Abstract: Because of its high biocompatibility, flexibility and prebiotic activities, increasing attention has been paid in recent years to inulin derivatives for expanding the applications of inulin. The present review focuses on synthetic methods, characterization, bioactivity and potential application of inulin derivatives. Three types of modification that inulin grafting with functional groups, bioactive molecules and biological macromolecules, were summarized. And the structure of inulin derivatives can be characterized by a variety of instrumental analysis methods. Compared with natural inulin, inulin derivatives exhibit better biological activities such as enhanced antioxidant, anti-inflammatory and anti-cancer activities. As emulsifiers, embedded materials, coating materials and fluorescent marker carriers, inulin derivatives with different physical properties also can be applied in many fields.