Moritz Bernd, Locatelli Valentina, Niess Michele, Bathke Andrea, Kiessig Steffen, Entler Barbara, Finkler Christof, Wegele Harald, Stracke Jan
F. Hoffmann-La Roche Ltd, Basel, Switzerland.
IMC Fachhochschule Krems, University of Applied Sciences, Krems, Austria.
Electrophoresis. 2017 Dec;38(24):3136-3146. doi: 10.1002/elps.201700145. Epub 2017 Oct 9.
CZE is a well-established technique for charge heterogeneity testing of biopharmaceuticals. It is based on the differences between the ratios of net charge and hydrodynamic radius. In an extensive intercompany study, it was recently shown that CZE is very robust and can be easily implemented in labs that did not perform it before. However, individual characteristics of some examined proteins resulted in suboptimal resolution. Therefore, enhanced method development principles were applied here to investigate possibilities for further method optimization. For this purpose, a high number of different method parameters was evaluated with the aim to improve CZE separation. For the relevant parameters, design of experiments (DoE) models were generated and optimized in several ways for different sets of responses like resolution, peak width and number of peaks. In spite of product specific DoE optimization it was found that the resulting combination of optimized parameters did result in significant improvement of separation for 13 out of 16 different antibodies and other molecule formats. These results clearly demonstrate generic applicability of the optimized CZE method. Adaptation to individual molecular properties may sometimes still be required in order to achieve optimal separation but the set screws discussed in this study [mainly pH, identity of the polymer additive (HPC versus HPMC) and the concentrations of additives like acetonitrile, butanolamine and TETA] are expected to significantly reduce the effort for specific optimization.
毛细管区带电泳(CZE)是一种成熟的生物制药电荷异质性检测技术。它基于净电荷与流体动力学半径之比的差异。在一项广泛的公司间研究中,最近表明CZE非常稳健,并且可以在以前未进行过该检测的实验室中轻松实施。然而,一些被检测蛋白质的个体特征导致分辨率欠佳。因此,这里应用了增强的方法开发原则来研究进一步优化方法的可能性。为此,评估了大量不同的方法参数,目的是改善CZE分离效果。对于相关参数,针对分辨率、峰宽和峰数量等不同响应集,以多种方式生成并优化了实验设计(DoE)模型。尽管进行了针对产品的DoE优化,但发现优化参数的最终组合确实使16种不同抗体和其他分子形式中的13种的分离效果得到了显著改善。这些结果清楚地证明了优化后的CZE方法的通用适用性。为了实现最佳分离,有时可能仍需要根据个体分子特性进行调整,但本研究中讨论的固定参数(主要是pH值、聚合物添加剂的种类(羟丙基纤维素与羟丙基甲基纤维素)以及乙腈、丁醇胺和三亚乙基四胺等添加剂的浓度)有望显著减少特定优化所需的工作量。