The production of high-value pharmaceutical proteins and peptides in transgenic plants is an attractive and economically feasible alternative to conventional mammalian cell, yeast, and bacterial systems. In contrast to vegetative tissues, rice seeds allow higher accumulation of recombinant proteins and long-term stable storage. Rice is not only consumed as a staple food by a majority of the world's population, but is also used as a model monocot for biotechnological manipulation. Daily oral consumption of transgenic rice seeds that accumulate high concentrations of food-derived or synthetic bioactive peptides can be expected to provide a safe, reliable, and consistent oral delivery system that would contribute to the promotion of human health care.