Glycyrrhetinic acid (GA), a famous natural product, has been attracting more attention recently because of its remarkable biological activity, natural sweetness, and good biocompatibility. In the past few years, a considerable amount of literature has grown up around the theme of GA-based chemical modification to broaden its functional applications. Promising structures including gels, micelles, nanoparticles, liposomes, and so forth have been constantly reported. On the one hand, the assembly mechanisms of various materials based on GA derivatives have been elucidated via modern analytical techniques. On the other hand, their potential application prospects in edible additives, intelligent drug delivery, and other fields have been investigated fully due to availability, biocompatibility, and controllable degradability. Inspired by these findings, a systematic summary and classification of the materials formed by GA derivatives seems necessary and meaningful. This review sums up the new functional applications of GA derivatives for the first time and provides better prospects for their application and development.