Delivery Systems for Peptide Drugs: (125 NATO Science Series A:)

Recent years have seen enormous advances in the field of protein and peptide engineering and a greater understanding in the way in which biological response modifiers function in the body. It is now possible through the use of recombinant DNA techniques, or by solid phase protein synthesis, to produce significant quantities of a wide variety of regulatory agents that are therapeutically applicable. The list of these response modifiers expands almost daily to include interferons, macrophage activation factors, neuropeptides and agents that may have potential in cardiovascular disease, inflammation, contraception etc. Prospects to use some of these materials in medicine have reached the stage where products have either been approved by regulatory authorities or are the subject of applications as investigatory drugs or as new therapeutic agents. In some uses the pertinent agent will be administered on an acute basis in the form of a simple injection, as, for example, the use of a tissue plasminogen activator for the treatment of coronary infarct. In other cases regulatory proteins and peptides are indicated for chronic therapy and here they will need to be administered by an appropriate delivery system. Unfortunately, the research on delivery systems for peptides and proteins has not kept pace with the rapid progress in biotechnology and, consequently, there are presently few systems that are entirely appropriate for the administration of macromolecular drugs according to complex dosage regimens, (eg intermittent and pulsed therapy). Furthermore essential pharmacokinetic and pharmacodynamic data may be missing.

Table of Contents:
Advanced Delivery Systems for Peptides and Proteins — Pharmaceutical Considerations.- Biotechnology and Protein Production.- Peptide Analysis: Critical Technology for Evaluating Delivery Approaches.- Bioreversible Derivatization of Peptides.- An Approach to Target Therapy. Synthesis and Biological Activity of Hydrophobic and Hydrophilic Enkephalin Analogues.- Temporal and Pharmacokinetic Aspect in Delivery of Peptides and Proteins.- Enzymatic Barriers to Peptide and Protein Absorption and the Use of Penetration Enhancers to Modify Absorption.- Intracellular Sorting of Proteins.- Biodegradable Polymers for Sustained Release of Polypeptides.- Controlled Delivery of Nafarelin, an Agonistic Analogue of LHRH, From Microspheres of Poly (D, L Lactic-Co-Glycolic) Acid.- The Oral Bioavailability of Peptides and Related Drugs.- Oral Delivery of Peptide Drugs.- Drug Delivery of Peptides: The Buccal Route.- Enhanced Absorption and Lymphatic Transport of Macromolecules via the Rectal Route.- Biopharmaceutical Aspects on the Intranasal Administration of Peptides.- Microspheres as a Potential Controlled Release Nasal Drug Delivery System.- NazlinR — Transnasal Systemic Delivery of Insulin.- Nasal Absorption of Enkephalins in Rats.- Intranasal Delivery of the Peptide, Salmon Calcitonin.- Metabolic Effects of Intranasally Administered Insulin and Glucagon in Man.- Human Calcitonin Administered by the Nasal Route: Bioavailability of Different Formulations and Efficacy in Post-Menopausal Osteoporosis.- Routes of Administration for Polar Compounds of Moderate Molecular Weight with Particular Reference to Analogues of Somatostatin.- The Transdermal Route for the Delivery of Peptides and Proteins.- Controlled-Release and Localized Targeting of Interferons.- Delivery of MacrophageActivating Factors by Means of Liposomes.- Activators of Plasminogen.- Biosynthetic Human Growth Hormone Identical to Authentic Material.- Delivery Systems for Recombinant Methionyl Human Growth Hormone.- Eledoisin and Ceruletide, Two Naturally Occurring Peptide Drugs of Nonmammalian Origin.- Consideration of the Proteins and Peptides Produced by New Technology for use as Therapeutics.- Key Issues in the Delivery of Peptides and Proteins.- Photo.- Contributors.