Sucrose and Trehalose in Therapeutic Protein Formulations

Sucrose and trehalose are key ingredients in the formulation and stabilization of biotherapeutics. Their utility and function is driven by their unique chemical and physical properties, especially in aqueous solutions which are summarized in this chapter. There are commonalities as well as differences in these properties that arise from their conformation, H-bonding characteristics, water-binding ability, glass transition temperatures, polymorphic behavior, solubility, chemical stability etc. Both sugars are well suited to provide solution-state stabilization, as well as cryo- and lyo-protection, for therapeutic proteins as excipients in the formulations. Compendial monographs are available for both sugars, and the safety and tolerability have been well documented. Although the final assessment is dependent on the individual biotherapeutic, experience suggests that sucrose can generally be considered as suitable in most cases, unless constrained by a low-pH formulation.