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利用光耦 NMR 光谱原位评估单抗制剂的光稳定性。

Assessing Photostability of mAb Formulations In Situ Using Light-Coupled NMR Spectroscopy.

机构信息

Department of Chemistry, School of Natural Sciences, Faculty of Science and Engineering, The University of Manchester, Manchester M1 7DN, U.K.

Dosage Form Design & Development, BioPharmaceutical Development, R&D, AstraZeneca, Cambridge CB2 0AA, U.K.

出版信息

Anal Chem. 2024 Jun 18;96(24):9935-9943. doi: 10.1021/acs.analchem.4c01164. Epub 2024 Jun 7.

Abstract

Biopharmaceuticals, such as monoclonal antibodies (mAbs), need to maintain their chemical and physical stability in formulations throughout their lifecycle. It is known that exposure of mAbs to light, particularly UV, triggers chemical and physical degradation, which can be exacerbated by trace amounts of photosensitizers in the formulation. Although routine assessments of degradation following defined UV dosages are performed, there is a fundamental lack of understanding regarding the intermediates, transient reactive species, and radicals formed during illumination, as well as their lifetimes and immediate impact post-illumination. In this study, we used light-coupled NMR spectroscopy to monitor in situ live spectral changes in sealed samples during and after UV-A illumination of different formulations of four mAbs without added photosensitizers. We observed a complex evolution of spectra, reflecting the appearance within minutes of transient radicals during illumination and persisting for minutes to tens of minutes after the light was switched off. Both mAb and excipient signals were strongly affected by illumination, with some exhibiting fast irreversible photodegradation and others exhibiting partial recovery in the dark. These effects varied depending on the mAb and the presence of excipients, such as polysorbate 80 (PS80) and methionine. Complementary ex situ high-performance size-exclusion chromatography analysis of the same formulations post-UV exposure in the chamber revealed significant loss of purity, confirming formulation-dependent degradation. Both approaches suggested the presence of degradation processes initiated by light but continuing in the dark. Further studies on photoreaction intermediates and transient reactive species may help mitigate the impact of light on biopharmaceutical degradation.

摘要

生物制药,如单克隆抗体(mAbs),需要在其整个生命周期的制剂中保持其化学和物理稳定性。已知 mAbs 暴露于光下,特别是 UV 光下,会引发化学和物理降解,而制剂中的痕量光敏剂会加剧这种降解。尽管对规定的 UV 剂量后降解进行了常规评估,但对于在光照过程中形成的中间体、瞬态反应性物质和自由基,以及它们的寿命和光照后的即时影响,仍然缺乏基本的了解。在这项研究中,我们使用光耦合 NMR 光谱法在没有添加光敏剂的情况下,监测不同 mAb 制剂在 UV-A 光照期间和之后的密封样品中的原位实时光谱变化。我们观察到光谱的复杂演变,反映了在光照过程中瞬态自由基出现的几分钟内,以及在关闭光后几分钟到几十分钟内持续存在的情况。mAb 和赋形剂信号都受到光照的强烈影响,有些表现出快速不可逆的光降解,而有些则在黑暗中部分恢复。这些影响取决于 mAb 和赋形剂的存在,如聚山梨酯 80(PS80)和蛋氨酸。在腔室内对相同制剂进行 UV 暴露后的原位高效尺寸排阻色谱分析,发现纯度显著损失,证实了制剂依赖性降解。这两种方法都表明存在由光引发但在黑暗中继续进行的降解过程。对光反应中间体和瞬态反应性物质的进一步研究可能有助于减轻光对生物制药降解的影响。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/83f1/11190875/8cf7ba13a8d1/ac4c01164_0001.jpg

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