Trehalose: A Powerful Excipient in the Formulation Toolbox – Product Information

Trehalose is a non-reducing disaccharide consisting of two glucose molecules linked by an α,α–1,1 glycosidic bond. In the pharmaceutical industry, products that benefit from the stabilizing effects of trehalose include, but are not limited to: monoclonal antibodies (mAbs), antibody drug conjugates (ADCs), fusion proteins, peptides, stem cells, and vaccines. Table 1 is a brief list of drugs that include trehalose as a component of their formulations.

Many of the stabilizing effects of trehalose are derived from its unique properties. The glass transition temperature (T_g) is between 110°C and 120°C, which is the highest of the disaccharides. Formulations lyophilized in a glassy amorphous matrix of trehalose can be stored at higher temperatures without concern of negative consequences associated with molecular mobility, since molecular mobility is negligible upon storage 50°C below the T_g of the amorphous matrix. Primary drying during lyophilization should be below the freeze concentration glass transition temperature (T_g’) to prevent cake collapse. In comparison to sucrose, the T_g’ of trehalose is about 3°C higher, translating to an ~13% reduction in primary drying time for every 1°C difference in T_g’. Trehalose itself is intrinsically stable and is not susceptible to breakdown to reducing sugars, since the free energy of the glycosidic bond is <1 kcal/mol. Formulation at pH below 5 is also possible with trehalose. After 1 hour in solution at pH 3.5, >99% of trehalose remains compared to ~0% sucrose remaining in the same conditions.

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Source: Drug Development and Delivery

Ben Nelson, PhD, and Chris Wilcox, Trehalose: A Powerful Excipient in the Formulation Toolbox, https://drug-dev.com/trehalose-a-powerful-excipient-in-the-formulation-toolbox/