Click chemistry-functionalized gold nanoparticles for the functional reversal of P2Y12 inhibitors

Antiplatelet agents (APAs) are crucial for the clinical prevention and treatment of thrombotic diseases, but their long-term use has serious bleeding risk. In emergency situations, it is essential to rapidly reverse the effect of APAs and restore the hemostatic function of platelets. However, there are currently no specific antiplatelet reversal agents approved for clinical use. Here, we describe a click chemistry-functionalized gold nanoplatform for the reversal of APAs. The gold nanoparticles (AuNPs), modified with dibenzocyclooctyne or maleimide on their surface, are able to neutralize the antiplatelet activity of azido-modified ticagrelor and clopidogrel, respectively. The in vitro platelet aggregation assays and in vivo tail bleeding or liver injury experiments validate the effectiveness of the gold nanoplatform. In summary, our study introduces a gold nanoplatform that can be easily prepared through a simple method and has great potential to be used for the functional reversal of various APAs.