Synthesis and Physical Characterization of Poly(ethylene glycol)-Gelatin Conjugates

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• 作者：Toshihiro Kushibiki ; Hideki Matsuoka ; and Yasuhiko Tabata
• 刊名：Biomacromolecules
• 出版年：2004
• 出版时间：January 2004
• 年：2004
• 卷：5
• 期：1
• 页码：202 - 208
• 全文大小：123K
• 年卷期：v.5,no.1(January 2004)
• ISSN：1526-4602

文摘

Poly(ethylene glycol) (PEG) with the terminal group of active ester was coupled to the amino group ofgelatin to prepare PEG-grafted gelatin (PEG-gelatin). The affinity chromatographic study revealed that thePEG-gelatin with high degrees of PEGylation did not adsorb onto the gelatin affinity column, in remarkedcontrast to gelatin alone and the PEG-gelatin with low PEGylation degrees. The former PEG-gelatin showeda critical micelle concentration while it had the apparent molecular size of about 100 nm and a surfacecharge of almost zero. These findings indicate that the PEG-gelatin formed a micelle structure of which thesurface is covered with PEG molecules grafted. When the body distribution of ¹²⁵I-labeled gelatin and PEG-gelatin after intravenous injection was evaluated, the radioactivity of micellar PEG-gelatin was retained inthe blood circulation compared with that of gelatin and the PEG-gelatin of no micelle formation. At thesame PEGylation degree, the blood concentration was significantly higher for the PEG-gelatin preparedfrom PEG with a molecular weight of 12 000 than that of molecular weights of 2000 and 5000. It is concludedthat the PEG-gelatin is a drug carrier with a micelle structure which retains in the blood circulation.