The intestinal mucus protects poly(isobutylcyanoacrylate) nanoparticles from enzymatic degradation

Poly(alkylcyanoacrylate) nanoparticles are of interest as possible carriers for the controlled release of drugs. For several drugs, they have shown si gnificant enhancements in their bioavailability when administered orally. T he aim of this study was to investigate the influence of several media (in vitro and ex vivo) present in the gastro-intestinal tract on the stability of poly(isobutylcyanoacrylate) nanoparticles. Poly(isobutylcyanoacrylate) n anoparticles were proven to be stable in a gastric environment, and bioerod able in a simulated intestinal medium. Esterase caused a rapid degradation of the nanoparticles that was proportional to the amount of enzyme added to the medium. These results were confirmed when using media extracted from r at intestine. Degradation in the media corresponding to the luminal content of the proximal part of the intestine was intense while it was lowered in the distal part of the intestine. However, extracted mucus had a much lower enzymatic activity, suggesting that the mucus could provide an efficient p rotecting layer when nanoparticles are entrapped in it by a mucoadhesion ph enomenon.