Improvement of Drug Therapy by Covalent PEG Conjugation: An Overview From a Research Laboratory

Abstract

AbstractIn the last two decades, efforts focused in the field of drug delivery have made it possible to reach important goals, especially with proteins and peptides. The story of the evolution of this matter is vast and it is difficult to summarize its various aspects in a single review. On the other hand, it could be really interesting to look at the inside story of a typical academic research lab that has dedicated almost all its resources to drug delivery. In our case, an initial interest in the issue of protein conformation stability soon paved the way for a new area of study: the modification of proteins with synthetic polymers. We have seen this technique transformed from a crude and inhomogeneous procedure into a well‐recognized and successful approach. This great advance has been possible thanks to the development of dedicated chemical coupling methods and to the better understanding of the behavior of polymers in vivo. In particular, among the several polymers investigated, PEG has became the best polymer for protein modification. Exploiting the unique properties of this polymer, we have conducted several investigations in the field of protein PEGylation and then transferred the acquired know‐how to the development of conjugates with low molecular weight drug. This last aspect still presents several unmet needs that are awaiting proper solutions.