Abstract: Hesperidin, a natural flavanone, predominantly existed in citrus fruit, has many biological functions, such as antioxidant, anti-inflammatory, bacteriostasis and anti-cancer. Current research suggests that hesperidin possesses a lower bioavailability due to its poor water solubility and absorption. Therefore, more and more attention from domestic and foreign scholars has been focused on physical, chemical and biological modification of hesperidin to increase its solubility and bioavailability. In this paper, the biological activity, modification technology and modification derivatives of hesperidin are reviewed to provide theoretical support for the efficient utilization of hesperidin.