There are some reported anticancer and antibacterial effects for embelin, although, its poor aqueous solubility and bioavailability are main hindrance to applying embelin in therapeutics. In this regard, nanoformulations based on bare or functionalized nanomaterials can overcome these disadvantages. Embelin can be loaded or incorporated in biocompatible polymeric or protein nanoparticles (NPs) such as albumin NPs to improve solubility. In addition, targeting specific active sites of some major biological components such as amino acids of efflux pump in multidrug-resistant (MDR) bacteria can be possible by nanoformulation of embelin. The induction of apoptosis processes in cancer cells is also one of the major anticancer mechanisms of embelin, which has exhibited significant in vitro and in vivo results when nanoformulations are employed. The main aim of this review is to make a discussion about the advantages of these new nanoformulations in comparison with pure embelin. Overlay, embelin may be loaded or incorporated in biocompatible protein or polymeric NPs such as albumin NPs. Specifically, for antibacterial activity, nanoformulation of embelin-loaded chitosan Au-NPs with ciprofloxacin antibiotic exhibited the efficient interactions between embelin and the active sites of the efflux pump. Additionally, hyaluronic acid-coated amphiphilic polymeric NPs have the ability to enhance embelin uptake by triple-negative breast cancer cells (Reference).