Orlistat is a FDA-approved antiobesity drug that shows anticancer effect in a wide range of cancers. However, off-target effects and poor bioavailability hinder its clinical translation as a repurposed new drug against triple-negative breast cancer (TNBC). Orlistat loaded in HEA-b-EHA polymeric micellar-nanoparticles improved the solubility, bioavailability, and therapeutic efficacy of orlistat in vitro in cells and in vivo in tumor xenografts of TNBC in mice. The cover image shows a schematic illustration of the orlistat-loaded HEA-b-EHA polymeric micelles with different functional moieties used for tumor targeting (folic acid) and imaging (DyLight-747-B1-NIR Dye) in living animals. The results of this study indicate that the orlistat packaged in HEA-b-EHA micellar-NP is a highly promising new drug formulation for TNBC therapy. For details, see the article by Paulmurugan and colleagues on page 221.