一种通过抑制感染和炎症用于脓毒症急救的靶向感染微环境且具有响应性的肽-药物纳米系统
An infection-microenvironment-targeted and responsive peptide-drug nanosystem for sepsis emergency by suppressing infection and inflammation.
作者信息
He Wei, Fu Daan, Gai Yongkang, Liu Xingxin, Yang Chang, Ye Zhilan, Chen Xu, Liu Jia, Chang Bingcheng
机构信息
The Second Clinical College, The Second Affiliated Hospital, Guizhou University of Traditional Chinese Medicine, Guiyang 550003, China.
Department of Anesthesiology, Tongji Medical College, Union Hospital, Huazhong University of Science and Technology, Wuhan 430022, China.
出版信息
Asian J Pharm Sci. 2023 Nov;18(6):100869. doi: 10.1016/j.ajps.2023.100869. Epub 2023 Nov 28.
Sepsis is a life-threatening emergency that causes millions of deaths every year due to severe infection and inflammation. Nevertheless, current therapeutic regimens are inadequate to promptly address the vast diversity of potential pathogens. Omiganan, an antimicrobial peptide, has shown promise for neutralizing endotoxins and eliminating diverse pathogens. However, its clinical application is hindered by safety and stability concerns. Herein, we present a nanoscale drug delivery system (Omi-hyd-Dex@HA NPs) that selectively targets infectious microenvironments (IMEs) and responds to specific stimuli for efficient intervention in sepsis. The system consists of omiganan-dexamethasone conjugates linked by hydrazone bonds which self-assemble into nanoparticles coated with a hyaluronic acid (HA). The HA coating not only facilitates IMEs-targeting through interaction with intercellular-adhesion-molecule-1 on inflamed endotheliocytes, but also improves the biosafety of the nanosystem and enhances drug accumulation in primary infection sites triggered by hyaluronidase. The nanoparticles release dual drugs in IMEs through pH-sensitive cleavage of hydrazone bonds to eradicate pathogens and suppress inflammation. In multiple tissue infection and sepsis animal models, Omi-hyd-Dex@HA NPs exhibited rapid source control and comprehensive inflammation reduction, thereby preventing subsequent fatal complications and significantly improving survival outcomes. The bio-responsive and self-delivering nanosystem offers a promising strategy for systemic sepsis treatment in emergencies.
脓毒症是一种危及生命的紧急情况,每年因严重感染和炎症导致数百万人死亡。然而,目前的治疗方案不足以迅速应对种类繁多的潜在病原体。抗菌肽奥米加南已显示出中和内毒素和清除多种病原体的潜力。然而,其临床应用受到安全性和稳定性问题的阻碍。在此,我们提出了一种纳米级药物递送系统(Omi-hyd-Dex@HA纳米颗粒),该系统可选择性地靶向感染性微环境(IME),并对特定刺激做出反应,以有效干预脓毒症。该系统由通过腙键连接的奥米加南-地塞米松缀合物组成,这些缀合物自组装成包裹有透明质酸(HA)的纳米颗粒。HA涂层不仅通过与炎症内皮细胞上的细胞间粘附分子-1相互作用促进对IME的靶向,还提高了纳米系统的生物安全性,并增强了由透明质酸酶触发的原发性感染部位的药物积累。纳米颗粒通过腙键的pH敏感裂解在IME中释放双重药物,以根除病原体并抑制炎症。在多种组织感染和脓毒症动物模型中,Omi-hyd-Dex@HA纳米颗粒表现出快速的源头控制和全面的炎症减轻,从而预防随后的致命并发症并显著改善生存结果。这种生物响应性和自我递送的纳米系统为紧急情况下的全身性脓毒症治疗提供了一种有前景的策略。