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Proteins and peptides are involved in a wide range of vital functions and processes in the body that are essential for life. Proteins and peptides also have various roles in pathological conditions such as cancer and diabetes. Therefore, the use of proteins and peptides as therapeutic agents is considered as an attractive approach to combating various diseases. However, the physicochemical properties of proteins and peptides make them challenging for exogenous administration, especially by the oral route of administration. Various protein/peptide drug delivery systems have been extensively investigated to overcome the problems associated with the exogenous administration of protein and peptide therapeutics. In this chapter, different approaches for the delivery of proteins and peptides are discussed including chemical modifications, absorption enhancers, carrier systems, and various other approaches.