The challenges of oral drug delivery via nanocarriers

AbstractThe oral application of pharmaceuticals is unarguably the most convenient method of application. Especially for protein- or peptide-based drugs, however, the effectiveness is significantly reduced due to enzymatic digestion in the stomach as well as a poor bioavailability in the small intestine. For these difficult formulations, the encapsulation into nanocarriers would protect the sensitive drug and thus could considerably improve the efficiency of oral drug delivery. In the last years, many candidate biodegradable nanomaterials for such carrier systems have been published. However, before the cargo can be released, the nanocarrier needs to cross multiple barriers of the human body, including a layer of intestinal mucus and epithelial as well as endothelial cells. For overcoming these cellular barriers, transcytosis is favored over a paracellular transport for most nanomaterials as paracellular transport routes lack selectivity of transported molecules once opened up. The exact mechanisms behind ...