Gastric retention and stability of lipidized Bowman-Birk protease inhibitor in mice.

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 original polypeptide.