Xu Xuan, Li Mingxi, Yu Fuchao, Wei Qin, Liu Yang, Tong Jiayi, Yang Fang
Department of Cardiology, Zhongda Hospital Affiliated to Southeast University, 87, Dingjiaqiao, Nanjing, 210009, P. R. China.
State Key Laboratory of Digital Medical Engineering, Jiangsu Key Laboratory for Biomaterials and Devices, School of Biological Sciences and Medical Engineering, Southeast University, Nanjing, 210096, P. R. China.
Adv Sci (Weinh). 2024 Apr;11(16):e2308727. doi: 10.1002/advs.202308727. Epub 2024 Feb 12.
Although treatments for myocardial infarction have advanced significantly, the global mortality due to ischemia and subsequent reperfusion injury remains high. Here, a platelet (PLT) membrane nanocarrier (PL720) that encapsulates L-arginine and FTY720 to facilitate the cascade-targeted delivery of these substances to the myocardial injury site and enable the controlled release of L-arginine and FTY720 is developed. Such an innovative approach shows enhanced cardioprotection through multiple target strategies involved in ischemia-reperfusion injury and late reperfusion inflammation. During the ischemia-reperfusion phase, PL720 targets and accumulates in damaged coronary arteries. PL720 rapidly releases L-arginine, stimulating endothelial cells to produce NO, thereby dilating blood vessels and promoting blood flow recovery, while FTY720's sustained release exerts anti-apoptotic effects. During the late reperfusion inflammatory phase, PL720 is captured by circulating inflammatory monocytes and transported into a deeper ischemic myocardial lesion. PL720 promotes macrophage polarization and accelerates the inflammatory repair. Furthermore, the issue of bradycardia associated with the clinical use of FTY720 is innovatively relieved. Therefore, PL720 is a vascular injury and inflammation dual targeting strategy, exhibiting significant potential for multi-targeted therapy and clinical translation for cardiac injury.
尽管心肌梗死的治疗已取得显著进展,但由于缺血及随后的再灌注损伤导致的全球死亡率仍然很高。在此,开发了一种血小板(PLT)膜纳米载体(PL720),其包裹L-精氨酸和FTY720,以促进这些物质向心肌损伤部位的级联靶向递送,并实现L-精氨酸和FTY720的控释。这种创新方法通过参与缺血再灌注损伤和晚期再灌注炎症的多种靶向策略显示出增强的心脏保护作用。在缺血再灌注阶段,PL720靶向并积聚在受损冠状动脉中。PL720迅速释放L-精氨酸,刺激内皮细胞产生一氧化氮,从而扩张血管并促进血流恢复,而FTY720的持续释放发挥抗凋亡作用。在晚期再灌注炎症阶段,PL720被循环中的炎性单核细胞捕获并转运至更深的缺血心肌损伤部位。PL720促进巨噬细胞极化并加速炎症修复。此外,创新性地缓解了与FTY720临床应用相关的心动过缓问题。因此,PL720是一种血管损伤和炎症双靶向策略,在心脏损伤的多靶点治疗和临床转化方面具有巨大潜力。