Lehrstuhl für Technische Thermodynamik (LTT), Friedrich-Alexander-Universität Erlangen-Nürnberg (FAU), D-91058 Erlangen, Germany.
Erlangen Graduate School in Advanced Optical Technologies (SAOT), Friedrich-Alexander-Universität Erlangen-Nürnberg (FAU), D-91058 Erlangen, Germany.
Sensors (Basel). 2022 Feb 1;22(3):1111. doi: 10.3390/s22031111.
Drying processes such as spray drying, as commonly used in the pharmaceutical industry to convert protein-based drugs into their particulate form, can lead to an irreversible loss of protein activity caused by protein secondary structure changes. Due to the nature of these processes (high droplet number, short drying time), an in situ investigation of the structural changes occurring during a real drying process is hardly possible. Therefore, an approach for the in situ investigation of the expected secondary structural changes during single droplet protein drying in an acoustic levitator by time-resolved Raman spectroscopy was developed and is demonstrated in this paper. For that purpose, a self-developed NIR-Raman sensor generates and detects the Raman signal from the levitated solution droplet. A mathematical spectral reconstruction by multiple Voigt functions is used to quantify the relative secondary structure changes occurring during the drying process. With the developed setup, it was possible to detect and quantify the relative secondary structure changes occurring during single droplet drying experiments for the two chosen model substances: poly-L-lysine, a homopolypeptide widely used as a protein mimic, and lysozyme. Throughout drying, an increase in the β-sheet structure and a decrease in the other two structural elements, α-helix, and random coil, could be identified. In addition, it was observed that the degree of structural changes increased with increasing temperature.
干燥过程,如喷雾干燥,在制药工业中常用于将基于蛋白质的药物转化为颗粒形式,但会导致蛋白质二级结构变化引起的蛋白质活性不可逆丧失。由于这些过程的性质(高液滴数量、短干燥时间),很难在原位研究实际干燥过程中发生的结构变化。因此,本文开发了一种在声悬浮器中通过时间分辨拉曼光谱原位研究单液滴蛋白质干燥过程中预期二级结构变化的方法,并进行了验证。为此,自行开发的近红外拉曼传感器从悬浮溶液液滴中产生和检测拉曼信号。通过多个 Voigt 函数的数学光谱重建来定量分析干燥过程中发生的相对二级结构变化。使用所开发的装置,能够在两个选定的模型物质的单液滴干燥实验中检测和定量分析相对二级结构变化:聚-L-赖氨酸,一种广泛用作蛋白质模拟物的同聚多肽,以及溶菌酶。在整个干燥过程中,可以识别β-折叠结构的增加和其他两种结构元素α-螺旋和无规卷曲的减少。此外,还观察到结构变化的程度随温度的升高而增加。