Lawanprasert Atip, Singh Harminder, Pimcharoen Sopida, Vargas Mariangely González, Dewan Arshiya, Kirimanjeswara Girish S, Medina Scott H
Department of Biomedical Engineering, Pennsylvania State University, University Park, PA, USA.
Department of Veterinary and Biomedical Sciences, Pennsylvania State University, University Park, PA, USA.
Nat Commun. 2024 Dec 30;15(1):10897. doi: 10.1038/s41467-024-55304-9.
Over 80% of biologic drugs, and 90% of vaccines, require temperature-controlled conditions throughout the supply chain to minimize thermal inactivation and contamination. This cold chain is costly, requires stringent oversight, and is impractical in remote environments. Here, we report chemical dispersants that non-covalently solvate proteins within fluorous liquids to alter their thermodynamic equilibrium and reduce conformational flexibility. This generates non-aqueous, fluorine-based liquid protein formulations that biochemically rigidify protein structure to yield thermally stable biologics at extreme temperatures (up to 90 °C). These non-aqueous formulations are impervious to contamination by microorganismal pathogens, degradative enzymes, and environmental impurities, and display comparable pre-clinical pharmacokinetics and safety profiles to standard saline protein samples. As a result, we deliver a fluorochemical formulation paradigm that may limit the need for cold chain logistics of protein reagents and biopharmaceuticals.
超过80%的生物药物和90%的疫苗在整个供应链中都需要温度控制条件,以尽量减少热失活和污染。这种冷链成本高昂,需要严格监管,在偏远环境中也不实用。在此,我们报告了化学分散剂,其能在氟代液体中非共价溶剂化蛋白质,以改变其热力学平衡并降低构象灵活性。这产生了基于氟的非水液态蛋白质制剂,可在极端温度(高达90°C)下生物化学地强化蛋白质结构,从而产生热稳定的生物制品。这些非水制剂不受微生物病原体、降解酶和环境杂质的污染,并且与标准盐水蛋白质样品相比,显示出相当的临床前药代动力学和安全性概况。因此,我们提供了一种氟化物制剂模式,可能会减少对蛋白质试剂和生物制药冷链物流的需求。