PEGylation is a process in which a polyethylene glycol (PEG) chain is covalently conjugated to an active therapeutic (often a peptide, small protein, or an antibody fragment) in order to enhance solubility, reduce immunogenicity and/or prolong circulating half-life in the body. For biotherapeutics, most of which must be administered by injection due to poor oral absorption, the reduction in dose frequency afforded by an extended in-vivo half-life can provide significant advantage in terms of patient convenience, especially for indications requiring chronic treatment. However, PEGylated proteins can also present a number of special challenges during formulation development. These challenges may include potential for chemical instability of the conjugate and, in case of subcutaneous products where injection volumes are limited, increased intrinsic viscosity, which can pose challenges for processing of drug substance and make injection through a fine-gauge needle difficult. In this presentation, we will discuss formulation development of a small PEGylated protein and strategies used to address stability- and viscosity-related challenges to enable a viable drug product suitable for subcutaneous use.

Considerations in formulation development of a PEGylated protein

ACS Fall 2020 Virtual Meeting

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