Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10162181 | Journal of Pharmaceutical Sciences | 2015 | 6 Pages |
Abstract
Noncovalent PEGylation has great potential for stabilization of therapeutic proteins. Here, we demonstrated that the noncovalent PEGylation with a PEGylated polyelectrolyte stabilized a therapeutic protein, l-asparaginase (ASNase). Anionic ASNase and cationic poly(ethylene glycol)-block-poly(N,N-dimethylaminoethyl methacrylate) (PEG-b-PAMA) formed a water-soluble protein-polyelectrolyte complex (PPC) without loss of secondary structure and enzyme activity. PPC with PEG-b-PAMA successfully inhibited the shaking-induced inactivation and aggregation of ASNase as well as protease digestion, corresponding to the behaviors of covalently PEGylated ASNase. Thus, noncovalent PEGylation by PEGylated polyelectrolytes is a new candidate for handling of therapeutic proteins. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 104:587-592, 2015
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Authors
Takaaki Kurinomaru, Kentaro Shiraki,