Long-awaited dream of oral insulin: Where did we reach?

Asian Journal of Pharmaceutical and Clinical Research

Volumn 4, Issue SUPPL. 2, 2011, Pages 16-21

  Madhav, Mutalik ^a  

^a Sir Seewosagur Ramgoolam Medical College   (Mauritius)

Author keywords

Delivery system; Diabetes; Mucoadhesive; Nanoparticle; Oral insulin; Polymer

Indexed keywords

AGENTS AFFECTING CARBOHYDRATE METABOLISM; ANTIDIABETIC AGENT; CHITOSAN; DRUG CARRIER; EUDRAGIT; IN 105; INSULIN; INSULIN ASPART; NANOPARTICLE; NN 1952; ORAL ANTIDIABETIC AGENT; ORMD 0801; PIG INSULIN; PLACEBO; PROTEINASE INHIBITOR; RECOMBINANT HUMAN INSULIN; SOLID LIPID NANOPARTICLE; UNCLASSIFIED DRUG;

ABSENCE OF SIDE EFFECTS; AREA UNDER THE CURVE; CELL PROTECTION; DIABETES MELLITUS; DIZZINESS; DOSE RESPONSE; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG CAPSULE; DRUG DELIVERY SYSTEM; DRUG DOSE ESCALATION; DRUG DOSE INCREASE; DRUG FORMULATION; DRUG PENETRATION; DRUG SOLUBILITY; DRUG TRANSPORT; HUMAN; HYDROGEL; HYPERHIDROSIS; HYPERTRIGLYCERIDEMIA; HYPOGLYCEMIA; INSULIN DEPENDENT DIABETES MELLITUS; INSULIN RELEASE; INSULITIS; LIPOSOMAL DELIVERY; NANOENCAPSULATION; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; PANCREAS ISLET BETA CELL; REVIEW; SIDE EFFECT; WEIGHT CHANGE; WEIGHT GAIN;

EID: 83455188152     PISSN: 09742441     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (60)

1. Berger M. Oral insulin 1922-1992: The history of continuous ambition and failure. In: Berger M, Gries FA, editors. Frontiers in insulin pharmacology. Germany: Thieme Publishing Group; 1993. p. 144-8.
2. Wong TW. Design of oral insulin delivery. J Drug Target. 2010; 18(2):79-92.
3. Mesiha MS, El-Bitar HI. Hypoglycaemic effect of oral insulin preparations containing Brij 35, 52, 58 or 92 and stearic acid. Journal of Pharmacy and Pharmacology 1981; 33(1): 733-4. Article first published online: 12 April 2011. DOI: 10.1111/j.2042-7158.1981.tb13917.x
4. Wang H, Li YX, Sun Q, Yang GH. Oral administration of insulin to female nonobese diabetic mice inhibited diabetes and induced Fas ligand expression on islets of Langerhans. Chinese Med J 2000;113(5):433-36.
5. Wajchenberg BL. Beta-cell failure in diabetes and preservation by clinical treatment. Endocr Rev 2007; 28:187-218.
6. Kalra S, Kalra B, Agrawal N. Oral Insulin. Diabetology and Metabolic Syndrome 2010;2:66 DOI:10.1186/1758-5996-2-66
7. Stratton IM, Adler Al, Neil HAW, Matthews DR, Manley SE, Cull CA, et al. Association of glycemia with macrovascular and microvascular complications of type 2 diabetes (UKPDS 35): prospective observational study. BMJ 2000; 321: 405-12. DOI: 10.1136/bmj.321.7258.405
8. Cernea S, Kidron M, Wohlgelernter J, Modi P, Raz I. Dose-response relationship of oral insulin spray in healthy subjects. Diabetes Care 2005; 28(6):1353-7.
9. Cernea S, Kidron M, Wohlgelernter J, Raz I. Dose-response relationship of an oral insulin spray in six patients with type 1 diabetes: a single-center, randomized, single-blind, 5-way crossover study. Clin Ther. 2005; 27(10):1562-70.
10. Bergerot I, Arreaza GA, Cameron MJ, Burdick MD, Strieter RM, Chensue SW et al. Insulin B-chain reactive CD4+ regulatory T-cells induced by oral insulin treatment protect from type 1 diabetes by blocking the cytokine secretion and pancreatic infiltration of diabetogenic effector T-cells. Diabetes 1999; 48:1720-9.
11. Skyler JS, Krischer JP, Wolfsdorf J, Cowie C, Palmer JP, Greenbaum C, et al. Effects of oral insulin in relatives of patients with type 1 diabetes: the diabetes prevention trial-type 1. Diabetes Care 2005; 28(5): 1068-76. DOI: 10.2337/diacare.28.5.1068
12. Barker JM, McFann KK, Orban T. Effect of oral insulin on insulin autoantibody levels in the Diabetes Prevention Trial Type 1 oral insulin study. Diabetologica 2007; 50(8):1603-6.
13. Vehik K, Cuthbertson D, Ruhlig H, Schatz DA, Peakman M, Krischer JP. Long-Term Outcome of Individuals Treated With Oral Insulin - Diabetes Prevention Trial-Type 1 (DPT-1) oral insulin trial. Diabetes care 2011. Published online before print. May 24, 2011. DOI 10.2337/dc11-0523 Retrieved from www.Care.diabetesjournals.org
14. Heinemann L and Jacques Y. Oral insulin and buccal insulin: a critical reappraisal. J Diabetes Sci Technol 2009; 3:568-84.
15. Iyer H, Khedkar A, Verma M. Oral insulin - a review of current status. Diabetes Obes Metab 2010; 12:179-85.
16. Wang W. Oral protein delivery. J Drug Target 1996; 4:195-232.
17. Carino GP, Mathiowitz E. Oral insulin delivery. Adv Drug Deliv Rev 1999; 35:249-57.
18. Arbit E. The physiological rationale for oral insulin administration. Diabetes Technol Ther 2004; 6:510-7.
19. Ramesan RM and Sharma CP. Challenges and advances in nanoparticle-based oral insulin delivery. Expert Rev Med Devices 2009; 6(6):665-76.
20. Scarlett JA, Gray RS, Griffin J, Olefsky JM, Kolterman OG. Insulin treatment reverses the insulin resistance of type 2 diabetes mellitus. Diabetes Care 1982; 5:353-63.
21. Zhao L, Sun D, Cao F, Yin T, Wang H. Can insulin resistance be reversed by insulin therapy? Med Hypotheses 2009; 72:34-5.
22. Kaptiza C, Zijlstra E, Heinemann L, Castelli MC, Riley G, Heise T. Oral insulin: A comparison with subcutaneous regular human insulin in patients with type 2. Diabetes Care 2010; 33(6):1288-90.
23. Phillips J, Russel-Jones DL, Wright J, Brackenridge A, New R, Bansal G. Early evaluation of a novel oral insulin delivery system in healthy volunteers. Diabetes 2004; 53(Suppl. 2):A113.
24. Luzio S, Dunseath G, Lockett A, Broke-Smith TP, New RR, Owens D. Comparison of an oral insulin (Capsulin) and Actrapid during an isoglycemic clamp study in persons with type 2 diabetes. Diabetes 2008; 56(Suppl. 1):A10.
25. Fasano A, Uzzau S. Modulation of intestinal tight junctions zona occludens toxin permits enteral administration of insulin and other macromolecules in an animal model. J Clin Invest 1997; 99:1158-64.
26. Palin KJ, Phillips AJ, Ning A. The oral absorption of cefoxitin from oil and emulsion vehicles in rats. Int J Pharm 1986; 33:99-104.
27. Yamamoto A, Taniguchi T, Rikyuu K, Tsuji T, Fujita T, Murakami M et al. Effect of various protease inhibitors on the intestinal absorption and degradation of insulin in rats. Pharm Res 1994; 11:1496-1500.
28. Nikam KR, Pawar MG, Salunkhe KS, Bachhav DG. Recent trends in insulin drug delivery system. 2011. http://www.pharmatutor.org/articles/recent-trends-in-insulin-drug-delivery-system?utm_s. [Accessed May 28, 2011].
29. Clement S, Still JG, Kosutic G, McAllister RG. Oral insulin product hexyl-insulin monoconjugate 2 (HIM2) in type 1 diabetes mellitus: the glucose stabilization effects of HIM2. Diabetes Technol Ther 2002; 4(4):459-66.
30. Niu M, Lu Y, Hovgaard L, Wu W. Liposomes containing glycocholate as potential oral insulin delivery systems: preparation, in vitro characterization, and improved protection against enzymatic degradation. Int J Nanomedicine 2011; 6:1155-66. DOI: http://dx.doi.org/10.2147/IJN.S19917
31. Schwartz S, Geho B, Rosenberg L, Lau J. A 2-week randomized active comparator study of two HDV-Insulin routes (SC and oral) and SC human insulin in patients with type 1 diabetes. Diabetes 2008, 57(Suppl. 1):A124.
32. Thompson C, Cheng WP, Gadad P, Skene K, Smith M, Smith G, et al. Uptake and transport of novel amphiphilic polyelectrolyte-insulin nanocomplexes by Caco-2 cells--towards oral insulin. Pharm Res 2011; 28(4):886-96.
33. Aspden TJ, Mason JD, Jones NS. Chitosan as a nasal delivery system: the effect of chitosan solutions on in vitro and in vivo mucociliary transport rates in human turbinates and volunteers. J Pharm Sci 1997; 86:509-13.
34. Mathiowitz E, Jacob JS, Jong YS, Carino GP, Chickering DE, Charturvedi P, et al. Biologically erodible microspheres as potential oral drug delivery systems. Nature 1997; 386:410-4.
35. Damge C, Michael C, Aprahamian M, Couvreur P. New approach for oral administration of insulin with polyalkylcyanoacrylate nanocapsules as oral carrier. Diabetes 1988; 37:247-51.
36. Takka S, Acarturk F. Calcium alginate microparticles for oral administration. I: effect of sodium alginate type on drug release and drug entrapment efficiency. J Microencapsul: Micro Nano Carriers 1999; 16:275-90.
37. Rowsen ML, Dileep KJ, Sharma CP. Beta cyclodextrin-insulin encapsulated chitosan/alginate matrix: oral delivery system. J Appl Polym Sci 2000; 75:1089-96.
38. Dapergolas G, Gregoriadis G. Hypoglycaemic effect of liposome-entrapped insulin administered intragastrically into rats. Lancet 1976; 2:824-7.
39. Pappo J, Ermak TH. Uptake and translocation of fluorescent latex particles by rabbit Peyer's patch follicle epithelium: a quantitative model for M cell uptake. Clin Exp Immunol 1989; 76:144-8.
40. Sajeesh S and Sharma CP. Cyclodextrin-insulin complex encapsulated polymethacrylic acid based nanoparticles for oral insulin delivery. Int J Pharm 2006; 325(1-2):147-54. Epub 2006 June 18.
41. Mundargi RC, Rangaswamy V, Aminabhavi TM. Poly(N-vinylcaprolactam-co-methacrylic acid) hydrogel microparticles for oral insulin delivery. J Microencapsul 2011;28(5):384-94.
42. Jindal SK, Singh M, Goswami M. Formulation and evaluation of insulin enteric microspheres for oral drug delivery. Acta Pharmaceutica Sciencia 2009; 51: 121-7.
43. Rekha MR and Sharma CP. Glutamine-chitosan microparticles as oral insulin delivery matrix: In vitrocharacterization. J Appl Polym Sci 2011; 122:2374-82. DOI: 10.1002/app.34315
44. Sarmento B, Martins S, Ferreira D, Souto EB. Oral insulin delivery by means of solid lipid nanoparticles. Int J Nanomedicine 2007; 2(4):743-9. DOI: http://dx.doi.org/10.2147/IJN.S
45. Mundargi RC, Rangaswamy V, Aminabhavi TM. pH-sensitive oral insulin delivery systems using Eudragit microspheres. Drug Dev Ind Pharm 2011; 37(8): 977-85.
46. Khedkar A, Iyer H, Anand A, Verma M, Krishnamurthy S, Savale S, et al. A dose range finding study of novel oral insulin (IN-105) under fed conditions in type 2 diabetes mellitus subjects. Diabetes Obes Metab 2010; 12(8):659-64.
47. Biocon: oral insulin fails to meet primary target. 2011. Reuters US Edition, Jan 11, 2011 Bangalore, India http://www.reuters.com/article/2011/01/11/biocon-insulin-trials-idUSSGE70A02M20110111[Accessed Oct 21, 2011].
48. Biocon oral insulin to see more pre-launch tests. 2010. Oct 23, 2010. http://www.business-standard.com/india/news/biocons-oral-insulin-to-see-more-pre-launch-tests/412417/.19/07/2011[Accessed Oct 21, 2011].
49. Novo Nordisk. A two part trial investigating NN1952 in healthy subjects and subjects with type 1 and type 2 diabetes. 2009. Retrieved from http://www.novonordisk-trials.com/Website/pdf/registry/nn19523646.pdf [Accessed on October 27, 2011].
50. Eldor R, Arbit E, Miteva Y, Freier R, Kidron M. Oral Insulin:Type 1 Diabetes (T1DM) Patient Response Upon Preprandial Administration. Poster, ADA, Orlando 2010.
51. Oral insulin company Oramed gets good Phase IIb results. 2010. Published by Globes (online), Israel Business News. http://www.globes-online.com/ on May 10, 2010. Retrieved from http://www.globes.co.il/serveen/globes/docview.asp?did=1000558541&fid=1725 [Accessed Oct 21, 2010].
52. ORMD 0801 Oral insulin capsule. May 2010. http://www.oramed.com/index.php?page=14 [Accessed Oct 21, 2011].
53. A Two Part Trial Investigating NN1952 in Healthy Subjects and Subjects With Type 1 and Type 2 Diabetes This study has been completed [http://clinicaltrials.gov/ct2/show/study/NCT01028404] Study NCT01028404.
54. New Product: Oral Insulin Strip. Diabetes in control.com. Issue 552. Dec 17, 2010. http://www.diabetesincontrol.com/articles/newproduct/10224-new-product-oral-insulin-strip[Accessed Oct 21, 2011].
55. Oral Insulin. Monosol Rx, Midatech. 2011. (Positive Results for Oral Insulin Delivery in Pre-Clinical Trials. January 4, 2011) Page 1-9. Available from: http://asweetlife.org/a-sweet-life-staff/in-the-news/insulin-pumps-in-the-news/positive-re. [Accessed on July 19, 2011].
56. Gilles Gary. Oral Insulin Research Update. 2011 About.com Type 1 diabetes. Sept 17, 2011. http://type1diabetes.about.com/b/2011/09/17/oral-insulin-research-update.htm [Accessed Oct 21, 2011].
57. Donnelly JM. 2011. Generex advances oral insulin product - July 11, 2011. Boston Medical Journal. Available at http://www.bizjournals.com/boston/news/2011/07/11/generex-avances-oral-insulin.html19/07/2011 [Accessed July 19, 2011].
58. Steffens R. Aug 16, 2010. Good news for Generex: Positive data on oral insulin coming in September. http://seekingalpha.com/article/220670-good-news-for-generex-positive-data-on-oral-ins. [Accessed July 24, 2011].
59. Card JW, Magnuson BA. A review of efficacy and safety of nanoparticle-based insulin delivery systems. Am J Physiol Gastrointest Liver Physiol 2011; Sep 15 [Epub Ahead of print] PMID 21921287 [Pubmed - as supplied by Publisher]. [Accessed October 28, 2011].
60. Woitiski CB, Carvalho RA, Ribeiro AJ, Neufeld RJ, Veiga F. Strategies toward the improved oral delivery of insulin nanoparticles via gastrointestinal uptake and translocation. BioDrugs. 2008; 22(4):223-37.