Abstract <p>The primary prognostic determinant after an acute coronarysyndrome is the volume of irreversibly damaged cardiac tissue (orinfarct size). Experimental studies have shown that various cardioprotectiveinterventions performed in the early reperfusion period, includingpharmacological postconditioning, can significantly reduce infarctsize. Attempts to translate these findings into clinical practicehave been unsuccessful, including due to suboptimal pharmacokineticparameters of the drugs used, their low bioavailability, or thepresence of serious side effects upon systemic administration. To addressthese problems, recent years have seen the development of systemsfor targeted delivery of cardioprotectors to the zone of myocardialischemia-reperfusion injury using nanoscale carriers. Nanoparticleconjugation with such biomolecules as adenosine, cyclosporine A,erythropoietin, pioglitazone, and gasotransmitter donors allowstheir preferential accumulation in the heart with subsequent controlledrelease. Experimental studies in the field of targeted deliveryof cardioprotectors show a higher infarct-limiting efficacy of nanoparticle-biomoleculeconjugates. Platforms containing specific targeting ligands, aswell as groups sensitive to local environmental conditions and externalstimuli, such as ultrasound, are beginning to be used for activetargeted delivery of cardioprotectors. The largest number of studiesrelated to the development of targeted delivery systems for cardioprotectorsare focused on hydrogen sulfide donors and adenosine. Prospects forimproving targeted delivery systems are associated with active targetingof damaged myocardial tissue, including through the use of biomimeticplatelet or leukocyte membrane-coated nanoparticles.</p>