School of Chemistry and Biochemistry, Georgia Institute of Technology, Atlanta, GA 30332, USA.
School of Chemistry and Biochemistry, Georgia Institute of Technology, Atlanta, GA 30332, USA; Joint Department of Biomedical Engineering, North Carolina State University and The University of North Carolina, Chapel Hill, Raleigh, NC, USA; Comparative Medicine Institute, North Carolina State University, Raleigh, NC, USA.
Colloids Surf B Biointerfaces. 2018 Jun 1;166:89-97. doi: 10.1016/j.colsurfb.2018.03.003. Epub 2018 Mar 2.
Excessive bleeding and resulting complications are a major cause of death in both trauma and surgical settings. Recently, there have been a number of investigations into the design of synthetic hemostatic agents with platelet-mimicking activity to effectively treat patients suffering from severe hemorrhage. We developed platelet-like particles from microgels composed of polymers carrying polyethylene glycol (PEG) side-chains and fibrin-targeting single domain variable fragment antibodies (PEG-PLPs). Comparable to natural platelets, PEG-PLPs were found to enhance the fibrin network formation in vitro through strong adhesion to the emerging fibrin clot and physical, non-covalent cross-linking of nascent fibrin fibers. Furthermore, the mechanical reinforcement of the fibrin mesh through the incorporation of particles into the network leads to a ∼three-fold decrease of the overall clot permeability as compared to control clots. However, transport of biomolecules through the fibrin clots, such as peptides and larger proteins is not hindered by the presence of PEG-PLPs and the altered microstructure. Compared to control clots with an elastic modulus of 460+/-260 Pa, PEG-PLP-reinforced fibrin clots exhibit higher degrees of stiffness as demonstrated by the significantly increased average Younǵs modulus of 1770 +/±720 Pa, as measured by AFM force spectroscopy. Furthermore, in vitro degradation studies with plasmin demonstrate that fibrin clots formed in presence of PEG-PLPs withstand hydrolysis for 24 h, indicating enhanced stabilization against exogenous fibrinolysis. The entire set of data suggests that the designed platelet-like particles have high potential for use as hemostatic agents in emergency medicine and surgical settings.
过度出血和由此导致的并发症是创伤和外科环境中死亡的主要原因。最近,人们对具有血小板模拟活性的合成止血剂的设计进行了大量研究,以有效治疗严重出血的患者。我们从由带有聚乙二醇(PEG)侧链的聚合物和纤维蛋白靶向单结构域可变片段抗体(PEG-PLPs)组成的微凝胶中开发出了类似血小板的颗粒。与天然血小板类似,PEG-PLPs 通过与新形成的纤维蛋白凝块牢固结合以及对新生纤维蛋白纤维的物理非共价交联,在体外增强纤维蛋白网络的形成。此外,通过将颗粒纳入网络中对纤维蛋白网进行机械增强,导致与对照凝块相比,总凝块渗透率降低了约三倍。然而,通过 PEG-PLPs 的存在和改变的微结构,生物分子(例如肽和较大的蛋白质)的运输不会受到阻碍。与弹性模量为 460±260 Pa 的对照凝块相比,PEG-PLP 增强的纤维蛋白凝块表现出更高的刚性程度,这是通过 AFM 力谱法测量的平均杨氏模量明显增加至 1770±720 Pa 来证明的。此外,用纤溶酶进行的体外降解研究表明,在 PEG-PLPs 存在下形成的纤维蛋白凝块能够耐受 24 小时的水解,表明其对纤维蛋白溶解的稳定性增强。整套数据表明,设计的类似血小板的颗粒具有作为急救医学和外科环境中止血剂的高应用潜力。