Introduction into Formulation Development of Biologics

  • Daniel Weinbuch
  • Andrea Hawe
  • Wim Jiskoot
  • Wolfgang FriessEmail author
Part of the AAPS Advances in the Pharmaceutical Sciences Series book series (AAPS, volume 38)


Formulation development is an essential part of every biopharmaceutical development program and important for the therapeutic and commercial success of a protein drug product by assuring the quality, safety, and efficacy. The multiple phases of formulation development interact with other product development exercises as early as discovery research all the way until and beyond market approval. Every drug product demands a tailor-made formulation, due to the complexity of different degradation pathways potentially affecting product stability, the specific characteristics of the individual drug molecule, special patient needs, and even marketing considerations. Formulation development can be approached using various strategies, based on a rational design, relying on scientific knowledge in low or medium throughput, or high-throughput formulation screening of hundreds or even thousands of conditions employing miniaturized analytical methods. In this chapter, an introduction to the field of protein formulation development is given, the literature on current protein formulation development strategies is reviewed, and current challenges are summarized.


Protein stability Stability testing Preformulation High throughput screening Excipients Development strategy 

List of Abbreviations


Asymmetrical flow field-flow fractionation


Active pharmaceutical ingredient


Analytical ultracentrifugation


Clinical trial authorization


Dynamic light scattering


Deoxyribonucleic acid


Design of experiment


Drug product


Drug substance


Differential scanning calorimetry


Differential scanning fluorimetry


Fourier-transform infrared


Glutamic acid


Good manufacturing practice




Hydrogen peroxide




High-performance liquid chromatography


High-throughput formulation


International conference on harmonization


License application


Liquid chromatography-coupled mass spectrometry


Milligram per milliliter








Potential of hydrogen


Isoelectric point


Acid dissociation constant


Quality control


Relative humidity


Ribonucleic acid


Rounds per minute


Size exclusion chromatography


Static light scattering


Glass transition temperature


Ultrahigh-performance liquid chromatography


United States Pharmacopeia




Degrees Celsius




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Further Reading

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Copyright information

© American Association of Pharmaceutical Scientists 2018

Authors and Affiliations

  • Daniel Weinbuch
    • 2
    • 3
  • Andrea Hawe
    • 2
  • Wim Jiskoot
    • 3
  • Wolfgang Friess
    • 1
    Email author
  1. 1.Department of Pharmacy—Pharmaceutical Technology and BiopharmaceuticsLudwig-Maximilians-Universität MünchenMunichGermany
  2. 2.Coriolis Pharma Research GmbHMartinsriedGermany
  3. 3.Division of BioTherapeutics, Leiden Academic Centre for Drug ResearchLeiden UniversityLeidenThe Netherlands

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