The Bombay Technologist

Enhancing the Oral Delivery of Proteins and Peptide Drugs

Aditya Kulkarni

Divya Vasudevan

Keywords: Peptides, Gastrointestinal Tract, Paracellular Transport, Colon-Specific Drug Delivery.

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Abstract

Many peptides and proteins possess biological activity that makes them potent therapeutics - particularly anticancer agents and hormones. Oral delivery of peptide drugs is preferred over other routes of administration due to better patient compliance. However, the use of many polypeptides as therapeutic agents is hampered by their rapid elimination from the circulation because of enzymatic degradation in the gastrointestinal tract (GIT), renal filtration, uptake by the reticuloendothelial system (RES) and accumulation in non-targeted organs and tissues. This therefore rcQuires large doses of polypeptide administration, which frequently results in non-specific toxicity and increased cost of the treatment. This review focuses on the challenges posed by the Gl system and how different pharmaceutical approaches can be used to make oral delivery of protein and peptide drugs more feasible. It also covers paracellular transport of the drug following oral delivery. The properties of the colon such as high pH conditions, presence of microbial flora etc are being exploited to use the colon as a specific site for delivery of peptide drugs. The review throws light not only on this area but also encompasses current approaches adopted by pharmaceutical companies to produce orally administered peptide drugs.