Elsayed Yomnah Y, Kühl Toni, Dauer Katharina, Sayin Alina, Wagner Karl G, Imhof Diana
Department of Pharmaceutical Biochemistry and Bioanalytics, Pharmaceutical Institute, University of Bonn, An der Immenburg 4, Bonn D-53121, Germany.
Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Ain Shams University, Organization of African Unity Street, Cairo 11566, Egypt.
ACS Omega. 2022 Nov 1;7(45):40836-40843. doi: 10.1021/acsomega.2c03559. eCollection 2022 Nov 15.
Structural and functional integrities of formulated proteins are key characteristics that provide a better understanding of influencing factors and their adjustment during formulation development. Here, the procedures commonly used for protein analysis were applied and optimized to obtain a higher degree of accuracy, reproducibility, and reliability for the analysis of lysozyme extracts from hot-melt extrudates (HME). The extrudates were prepared with polyethylene glycol 20 000. The test lysozyme HMEs were subjected to extraction procedures and analytical methods following the International Council of Harmonization guidelines for testing the active protein ingredient Q 1 A (R2) in its pure and formulated form. Therefore, reversed-phase high-pressure liquid chromatography, sodium dodecyl sulfate-polyacrylamide gel electrophoresis, matrix-assisted laser desorption ionization mass spectrometry, and fluorescence-based activity measurements were applied to study lysozyme stability and function after formulation. Long-term accelerated stability studies were performed for the pure and formulated protein. Our findings revealed a high degree of stability for lysozyme toward different temperatures and storage times, confirming that HME is a suitable formulation alternative that preserves lysozyme's properties and stability. The presented methods and workflow are recommended to be exploited for further protein drugs to assess usability and compatibility concerning different pharmaceutical applications.
制剂蛋白质的结构和功能完整性是关键特性,有助于更好地理解制剂开发过程中的影响因素及其调控。在此,应用并优化了常用于蛋白质分析的程序,以提高对热熔挤出物(HME)中溶菌酶提取物分析的准确性、重现性和可靠性。挤出物用聚乙二醇20000制备。按照国际协调理事会关于测试活性蛋白成分Q1A(R2)纯品和制剂形式的指导原则,对测试用溶菌酶HME进行提取程序和分析方法研究。因此,采用反相高效液相色谱、十二烷基硫酸钠-聚丙烯酰胺凝胶电泳、基质辅助激光解吸电离质谱和基于荧光的活性测量来研究制剂后溶菌酶的稳定性和功能。对纯品和制剂形式的蛋白质进行了长期加速稳定性研究。我们的研究结果表明溶菌酶在不同温度和储存时间下具有高度稳定性,证实HME是一种合适的制剂替代方法,可保持溶菌酶的性质和稳定性。建议将所介绍的方法和工作流程用于进一步的蛋白质药物,以评估其在不同药物应用中的可用性和兼容性。