Physical and chemical characteristics of NPs highly depend on their shapes, sizes, structures, morphologies, surface properties, and chemical compositions, [8,9] which are modifiable. In addition, NPs can carry small molecules, imaging agents, deoxyribonucleic acid (DNA), antibodies, peptides, proteins, or other substances to specific parts of the body. [10,11] On the other hand, investigations on different diseases have confirmed the need for a paradigm shift in the development of drugs and delivery systems. Hence, developing novel therapeutics and delivery approaches to treat diseases is a significant problem. [12] Therefore, many novel strategies based on innovative solutions have been developed. [13][14][15] Among these strategies, the synthesis of nanocarriers using microfluidic (MF) technology has become popular in recent years. This multidisciplinary technology is a unique platform for chemistry, medicine, pharmacy, physics, biology, materials science, fluid mechanics, and engineering. [16,17] Specifically, it has played a pivotal role in developing drug delivery systems. [18][19][20] Therefore, it is crucial to study MF experiments' practical potential and advantages over conventional methods. Furthermore, considering a high surface-to-volume ratio in MFs, they require fewer chemical reagents and generate less waste, making them suitable for Novel nanocarriers such as multifunctional nanoparticles (NPs) have recently attracted attention due to their various applications, specifically in medicine and treatment. However, it is vital that these particles be synthesized with meticulous control of different structural, chemical, and physical properties. In response to this demand, microfluidic (MF) technology as a reliable procedure can provide promising results in the development of desired NPs and efficient drug delivery systems. By controlling the flow rates of multiphase fluids and conditions of chemical reactions, MF technology enables the fabrication of uniform and highly stable particles with enhanced surfaces, higher encapsulation efficiency, and controlled release of therapeutic agents compared with conventional bulk methods. This review article investigates the MF-based methods utilized in the synthesis of NPs and their advantages in developing novel drug delivery systems. It also provides a comprehensive comparison with conventional methods from a different point of view, emphasizing a novel category of nanocarriers' critical characteristics. In addition, a summary of the most recent representative works on NPs fabrication by MF procedures is presented, and their potential and applications in drug delivery are discussed.The ORCID identification number(s) for the author(s) of this article can be found under