Background Rutin as a natural flavonoid compound has revealed an extensive range of therapeutic potentials. Purpose The current paper is focused on the numerous studies on rutin nanoformulations regarding its broad spectrum of therapeutic potentials. Study and methods A review was conducted in electronic databases (PubMed) to identify relevant published literature in English. No restrictions on publication date were imposed. Results The literature search provided 7,078 results for rutin. Among them, 25 papers were related to the potential biological activities of rutin nanoformulations. Polymeric nanoparticles were the most studied nanoformulations for rutin (14 titles) and lipid nanoparticles (5 titles) were in second place. The reviewed literature showed that rutin has been used as an antimicrobial, antifungal, and anti‐allergic agent. Improving the bioavailability of rutin using novel drug‐delivery methods will help the investigators to use its useful effects in the treatment of various chronic human diseases. Conclusion It can be concluded that the preparation of rutin nanomaterials for the various therapeutic objects confirmed the enhanced aqueous solubility as well as enhanced efficacy compared to conventional delivery of rutin. However, more investigations should be conducted to confirm the improved bioavailability of the rutin nanoformulations. The graphical shows different rutin‐loaded nanomaterials for in vitro, in vivo and, clinical investigations.