The pH-Dependent Formation of PEGylated Bovine Lactoferrin by Branched Polyethylene Glycol (PEG)-N-Hydroxysuccinimide (NHS) Active Esters(Miscellaneous)
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概要
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PEGylation is an established method for improving the pharmacokinetic properties and pharmacodynamic effects of therapeutic proteins. Amino conjugation by N-hydroxysuccinimide activated polyethylene glycol (PEG-NHS) represents the most common modification of the target proteins. In this study, we compared the reaction velocities of pH-dependent preparations of bovine lactoferrin modified with branched PEG-NHS conducted at pH7.4 to pH9.0. PEGylation reaction rates were dependent on pH value, but not on PEG molecular mass. At pH7.4, reactions advanced gradually and reached steady state by 2h, whereas at pH9.0, reactions advanced very quickly and reached steady state within 10min. Hydrolysis half-life of PEG-NHS exceeded 120min at pH7.4, but was below 9min at pH9.0. Thus, the pH value is one of the most important factors to obtain the optimal condition for PEGylation by NHS esters.
- 2009-03-01
著者
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Nojima Yasuhiro
School Of Bioscience And Biotechnology Tokyo University Of Technology:(present Office)department Of
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SATO Atsushi
School of Bioscience and Biotechnology, Tokyo University of Technology
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Suzuki Yosuke
Department Of Clinical Pharmacy Oita University Hospital
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IGUCHI Kazuma
School of Bioscience and Biotechnology, Tokyo University of Technology
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SUZUKI Yosuke
School of Bioscience and Biotechnology, Tokyo University of Technology
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Iguchi Kazuma
School Of Bioscience And Biotechnology Tokyo University Of Technology
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Suzuki Yosuke
School Of Bioscience And Biotechnology Tokyo University Of Technology
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Sato Atsushi
School Of Bioscience And Biotechnology Tokyo University Of Technology
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Sato Atsushi
School Of Bionics Tokyo University Of Technology
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