Bešić Erim, Rajić Zrinka, Šakić Davor
University of Zagreb Faculty of Pharmacy and Biochemistry 10000 Zagreb, Croatia.
Acta Pharm. 2025 Jan 9;74(4):551-594. doi: 10.2478/acph-2024-0037. Print 2024 Dec 1.
Electron paramagnetic resonance (EPR) spectroscopy has long been established across various scientific disciplines for characterizing organic radicals, organometallic complexes, protein structures and dynamics, polymerization processes, and radical degradation phenomena. Despite its extensive utility in these areas, EPR spectroscopy's application within pharmaceutical science has historically been constrained, primarily due to factors such as high equipment costs, a steep learning curve, complex spectral deconvolution and analysis, and a traditional lack of emphasis on single-electron chemistry in pharmaceutical research. This review aims to provide a thorough examination of EPR spectroscopy's applications in analyzing a wide array of para-magnetic species relevant to pharmaceutical research. We detail how EPR spectroscopy can be employed to assess free radical scavenging properties in pharmaceutical compounds, elucidate drug mechanisms of action, and explore pharmacokinetics. Additionally, we investigate the role of free radicals in drug-induced toxicity and drug-membrane interactions, while also covering the application of EPR spectroscopy in drug delivery research, advanced studies of metallodrugs, and monitoring of oxygen levels in biological systems through EPR oximetry. The recent advancements in the miniaturization of EPR spectro meters have paved the way for their application in and mo nitoring during the manufacturing process and quality control of pharmaceutical substances and final drug formulations due to being the only direct and non-invasive detection technique for radical detection. Through these discussions, we highlight the substantial contributions of EPR spectroscopy to the advancement of pharmaceutical sciences.
电子顺磁共振（EPR）光谱长期以来在各个科学领域中都已确立，用于表征有机自由基、有机金属配合物、蛋白质结构与动力学、聚合过程以及自由基降解现象。尽管EPR光谱在这些领域具有广泛的用途，但其在药学领域的应用在历史上一直受到限制，主要是由于设备成本高、学习曲线陡峭、光谱反卷积和分析复杂以及药学研究中传统上对单电子化学缺乏重视等因素。本综述旨在全面考察EPR光谱在分析与药学研究相关的各种顺磁物种方面的应用。我们详细介绍了如何利用EPR光谱评估药物化合物中的自由基清除特性、阐明药物作用机制以及探索药代动力学。此外，我们研究了自由基在药物诱导的毒性和药物 - 膜相互作用中的作用，同时还涵盖了EPR光谱在药物递送研究、金属药物的深入研究以及通过EPR血氧测定法监测生物系统中的氧水平方面的应用。EPR光谱仪小型化的最新进展为其在药物物质和最终药物制剂的制造过程及质量控制中的应用和监测铺平了道路，因为它是唯一用于自由基检测的直接且非侵入性的检测技术。通过这些讨论，我们强调了EPR光谱对药学科学发展的重大贡献。
