Höchsmann Alisa, Dhellemmes Laura, Leclercq Laurent, Cottet Hervé, Neusüß Christian
Faculty of Chemistry, Aalen University, Aalen, Germany.
Faculty of Science, Eberhard Karls University of Tübingen, Tübingen, Germany.
Electrophoresis. 2025 Mar;46(5-6):279-289. doi: 10.1002/elps.202400084. Epub 2024 Sep 17.
The characterization of the impurities of pharmaceutical monoclonal antibodies (mAbs) is crucial for their function and safety. Capillary zone electrophoresis (CZE) is one of the most efficient tools to separate charge variants of mAbs; however, peak characterization remains difficult, since the hereby used background electrolytes (BGEs) are not compatible with electrospray ionization-mass spectrometry (ESI-MS). Here, a method that allows the separation of intact mAb charge variants is presented using CZE-ESI-MS, combining a cationic capillary coating and an acidic BGE. Therefore, a successive multiple ionic-polymer layer coating was developed based on diethylaminoethyl-dextran-poly(sodium styrene sulfonate). This coating leads to a relatively low reversed electroosmotic flow (EOF) with an absolute mobility slightly higher than that of antibodies, enabling the separation of variants with slightly different mobilities. The potential of the coating is demonstrated using USP mAb003, where it was possible to separate C-terminal lysine variants from the main form, as well as several acidic variants and monoglycosylated mAb forms. The presented CZE-MS method can be applied to separate charge variants of a range of other antibodies such as infliximab, NISTmAB (Reference Material from the National Institute of Standards and Technology), adalimumab, and trastuzumab, demonstrating the general applicability for the separation of proteoforms of mAbs.
药物单克隆抗体(mAb)杂质的表征对于其功能和安全性至关重要。毛细管区带电泳(CZE)是分离mAb电荷变体最有效的工具之一;然而,峰的表征仍然很困难,因为在此使用的背景电解质(BGE)与电喷雾电离质谱(ESI-MS)不兼容。本文提出了一种使用CZE-ESI-MS分离完整mAb电荷变体的方法,该方法结合了阳离子毛细管涂层和酸性BGE。因此,基于二乙氨基乙基-葡聚糖-聚(苯乙烯磺酸钠)开发了一种连续多层离子聚合物涂层。这种涂层导致相对较低的反向电渗流(EOF),其绝对迁移率略高于抗体,从而能够分离迁移率略有不同的变体。使用美国药典mAb003证明了该涂层的潜力,在该实验中,可以将C端赖氨酸变体与主要形式分离,以及几种酸性变体和单糖基化mAb形式。所提出的CZE-MS方法可用于分离一系列其他抗体的电荷变体,如英夫利昔单抗、NISTmAB(美国国家标准与技术研究院的参考物质)、阿达木单抗和曲妥珠单抗,证明了该方法对mAb蛋白变体分离的普遍适用性。