Carboxymethyl high amylose starch for F4 fimbriae gastro-resistant oral formulation.

The carboxymethyl high amylose starch (CM-HAS) was proposed as excipient able to protect F4 fimbriae oral vaccine against gastric acidity and pepsin, allowing its subsequent liberation in the intestinal fluid. Thus, F4 fimbriae formulated with CM-HAS as tablets displayed a markedly higher stability after 2h of incubation in simulated gastric fluid (containing pepsin) than the free, non-protected F4 fimbriae, which, in these conditions, were almost completely digested after 120 min. In the presence of pancreatin (with alpha-amylase, lipase and proteolytic activities) in simulated intestinal conditions, the F4 fimbriae were liberated from CM-HAS tablets over a period of up to 5 h. The presence of pancreatin in intestinal medium did not affect the structural stability of the F4 fimbriae major subunits. Thus, F4 fimbriae formulated with CM-HAS would retain their receptor binding activity essential for the induction of an intestinal mucosal immune response.