The final aim/target of Pharmaceutical Sciences is to design successful dosage forms for effective therapy, considering individual patient needs and compliance. Development of new drug entities, particularly using peptides and proteins, is growing in importance and attracting increased interest, as they are specifically effective at a comparably low dose. These very potent and specific peptides and proteins can now be produced in large quantities due to increased knowledge and advancements in biotechnological and pharmaceutical applications. A number of peptide and protein products are now available on the market, and numerous studies investigating them have been published in the literature. Although many peptide/protein like products are generally designed for parenteral administration, some other noninvasive routes have also been used. For example, desmopressin is delivered nasally and deoxyribonuclease by inhalation. Although peptides and proteins are generally orally inactive, cyclosporine is an exception. In order to design and develop long-acting, more effective peptide/protein drugs, the controlled release mechanisms and effective parameters need to be understood and clarified. Therefore, we review herein various peptide/protein delivery systems, including biodegradable and nondegradable microspheres, microcapsules, nanocapsules, injectable implants, diffusion- controlled hydrogels and other hydrophilic systems, microemulsions and multiple emulsions, and the use of iontophoresis or electroporation, and discuss the results of recent researches.