coating method, and the spray coating method, are outlined, and their advantages and disadvantages are explained. Then, it is followed by a brief description of the combination of smart response technology and DCB, which introduces the principles of action and potential applications of smart DCB such as ultrasound-responsive, light-driven, gas-driven, reactive oxygen species (ROS)-responsive, and microneedle (MN) coatings. Finally, based on the above, the problems of DCB are analyzed, and the future development direction of DCB is projected.