Abstract
Basic fibroblast growth factor(bFGF)is a prototype of heparin-binding growth factor family and could play a crucial role in wound healing processes. Water-insoluble aluminum salts of cyclodextrin sulfates (Al·CyD-Suls) were prepared, and their potential use in oral formulations of bFGF intended for treatment of gastrointestinal ulcers was investigated. Adsorbates of bFGF with Al·CyrD-Suls were prepared by incubating the growth factor with a suspension of Al·CyD-Suls in water. The mitogenic activity of bFGF released from the adsorbate was almost comparable to that of the intact bFGF. Al·CyD-Suls significantly protected bFGF against proteolytic degradation by pepsin, compared with their sodium salts and other sulfated oligosaccharides tested. The in vitro release of bFGF from the Al·β-CyD-Sul adsorbate into isotonic phosphate buffer (pH 7.4) was sustained in proportion to a rise in the ratio of Al·βCyD-Sul to the growth factor. The oral administration of the adsorbate of bFGF with Al·β-CyD-Sul had the most prominent healing effects on acetic acid-induced gastric ulcers. These results suggest that Al·CyD-Suls may potentiate the healing effect of bFGF by both stabilizing and anchoring the growth factor at the site where its action is desired.
