在浓缩抗体溶液中,静电和黏度密切相关

IF 9.1 1区 综合性期刊 Q1 MULTIDISCIPLINARY SCIENCES
Fabrizio Camerin, Marco Polimeni, Anna Stradner, Emanuela Zaccarelli, Peter Schurtenberger
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引用次数: 0

摘要

单克隆抗体是现代医学中最有前途的治疗药物之一,但将其配制成高浓度的皮下自给药溶液是一个重大挑战。一个关键的障碍是在这些条件下经常观察到粘度的显著增加。为了更深入地了解这一现象,从软物质物理学中衍生的粗粒度模型已被广泛使用。然而,这些模型还没有被充分利用来分析这种体系的流变集体特性。在本研究中,利用分子动力学模拟,我们从常用的静电相互作用通过有效筛选的库仑电位处理的模型开始,直接计算抗体溶液粘度。我们证明这种方法无法重现实验证据,并且通过分析系统中的应力相关性,我们表明有必要用显式库仑相互作用来处理异质带电域,也包括反离子和盐离子。通过深入分析该体系的微观结构,我们进一步揭示了瞬态强相关抗体的存在,如果隐式处理电荷,则不会存在这种抗体,从而指出静电在决定高浓度下粘度增加方面的突出作用。通过利用我们的实际治疗方法,可以设计出新的方法来确保抗体溶液表现出预期的广泛使用和有效部署所需的特性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Electrostatics and viscosity are strongly linked in concentrated antibody solutions
Monoclonal antibodies are among the most promising therapeutic agents in modern medicine, yet their formulation into high-concentration solutions for subcutaneous self-administration poses a major challenge. A key obstacle is the marked increase in viscosity often observed under these conditions. To gain deeper insights into this phenomenon, coarse-grained models derived from soft matter physics have been widely employed. However, these models have yet to be fully leveraged for analyzing the rheological collective properties of such systems. In this study, using molecular dynamics simulations, we directly compute the antibody solution viscosity by starting from commonly used models in which electrostatic interactions are treated through effective screened Coulomb potentials. We demonstrate that this approach fails to reproduce experimental evidence and we show, by analyzing stress correlations in the system, that it is necessary to treat the heterogeneously charged domains with explicit Coulomb interactions, also including counterions and salt ions. By thoroughly analyzing the microscopic structure of the system, we further reveal the presence of transient strongly correlated antibodies which would not be present if charges were treated implicitly, thus pointing to a prominent role of electrostatics in determining the increase in viscosity at high concentrations. By taking advantage of our realistic treatment, new approaches can be devised to ensure that antibody solutions exhibit the desired characteristics for their intended broad use and effective deployment.
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来源期刊
CiteScore
19.00
自引率
0.90%
发文量
3575
审稿时长
2.5 months
期刊介绍: The Proceedings of the National Academy of Sciences (PNAS), a peer-reviewed journal of the National Academy of Sciences (NAS), serves as an authoritative source for high-impact, original research across the biological, physical, and social sciences. With a global scope, the journal welcomes submissions from researchers worldwide, making it an inclusive platform for advancing scientific knowledge.
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