Recent and rapid progress in the field of biotechnology has resulted in an increasing number of novel macromolecular drugs with great promise for further advanced research and clinical application. However, the delivery of these macromolecular drugs by routes other than the parenteral route is difficult. The pipeline of macromolecular drugs derived from biotechnology presents a challenging opportunity to develop practical dosage forms that could be dosed via the oral route. Given this, the successful oral delivery of macromolecular drugs presents an enormous opportunity. Oral Delivery of Macromolecular Drugs will provide an overview of the innovative oral delivery technologies that have demonstrated success in human testing and will go on to cite the challenges, strategies, and future trends that are to be expected.