Protein therapeutics include over 180 FDA approved drugs and represent a growing pipeline. However, macromolecular drugs generally display suboptimal pharmacokinetic profiles and may possess undesirable inherent immunogenicity. This can be generally addressed through the PEGylation technology, wherein polyethylene glycol (PEG) is chemically conjugated to the protein to impart a steric barrier that shields it from the immune system thereby prolonging half-life and reducing immunogenicity. However, non-biodegradable PEG imposes size limitations on such macromolecular assemblies and requires chemical conjugation, which can result in undesirable reaction byproducts. We developed a series of novel water-soluble polyphosphazene carriers with PEG pendant groups that are biodegradable under physiological conditions and form non-covalent complexes with proteins. In vitro experiments proved that polyphosphazenes could effectively suppress immunogenicity of proteins, improve their thermal stability and dramatically increase their molecular sizes.

Biodegradable polyphosphazene systems for non-covalent PEGylation of proteins

254th National Meeting (2017)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.