Development of a microscale high throughput screening platform for the evaluation of biopharmaceutical photodegradation

• Applicant: Dr. Björn-Hendrik Peters
• Subject Area: Pharmacy
• Term: from 2016 to 2020
• Project identifier: Deutsche Forschungsgemeinschaft (DFG) - Project number 317009936

In order to ensure safety, efficacy and quality of biopharmaceutical drugs it is essential to stabilize the products against degradation induced by storage and stress factors, such as light. In particular, light stress gained increasing attention because photodegradation has been related to aggregation and immunogenicity.The proposed research project will develop a microscale high throughput screening (HTS) platform to investigate photoirradiation effects on relevant biopharmaceutical formulations in small scale at the solid state and in solution. A robust, microscale HTS platform is essential in order to systematically screen numerous, complex formulations and to assess a broad range of critical quality attributes in a short time. The combined HTS platform and mass spectrometry (MS) approach provides a solution to these unmet screening needs already at early-stage development by minimizing material consumption and the utilization of a highly sensitive analytical method. Due to the current lack of such sensitive analytical methods, potentially harmful photodegradation was often not analyzed. This research project will evaluate the influence commonly used biopharmaceutical formulation additives on the photodegradation of three photolabile therapeutics and the capability of novel photostabilizers to reduce such photodegradation.Degradation products will be identified using an Xtreme Ultra-Pressure Chromatography / MS System. Further characterization of photodegradation products will be performed using size exclusion high performance liquid chromatography (SE-HPLC) and reverse phase high performance liquid chromatography (RP-HPLC). Solid state samples will be prepared by freeze-drying. The development of the freeze-drying process will be guided by differential scanning calorimetry (DSC). Freeze-dried samples will be characterized by Karl Fischer titration (KF), and X-ray diffraction (XRD).The successful development of this novel HTS platform will provide an opportunity for future scientific projects and academic collaborations in the field of protein and peptide stability. The successful development of this HTS platform will furthermore provide an opportunity for technology transfer between academic and industrial partners and the development of professional research services.

• DFG Programme: Research Fellowships
• International Connection: USA
• Host: Professor Dr. Christian Schöneich