Shin Ha Eun, Giannakopoulos Stefanos, Park Joo Dong, Jang Hye Jung, Park Chun Gwon, Murphy Sean V, Park Juwon, Verma Saguna, Park Wooram
Department of Tropical Medicine, Medical Microbiology, and Pharmacology, John A. Burns School Medicine, University of Hawai'i at Manoa, Honolulu, HI 96813, USA.
Department of Integrative Biotechnology, College of Biotechnology and Bioengineering Sungkyunkwan University (SKKU), Suwon, Gyeonggi 16419, Republic of Korea.
J Control Release. 2025 Jun 10;382:113736. doi: 10.1016/j.jconrel.2025.113736. Epub 2025 Apr 18.
The need to understand key players driving pulmonary inflammation and fibrosis in COVID-19 patients leading to effective preventive strategies is imminent. Excessive neutrophil activation, including extracellular trap (NET) formation, is associated with severe COVID-19 and long-term sequelae. However, the clinical applications of neutrophil-targeting therapies are challenging due to short bioavailability and lack of cell-type specificity. This study presents a lipid nanoparticle (LNP) platform designed to deliver two established NET inhibitors, DNase I and Sivelestat (Siv) referred to as DPNLNPs, specifically to lung neutrophils. In vitro and in vivo experiments demonstrate that DPNLNPs preferentially accumulate in the lung neutrophils and degrade NETs as efficiently as the free DNase I and Siv. Additionally, administration of DPNLNPs in K18-hACE2 mice significantly inhibited SARS-CoV-2-induced NETs at a much lower dose than the free drugs and correlated with reduced lung and systemic inflammation, lung epithelium injury, and collagen deposition. Importantly, DPNLNP treatment only during the symptomatic phase of infection improved SARS-CoV-2 outcome revealing the complex role of NETs in COVID-19 pathogenesis. Together, this study serves as a proof-of-concept for adapting the LNP platform to deliver more than one immunomodulatory drug in a cell-specific manner to manage NET-associated complications in COVID-19 and other respiratory diseases.
迫切需要了解导致COVID-19患者肺部炎症和纤维化的关键因素,从而制定有效的预防策略。包括细胞外陷阱(NET)形成在内的中性粒细胞过度激活与严重的COVID-19及长期后遗症相关。然而,由于生物利用度短和缺乏细胞类型特异性,针对中性粒细胞的治疗方法在临床应用中具有挑战性。本研究提出了一种脂质纳米颗粒(LNP)平台,旨在将两种成熟的NET抑制剂,即脱氧核糖核酸酶I(DNase I)和西维来司他(Siv,称为DPNLNPs)特异性递送至肺中性粒细胞。体外和体内实验表明,DPNLNPs优先在肺中性粒细胞中积累,并与游离的DNase I和Siv一样有效地降解NETs。此外,在K18-hACE2小鼠中给予DPNLNPs,以比游离药物低得多的剂量显著抑制了SARS-CoV-2诱导的NETs,这与肺部和全身炎症、肺上皮损伤及胶原蛋白沉积减少相关。重要的是,仅在感染的症状期进行DPNLNP治疗改善了SARS-CoV-2的预后,揭示了NETs在COVID-19发病机制中的复杂作用。总之,本研究为调整LNP平台以细胞特异性方式递送多种免疫调节药物来管理COVID-19和其他呼吸系统疾病中与NET相关的并发症提供了概念验证。