Polymers for Protein Conjugation

Abstract

Polyethylene glycol (PEG) at the moment is considered the leading polymer for protein conjugation in view of its unique properties, as well as to its low toxicity in humans, qualities which have been confirmed by its extensive use in clinical practice. Other polymers that are safe, biodegradable and custom-designed have, nevertheless, also been investigated as potential candidates for protein conjugation. This review will focus on natural polymers and synthetic linear polymers that have been used for protein delivery and the results associated with their use. Genetic fusion approaches for the preparation of protein-polypeptide conjugates will be also reviewed and compared with the best known chemical conjugation ones.

Smart polymers in drug delivery systems on crossroads: Which way deserves following?

“…The conjugation of polymers to drugs is a well-established strategy in drug delivery to enhance the solubility of the drug and increase the circulation time in the body, while at the same time lowering the immunogenicity [29]. The versatility and potential of PEtOX as an alternative to PEO were also demonstrated for both protein and smalldrug conjugates; comparable results were obtained for PEtOX and PEO in regard to, for example, protein-rejecting properties, drug-release profile, and in vitro cytotoxicity [75][76][77][78].…”

Self-assembly of bioactive peptides, peptide conjugates, and peptide mimetic materials

“…For example, although PEG is often considered an "inert" polymer, high molar mass PEG is not degraded in vivo and can cause toxicity, as can high doses of PEG polymers of low molar mass. [82][83][84][85] Immunogenic response to PEG has been reported. 84,86 Furthermore, synthetic PEG may contain impurities or unreacted monomer which is highly toxic.…”

Biobetters

“…This developing area is considered as one of the most important breakthroughs in biological drug development (Pasut 2014b ), offering multiple advantages over the chemical coupling with synthetic polymers. In particular, two distinct technologies have emerged, PASylation ® ) and XTEN ™ (Schellenberger et al 2009 ), which both employ recombinant polypeptides to mimic the size-enlarging effect of PEG for plasma half-life extension.…”