Abstract The science innovations improved the patient quality of life and perspectives. In particular, the revolutionary turmoil of the second half of twentieth century in the Science Academia poses the milestone to develop innovative supramolecular nanotherapeutics and enforce nanotechnology and drug delivery. The driving force of this revolution was the synthesis of novel, safe and biocompatible nanomaterials, which can be easily combined to design new supramolecular nanotherapeutics. Additionally, these innovative nanomaterials can, per se or as supramolecular nanocarriers, deliver bioactive compounds, which show different physical-chemical features, and treat different diseases. Recently, pharmaceutical industry and academia show a specific interest for natural products, which emerge as potential new drug candidates for the therapeutic treatment of inflammatory pathologies. In fact, the delivery of natural products by using supramolecular nanotherapeutics can represent a great opportunity in nanomedicine and an alternative therapeutic option to conventional medicine for treating inflammatory diseases. In this review, we will discuss the recent innovation of supramolecular nanotherapeutics delivering natural anti-inflammatory compounds and provide an overview of their application in nanomedicine.