Gastrointestinal patch systems with integrated multifunctions could surmount the challenges associated with conventional drug delivery. Several gastrointestinal patch systems provide bioadhesion, drug protection and unidirectional release. This combination of function could improve the overall oral bioavailability of large molecules that can currently be delivered only by injection, for example, epoetin-alpha and granulocyte-colony-stimulating factor, which are commonly used to treat chemotherapy-associated anemia and leukopenia, respectively. Furthermore, self-regulated release and cell-specific targeting provide additional 'smart' characteristics to this innovative therapeutic platform.