Oral insulin delivery for treatment of diabetes mellitus


  • Durga Devi K Department of Pharmaceutics, JNTUK Science and Technologies and School of Pharmacy.




Proteins, permeations enhancers, enteric coatings, polymer micro-sphere


Diabetes mellitus is characterized by a condition known as hyperglycemia which may be controlled through medication and insulin. Current insulin therapy for diabetes mellitus involves frequent dosing of subcutaneous injections, causing local discomfort, patient incompliance, hypoglycemia, and hyperinsulinemia, among others, one of the approaches to overcoming these issues is to administer insulin through oral route. An oral form of insulin has been the elusive goal for many investigators since the protein initial discovery by Banting and Best in 1922. Oral delivery of insulin is one of the promising and anticipated areas in the treatment of diabetes, primarily because it may significantly improve the quality of life of patients who receives insulin regularly. However, there are several challenges in developing an oral route for insulin delivery; include low bioavailability due to rapid enzyme degradation in the stomach, inactivation, and digestion by proteolytic enzymes in the intestinal lumen, poor permeability, and poor stability. Several companies have developed technology platforms that protect polypeptides and proteins from enzymatic hydrolysis, enable their transport across the epithelial lining, and promote their absorption from the GI tract. Most notably, the use of permeation enhancers, protease inhibitors, enteric coatings, and polymer microsphere formulation will be covered, including commentary on which methods hold more promise towards the successful development of oral insulin. This review, considers the current literature on the advances, methods, needs, and challenges in the development of oral insulin.


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Pedro Fonte, Ms.C.,1,2 Francisca Araújo, Ms.C.,1 Salette Reis, Ph.D.,2 and Bruno Sarmento, Ph.D.1,3,4 Journal of diabetes science and technology volume 7, issues 2,

Diabetology. http://www.diabetology.co.uk/. Accessed January 21, 2012.

Oramed Pharmaceuticals. http://www.oramed.com/. Accessed January 22, 2012.

BOWS Pharmaceuticals AG. http://www.bowspharma.com/. Accessed January 22, 2012. 5.Emisphere Technologies. http://www.emisphere.com/. Accessed January 22, 2012.

Novo Nordisk. http://www.novonordisk.com/. Accessed January 22, 2012.

Merrion Pharmaceuticals. http://www.merrionpharma.com/. Accessed January 21, 2012. 8.Biocon Biopharmaceuticals. http://www.biocon.com/. Accessed January 21, 2012.

Diasome Pharmaceuticals. http://www.diasome.com/. Accessed January 21, 2012.si

Prashanth V. Shinde, novel carrier system for oral delivery of insulin, Asian journal of pharmaceutical technology and innovations.Lee VH. Oral route of peptide and protein delivery, peptide and protein drug delivery, chapter 16, Marcel Dekker Inc.1991,691-738.

Agarwal V, Khan MA. Current status of the delivery of insulin. Pharmaceutical technology, October 2001,76-90.

Shah RB, Ahsan F, Khan MA. Oral delivery of proteins: Progress and prognostication. Crit. Rev. Ther. Drug Carrier Syst. 2002, 19(2): 135–169.

Salamat-Miller N, Johnston TP. Current strategies used to enhance the paracellular transport of therapeutic polypeptides across the intestinal epithelium. Int. J. Pharm. 2005; 294: 201–216 15.Soltero R, Ekwuribe N. The oral delivery of protein and peptide drugs- A report; In novat. Pharmaceut. Technol. 2001, 1:106–110.

Li CL, Deng YJ. Oil-based formulations for oral delivery of insulin. J. Pharm. Pharmacol. 2004; 56 (9), 1101–1107.

Eaimtrakarn S, Ramaprasad YV, Ohno T et al. Absorption-enhancing effect of labrasol on the intestinal absorption of insulin in rats, J. Drug Target. 2002; 10 (3), 255–260.

Liang JF, Yang VC. Insulin-cell penetrating peptide hybrids with improved intestinal absorption efficiency. Biochem. Biophys. Res.Commun. 2005; 335: 734–738.

Rieux A, Fievez V, Garinot M, Schneider YJ, Preat V. Nanoparticles as potential oral delivery systems of proteins and vaccines: A mechanistic approach. J. Cont. Release 2006; 116: 1-27.

Thanou M, Verhoef JC, Junginger HE. Chitosan and its derivatives as intestinal absorption enhancers. Adv. Drug. Delivery. Rev 2001, 50: S91-S101.


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How to Cite

K, D. D. “Oral Insulin Delivery for Treatment of Diabetes Mellitus”. International Journal of Pharmaceutics and Drug Analysis, vol. 9, no. 2, July 2021, pp. 66-70, doi:10.47957/ijpda.v9i2.463.



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