Novel fibrillar insulin formulations for oral administration: Formulation and in vivo studies in diabetic mice

Journal of Controlled Release

Volumn 143, Issue 1, 2010, Pages 128-135

  Dekel, Y ^a   Glucksam, Y ^a   Margalit, R ^a  

^a TEL AVIV UNIVERSITY   (Israel)

Author keywords

Diabetes; Drug delivery; ICR mice; Insulin fibrils; Oral delivery

Indexed keywords

BLOOD GLUCOSE LEVEL; DIABETES; DIABETIC MICE; EATING HABITS; HYALURONAN; ICR MICE; IN-VIVO; MICRO PARTICLES; ORAL ADMINISTRATION; ORAL DELIVERY; ORAL DOSE; THERAPEUTIC PROTEIN; TIME SPAN;

DRUG DELIVERY; GLUCOSE;

INSULIN;

BOVINE INSULIN; DIPALMITOYLPHOSPHATIDYLETHANOLAMINE; HYALURONIC ACID; RECOMBINANT HUMAN INSULIN;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; DIABETES MELLITUS; DRUG ADMINISTRATION ROUTE; DRUG COATING; DRUG DELIVERY SYSTEM; DRUG EFFICACY; DRUG FORMULATION; DRUG STRUCTURE; DRUG SYNTHESIS; EXPERIMENTAL MOUSE; FREEZE DRYING; GLUCOSE BLOOD LEVEL; GLYCEMIC CONTROL; IN VIVO STUDY; MALE; MOUSE; NONHUMAN; PARTICLE SIZE; PRIORITY JOURNAL;

ADMINISTRATION, ORAL; ANIMALS; BLOOD GLUCOSE; CHEMISTRY, PHARMACEUTICAL; DIABETES MELLITUS, EXPERIMENTAL; DOSAGE FORMS; DRUG STABILITY; HYALURONIC ACID; HYDROPHOBICITY; HYPOGLYCEMIC AGENTS; INSULIN; MALE; MICE; MICE, INBRED ICR; PARTICLE SIZE; SURFACE PROPERTIES; TECHNOLOGY, PHARMACEUTICAL; TIME FACTORS;

EID: 77950519662     PISSN: 01683659     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.jconrel.2009.12.018     Document Type: Article

References (47)

1. Gonzalez C., Kanevsky D., De Marco R., Di Girolamo G., Santoro S. Non-invasive routes for insulin administration: current state and perspectives. Expert Opin. Drug Deliv. 2006, 3:763-770.
2. Lassmann-Vague V., Raccah D. Alternatives routes of insulin delivery. Diabetes Metab. 2006, 32:513-522.
3. Cefalu W.T. Concept, strategies, and feasibility of noninvasive insulin delivery. Diabetes Care 2004, 27:239-246.
4. Cui F., Shi K., Zhang L., Tao A., Kawashima Y. Biodegradable nanoparticles loaded with insulin-phospholipid complex for oral delivery: preparation, in vitro characterization and in vivo evaluation. J. Control. Release 2006, 114:242-250.
5. Morishita M., Peppas N.A. Is the oral route possible for peptide and protein drug delivery?. Drug Discov. Today 2006, 11:905-910.
6. Mesiha M.S., Ponnapula S., Plakogiannis F. Oral absorption of insulin encapsulated in artificial chyles of bile salts, palmitic acid and alpha-tocopherol dispersions. Int. J. Pharm. 2002, 249:1-5.
7. Bendayan M., Ziv E., Gingras D., Ben-Sasson R., Bar-On H., Kidron M. Biochemical and morpho-cytochemical evidence for the intestinal absorption of insulin in control and diabetic rats. Comparison between the effectiveness of duodenal and colon mucosa. Diabetologia 1994, 37:119-126.
8. Brange J., Andersen L., Laursen E.D., Meyn G., Rasmussen E. Toward understanding insulin fibrillation. J. Pharm. Sci. 1997, 86:517-525.
9. Whittingham J.L., Scott D.J., Chance K., Wilson A., Finch J., Brange J., et al. Insulin at pH 2: structural analysis of the conditions promoting insulin fibre formation. J. Mol. Biol. 2002, 318:479-490.
10. Margalit R., Peer D. Lipidated glycosaminoglycan particles and their use in drug and gene delivery for diagnosis and therapy 2009, US patent 7,544,372.
11. Barkay Z., Rivkin I., Margalit R. Three-dimensional characterization of drug-encapsulating particles using STEM detector in FEG-SEM. Micron 2009, 40:480-485.
12. Sandri G., Rossi S., Ferrari F., Bonferoni M.C., Zerrouk N., Caramella C. Mucoadhesive and penetration enhancement properties of three grades of hyaluronic acid using porcine buccal and vaginal tissue, Caco-2 cell lines, and rat jejunum. J. Pharm. Pharmacol. 2004, 56:1083-1090.
13. Peer D., Florentin A., Margalit R. Hyaluronan is a key component in cryoprotection and formulation of targeted unilamellar liposomes. Biochim. Biophys. Acta 2003, 1612:76-82.
14. Peer D., Margalit R. Physicochemical evaluation of a stability-driven approach to drug entrapment in regular and in surface-modified liposomes. Arch. Biochem. Biophys. 2000, 383:185-190.
15. Margalit R. Liposome-mediated drug targeting in topical and regional therapies. Crit. Rev. Ther. Drug Carrier Syst. 1995, 12:233-261.
16. Carson F.L. Histotechnology: A Self Instructional Text 1990, ASCP Press, Chicago.
17. Fischer S., Arad A., Margalit R. Lipsome-formulated enzymes for organophosphate scavenging: butyrylcholinesterase and Demeton-S. Arch. Biochem. Biophys. 2005, 434:108-115.
18. USP 27 NF 22. The United States Pharmacopoeia, p. 2724, 2004.
19. Dekel Y., Glucksam Y., Elron-Gross I., Margalit R. Insights into modeling streptozotocin-induced diabetes in ICR mice. Lab. Anim. (NY) 2009, 38:55-60.
20. Damge C., Reis C.P., Maincent P. Nanoparticle strategies for the oral delivery of insulin. Expert Opin. Drug Deliv. 2008, 5:45-68.
21. Dekel Y, Margalit R. Diabetes treatment by oral delivery of novel insulin-fibril formulations. 2008: in preparation.
22. Margalit R. Liposome-encapsulated Insulin Formulations, Pending Patent Application, WO03/030829 A3 2001.
23. Rekha M.R., Sharma C.P. Synthesis and evaluation of lauryl succinyl chitosan particles towards oral insulin delivery and absorption. J. Control. Release 2009, 135:144-151.
24. Sonaje K., Lin Y.H., Juang J.H., Wey S.P., Chen C.T., Sung H.W. In vivo evaluation of safety and efficacy of self-assembled nanoparticles for oral insulin delivery. Biomaterials 2009, 30:2329-2339.
25. Morishita M., Goto T., Nakamura K., Lowman A.M., Takayama K., Peppas N.A. Novel oral insulin delivery systems based on complexation polymer hydrogels: single and multiple administration studies in type 1 and 2 diabetic rats. J. Control. Release 2006, 110:587-594.
26. Murphy R.M. Kinetics of amyloid formation and membrane interaction with amyloidogenic proteins. Biochim. Biophys. Acta 2007, 1768:1923-1934.
27. Gorbenko G.P., Kinnunen P.K. The role of lipid-protein interactions in amyloid-type protein fibril formation. Chem. Phys. Lipids 2006, 141:72-82.
28. Chi E.Y., Ege C., Winans A., Majewski J., Wu G., Kjaer K., et al. Lipid membrane templates the ordering and induces the fibrillogenesis of Alzheimer's disease amyloid-beta peptide. Proteins 2008, 72:1-24.
29. Knight J.D., Miranker A.D. Phospholipid catalysis of diabetic amyloid assembly. J. Mol. Biol. 2004, 341:1175-1187.
30. Engel M.F., Khemtemourian L., Kleijer C.C., Meeldijk H.J., Jacobs J., Verkleij A.J., et al. Membrane damage by human islet amyloid polypeptide through fibril growth at the membrane. Proc. Natl. Acad. Sci. U. S. A. 2008, 105:6033-6038.
31. Nayak A., Dutta A.K., Belfort G. Surface-enhanced nucleation of insulin amyloid fibrillation. Biochem. Biophys. Res. Commun. 2008, 369:303-307.
32. Linse S., Cabaleiro-Lago C., Xue W.F., Lynch I., Lindman S., Thulin E., et al. Nucleation of protein fibrillation by nanoparticles. Proc. Natl. Acad. Sci. U. S. A. 2007, 104:8691-8696.
33. Wang M., Zhao X.R., Wang P., Li L., Dai Y., Huang H., et al. Glucose regulated proteins 78 protects insulinoma cells (NIT-1) from death induced by streptozotocin, cytokines or cytotoxic T lymphocytes. Int. J. Biochem. Cell Biol. 2007, 39:2076-2082.
34. Itoh T., Kita N., Kurokawa Y., Kobayashi M., Horio F., Furuichi Y. Suppressive effect of a hot water extract of adzuki beans (Vigna angularis) on hyperglycemia after sucrose loading in mice and diabetic rats. Biosci. Biotechnol. Biochem. 2004, 68:2421-2426.
35. Bloch K., Vorobeychik M., Yavrians K., Azarov D., Bloch O., Vardi P. Improved activity of streptozotocin-selected insulinoma cells following microencapsulation and transplantation into diabetic mice. Cell. Biol. Int. 2006, 30:138-143.
36. Kondo Y., Nakatani A., Hayashi K., Ito M. Low molecular weight chitosan prevents the progression of low dose streptozotocin-induced slowly progressive diabetes mellitus in mice. Biol. Pharm. Bull. 2000, 23:1458-1464.
37. Xiong X.Y., Li Y.P., Li Z.L., Zhou C.L., Tam K.C., Liu Z.Y., et al. Vesicles from Pluronic/poly(lactic acid) block copolymers as new carriers for oral insulin delivery. J. Control. Release 2007, 120:11-17.
38. Chalasani K.B., Russell-Jones G.J., Yandrapu S.K., Diwan P.V., Jain S.K. A novel vitamin B12-nanosphere conjugate carrier system for peroral delivery of insulin. J. Control. Release 2007, 117:421-429.
39. Damge C., Maincent P., Ubrich N. Oral delivery of insulin associated to polymeric nanoparticles in diabetic rats. J. Control. Release 2007, 117:163-170.
40. Karmaker S., Saha T.K., Yoshikawa Y., Yasui H., Sakurai H. A novel drug delivery system for type 1 diabetes: insulin-mimetic vanadyl-poly(gamma-glutamic acid) complex. J. Inorg. Biochem. 2006, 100:1535-1546.
41. Calceti P., Salmaso S., Walker G., Bernkop-Schnurch A. Development and in vivo evaluation of an oral insulin-PEG delivery system. Eur. J. Pharm. Sci. 2004, 22:315-323.
42. Cheng J., Teply B.A., Jeong S.Y., Yim C.H., Ho D., Sherifi I., et al. Magnetically responsive polymeric microparticles for oral delivery of protein drugs. Pharm. Res. 2006, 23:557-564.
43. Lin Y.H., Mi F.L., Chen C.T., Chang W.C., Peng S.F., Liang H.F., et al. Preparation and characterization of nanoparticles shelled with chitosan for oral insulin delivery. Biomacromolecules 2007, 8:146-152.
44. Joshi H.M., Bhumkar D.R., Joshi K., Pokharkar V., Sastry M. Gold nanoparticles as carriers for efficient transmucosal insulin delivery. Langmuir 2006, 22:300-305.
45. Hayashi K., Kojima R., Ito M. Strain differences in the diabetogenic activity of streptozotocin in mice. Biol. Pharm. Bull. 2006, 29:1110-1119.
46. Milstein S.J., Leipold H., Sarubbi D., Leone-Bay A., Mlynek G.M., Robinson J.R., et al. Partially unfolded proteins efficiently penetrate cell membranes-implications for oral drug delivery. J. Control. Release 1998, 53:259-267.
47. Schatz G., Dobberstein B. Common principles of protein translocation across membranes. Science 1996, 271:1519-1526.