Journal
INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 204, Issue 1-2, Pages 111-116Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/S0378-5173(00)00489-0
Keywords
Bowman-Birk protease inhibitor; polypeptide lipidization; gastric retention; gastrointestinal absorption
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Bowman-Birk protease inhibitor (BBI) was modified with a reversible lipidizing agent. The palmitoylated product, Pal-BBI, and BBI were iodinated and orally administered to mice using a gavage needle. A prolonged retention of Pal-BBI was found in the stomach. Furthermore, a significant amount of Pal-BBI was detected as intact polypeptide in the stomach of mice fed with Pal-BBI, while only degradation products were detected with BBI. There was also a significant increase of radioactivity in the blood and liver in mice 1.5 h post-administration of Pal-BBI. These results indicate that lipidized polypeptide can have a longer retention and lower digestion in the stomach. They also suggest that the Pal-BBI may have a higher gastrointestinal absorption than the origin;ll polypeptide. (C) 2000 Elsevier Science B.V. All rights reserved.
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