Microencapsulation techniques to develop formulations of insulin for oral delivery: A review

Journal of Microencapsulation

Volumn 30, Issue 5, 2013, Pages 409-424

  Cárdenas Bailón, Fernando ^a   Osorio Revilla, Guillermo ^a   Gallardo Velázquez, Tzayhrí ^a  

^a INSTITUTO POLITÉCNICO NACIONAL   (Mexico)

Author keywords

Insulin; Insulin microencapsulation; Oral delivery; Peptides delivery

Indexed keywords

BIOPOLYMER; INSULIN; PENETRATION ENHANCING AGENT; PROTEINASE INHIBITOR; SOLID LIPID NANOPARTICLE;

BIOLOGICAL ACTIVITY; COMPLEX FORMATION; DRUG BIOAVAILABILITY; DRUG DELIVERY SYSTEM; DRUG FORMULATION; DRUG PENETRATION; DRUG RELEASE; ENZYMATIC DEGRADATION; GELATION; HUMAN; INTESTINE ABSORPTION; MICROEMULSION; MICROENCAPSULATION; NANOENCAPSULATION; NONHUMAN; PH; REVIEW; SCALE UP; STOMACH;

ADMINISTRATION, ORAL; ANIMALS; DRUG COMPOUNDING; DRUG DELIVERY SYSTEMS; HUMANS; HYPOGLYCEMIC AGENTS; INSULIN;

EID: 84879556810     PISSN: 02652048     EISSN: 14645246     Source Type: Journal    
DOI: 10.3109/02652048.2012.742159     Document Type: Review

References (77)

1. Agarwal V, Khan MA. Current status of the oral delivery of insulin. Pharm Technol, 2001;25(10):76-90.
2. Bai JP, Chang LL. Effects of enzyme inhibitors and insulin concentration on transepithelial transport of insulin in rats. J Pharm Pharmacol, 1996;48:1078-82. (Pubitemid 26400300)
3. Banting FG, Best CH, Collip JB, Campbell WR, Fletcher AA. Pancreatic extracts in the treatment of diabetes mellitus: Preliminary report. Reprint. Can Med Assoc J, 1991;145(10):1281-6.
4. Bendayan M, Ziv E, Gingras D, Sasson RB, Bar-On H, Kidron M. Biochemical and cytochemical evidence for the intestinal absorption of insulin in control and diabetic rats. Comparison between the effectiveness of duodenal and colon mucosa. Diabetologia, 1994;37:119-26. (Pubitemid 24042878)
5. Bendayan M, Ziv E, Sasson RB, Bar-On H, Kidron M. Morpho-cytochemical and biochemical evidence for insulin absorption by the rat ileal epithelium. Diabetologia, 1990;33:197-204. (Pubitemid 20136235)
6. Chalasani KB, Russell JGJ, Jain AK, Diwan PV, Jain SK. Effective oral delivery of insulin in animal models using vitamin B12-coated dextran nanoparticles. J Control Release, 2007b;122:141-50. (Pubitemid 47361403)
7. Chalasani KB, Russell JGJ, Yandrapu SK, Diwan PV, Jain SK. A novel vitamin B12-nanosphere conjugate carrier system for peroral delivery of insulin. J Control Release, 2007a;117:421-9. (Pubitemid 46237606)
8. Chang SG, Choi KD, Jang SH, Shin HC. Role of disulfide bonds in the structure and activity of human insulin. Mol Cells, 2003;16(3):323-30.
9. Cilek A, Celebi N, Tirnaksiz F. Lecithin-based microemulsion of a peptide for oral administration: Preparation, characterization, and physical stability of the formulation. Drug Deliv, 2006;13(1):19-24. (Pubitemid 43087616)
10. Cilek A, Celebi N, Tirnaksiz F, Tay A. A lecithin-based microemulsion of rh-insulin with aprotinin for oral administration: Investigation of hypoglycemic effects in non-diabetic and STZ-induced diabetic rats. Int J Pharm, 2005;298:176-85. (Pubitemid 40828338)
11. Constantinides PP, Scalart JP, Lancaster C, Marcello J, Marks G, Ellens H, Smith PL. Formulation and intestinal absorption enhancement evaluation of water in oil microemulsions incorporating mediumchain glycerides. Pharm Res, 1994;11:1385-90. (Pubitemid 24339642)
12. Cournarie F, Rosilio V, Cheron M, Vauthier C, Lacour V, Grossiord JL, Seiller M. Improved formulation of W/OW/multiple emulsion for insulin encapsulation. Influence of the chemical structure of insulin. Colloid Polym Sci, 2004a;282:562-8.
13. Cournarie F, Savelli MP, Rosilio V, Bretez F, Vauthier C, Grossiord JL, Seiller M. Insulin-loaded W/O/W multiple emulsions: Comparison of the performances of systems prepared with medium-chain triglycerides and fish oil. Eur J Pharm Biopharm, 2004b;58:477-82. (Pubitemid 39297094)
14. 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;114:242-50. (Pubitemid 44291843)
15. Cunha AS, Cheron M, Grossiord JL, Puisieux F, Seiller M. W/O/W multiple emulsions of insulin containing a protease inhibitor and an absorption enhancer: Biological activity after oral administration to normal and diabetic rats. Int J Pharm, 1998;169:33-44. (Pubitemid 28352596)
16. Cunha AS, Grossiord JL, Puisieux F, Seiller M. Insulin in w/o/w multiple emulsions: Preparation characterization and determination of stability towards proteases in vitro. J Microencapsul, 1997a;14(39):311-19. (Pubitemid 27190279)
17. Cunha AS, Grossiord JL, Puisieux F, Seiller M. W/O/W multiple emulsions of insulin containing a protease inhibitor and an absorption enhancer: Preparation, characterization and determination of stability towards proteases in vitro. Int J Pharm, 1997b;158:79-89. (Pubitemid 27504476)
18. Dai Y, Tang JG. Characteristic, activity and conformational studies of [A6- Ser, A11-Ser]-insulin. Biochim Biophys Acta, 1996;1296(1):63-8. (Pubitemid 26259809)
19. Dekel Y, Glucksam Y, Margalit R. Novel fibrillar insulin formulations for oral administration: Formulation and in vivo studies in diabetic mice. J Control Release, 2010;143:128-35.
20. El-Sayed A, Remawi MA, Qinna N, Farouk A, Badwan A. Formulation and characterization of an oily-based system for oral delivery of insulin. Eur J Pharm Biopharm, 2009;73:269-79.
21. Fasano A, Uzzau S. Modulation of intestinal tight junctions by zonula occludens toxin permits enteral administration of insulin and other macromolecules in an animal model. J Clin Invest, 1997;99:1158-64. (Pubitemid 27142750)
22. Foss AC, Goto T, Morishita M, Peppas NA. Development of acrylic-based copolymers for oral insulin delivery. Eur J Pharm Biopharm, 2004;57:163-9. (Pubitemid 38283691)
23. Graf A, Rades T, Hook SM. Oral insulin delivery using nanoparticles based on microemulsions with different structure-types: Optimisation and in vivo evaluation. Eur J Pharm Sci, 2009;37:53-61.
24. Harfenist EJ, Craig LC. The molecular weight of insulin. J Am Chem Soc, 1952;74:3087-9.
25. Hochman J, Artursson P. Mechanisms of absorption enhancement and tight junction regulation. J Control Release, 1994;29:253-67. (Pubitemid 24156373)
26. Hoffman A, Ziv E. Pharmacokinetic considerations of new insulin formulations and routes of administration. Clin Pharmacokinet, 1997;33:285-301. (Pubitemid 27429895)
27. Jain D, Panda AK, Majumdar DK. Eudragit S100 entrapped insulin microspheres for oral delivery. APPS PharmSciTech, 2005;688(1):100-7.
28. Jain S, Rathi VV, Jain AK, Das M, Godugu C. Folate-decorated PLGA nanoparticles as a rationally designed vehicle for the oral delivery of insulin. Nanomedicine, 2012;7(9):1-27.
29. Jelvehgari M, Milani PZ, Shadbad MRS, Loveymi BD, Nokhodchi A, Azari Z, Valizadeh H. Development of pH-sensitive insulin nanoparticles using Eudragit L100-55 and chitosan with different molecular weights. AAPS PharmSciTech, 2010;11(3):1237-42.
30. Kavimandan NJ, Peppas NA. Confocal microscopic analysis of transport mechanisms of insulin across the cell monolayer. Int J Pharm, 2008;354(1-2):143-8.
31. Kennedy FP. Recent developments in insulin delivery techniques: Current status and future potential. Drugs, 1991;42:213-27. (Pubitemid 21920761)
32. Kinesh VP, Neelam DP, Punit BP, Bhavesh SB, Pragna KS. Novel approaches for oral delivery of insulin and current status of oral insulin products. Int J Pharm Sci Nanotech, 2010;3(3):1057-64.
33. Krauland AH, Guggi D, Schnurch AB. Oral insulin delivery: The potential of thiolated chitosan-insulin tablets on non-diabetics rats. J Control Release, 2004;95:547-55. (Pubitemid 38340504)
34. Laskowski M, Haessler HA, Miech RP, Peanasky RJ, Laskowski M. Effect of trypsin inhibitor on passage of insulin across the intestinal barrier. Science, 1958;127:1115-16.
35. Lin YH, Mi FL, Chen CT, Chang WC, Peng SF, Liang HF, Sun HW. Preparation and characterization of nanoparticles shelled with chitosan for oral insulin delivery. Biomacromolecules, 2007;8:146-52.
36. Liu R, Huang SS, Wan YH, Ma GH, Su ZG. Preparation of insulin-loaded PLA/PLGA microcapsules by a novel membrane emulsification method and its release in vitro. Colloids Surf B-Biointerfaces, 2006;51:30-8. (Pubitemid 44094033)
37. Lowman AM, Morishita M, Kajita M, Nagai T, Peppas NA. Oral delivery of Insulin using pH-responsive complexation gels. J Pharm Sci, 1999;88(9):933-7. (Pubitemid 29438959)
38. Ma EL, Ma H, Liu Z, Zheng C, Duan M. In vitro and in vivo evaluation of a novel oral insulin formulation. Acta Pharmacol Sin, 2006;27(10):1382-8. (Pubitemid 44439975)
39. Makhlof A, Tozuka Y, Takeuchi H. Design and evaluation of novel pHsensitive chitosan nanoparticles for oral insulin delivery. Eur J Pharm Sci, 2011;42:445-51.
40. Marrero DG. Overcoming patient barriers to initiating insulin therapy in type 2 diabetes mellitus. Clin Cornerstone, 2007;8(2):33-43.
41. Marschu tz MK, Caliceti P, Schnurch AB. Design and in vivo evaluation of an oral delivery system for insulin. Pharm Res, 2000;17(12):1468-74. (Pubitemid 32217556)
42. Mathiowitz E, Furtado S, Abramson D, Burril R, Olivier G, Gourd C, Bubbers E. Oral delivery of insulin loaded poly(fumaric-co-sebacic) anhydride microspheres. Int J Pharm, 2008;347:149-55. (Pubitemid 350180326)
43. Morcol T, Nagappan P, Nerembum L, Mitchell A, Bell SJD. Calcium phosphate- PEG-insulin-casein (CAPIC) particles as oral delivery systems for insulin. Int J Pharm, 2004;277:91-7 (Pubitemid 38670424)
44. Morishita M, Goto T, Nakamura K, Lowman AM, Takayama K, Peppas NA. 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;110:587-94. (Pubitemid 43163448)
45. Morishita M, Matsuzawa A, Takayama K, Isowa K, Nagai T. Improving insulin enteral absorption using water-in-oil-in-water emulsion. Int J Pharm, 1998;172:189-98. (Pubitemid 28430256)
46. Morishita I, Morishita M, Takayama K, Mashida Y, Nagai T. Hypoglycemic effect of novel oral microspheres of insulin with protease inhibitor in normal and diabetic rats. Int J Pharm, 1992a;92:9-16.
47. Morishita M, Morishita I, Takayama K, Machida Y, Nagai T. Novel oral microspheres of insulin with protease inhibitor protecting from enzymatic degradation. Int J Pharm, 1992b;78:1-7.
48. Mukherjee B, Santra K, Pattnaik G, Ghosh S. Preparation, characterization and in vitro evaluation of sustained release protein-loaded nanoparticles based on biodegradable polymers. Int J Nanomed, 2008;3(4):487-96.
49. Musabayane CT, Munjeri O, Bwititi P, Osim EE. Orally administered, insulin-loaded amidated pectin hydrogel beads sustain plasma concentrations of insulin in streptozotocin-diabetic rats. J Endocrinol, 2000;164:1-6. (Pubitemid 30044323)
50. Park K, Kwon IC, Park K. Oral protein delivery: Current status and future prospect. React Funct Polym, 2011;71:280-7.
51. Ritschel WA. Microemulsions for improved peptide absorption from gastrointestinal tract. Meth Find Exp Clin Pharmacol, 1991;13:205-20.
52. Ryle AP, Sanger F, Smith LF, Kitai R. The disulphide bonds of insulin. Biochem J, 1955;60:542-56.
53. Sajeesh S, Sharma CP. Cyclodextrin-insulin complex encapsulated polymethacrylic acid based nanoparticles for oral insulin delivery. Int J Pharm, 2006;325(1-2):147-54. (Pubitemid 44573692)
54. Sanger F. The terminal peptides of insulin. Biochem J, 1949;45:563-74.
55. Sanger F. Chemistry of insulin: Determination of the structure of insulin opens the way to greater understanding of life processes. Science, 1959;129:1340-4.
56. Sarmento B, Martins S, Ferrerira D, Souto EB. Oral insulin delivery by means of solid lipids nanoparticles. Int J Nanomed, 2007a;2(4):743-9.
57. Sarmento B, Ribeiro A, Veiga F, Ferreira D. Development and characterization of new insulin containing polysaccharide nanoparticles. Colloids Surf B-Biointerfaces, 2006;53:193-202. (Pubitemid 44802985)
58. Sarmento B, Ribeiro A, Veiga F, Ferreira D, Neufeld R. Oral bioavailability of insulin contained in polysaccharide nanoparticles. Biomacromolecules, 2007b;8:3054-60. (Pubitemid 350011625)
59. Sharma G, Wilson K, Van der Walle CF, Sattar N, Petrie JR, Ravi Kumar MNV. Microemulsions for oral delivery of insulin: Design, development and evaluation in streptozotocin induced diabetic rats. Eur J Pharm Biopharm, 2010;76:159-69.
60. Sheeja VS, Reddy MH, Joseph J, Reddy ND. Insulin therapy in diabetes management. Int J Pharm Sci Rev Res, 2010;2(2):98-105.
61. Shilling RJ, Mitra AK. Intestinal mucosa transport of insulin. Int J Pharm, 1990;62:53-64.
62. Shima M, Tanaka M, Fujii T, Egawa K, Kimura Y, Adachi S, Matsuno R. Oral administration of insulin included in fine W/O/W emulsions to rats. Food Hydrocolloids, 2006;20:523-31. (Pubitemid 43213135)
63. Silva CM, Ribeiro AJ, Ferreira D, Veiga F. Insulin encapsulation in reinforced alginate microspheres prepared by internal gelation. Eur J Pharm Sci, 2006;29:148-59. (Pubitemid 44349058)
64. Singh S, Patel D, Patel NR, Kumar K, Gautam MK. Insulin oral delivery may be possible. Int J Pharm Prof Res, 2010;1(1):46-51.
65. Singnurkar PS, Gidwani SK. Insulin-egg yolk dispersions in self microemulsifying system. Indian J Pharm Sci, 2008;70(6):727-32.
66. Touitou E, Rubinstein A. Targeted enteral delivery of insulin to rats. Int J Pharm, 1986;30:95-9. (Pubitemid 16082943)
67. Tozaki H, Emi Y, Horisaka E, Fujita T, Yamamoto A, Muranishi S. Degradation of insulin and calcitonin and their protection by various protease inhibitors in rat caecal contents: Implications in peptide delivery to the colon. J Pharm Pharmacol, 1997;49(2):164-8. (Pubitemid 27096110)
68. Trenktrog T, Muller BW, Seifert J. In vitro investigation into enhancement of intestinal peptide absorption by emulsion systems. Eur J Pharm Biopharm, 1995;41:284-90.
69. Watnasirichaikul S, Rades T, Tucker IG, Davies NM. In-vitro release and oral bioactivity of insulin in diabetic rats using nanocapsules dispersed in biocompatible microemulsion. J Pharm Pharmacol, 2002;54:473-80. (Pubitemid 34308489)
70. Woitiski CB, Neufeld RJ, Veiga F, Carvalho RA, Figueiredo IV. Pharmacological effect of orally delivered insulin facilitated by multilayered stable nanoparticle. Eur J Pharm Sci, 2010;41:556-63.
71. Wu ZM, Zhou L, Guo XD, Jiang W, Ling L, Qian Y, Luo KQ, Zhang LJ. HP55-coated capsule containing PLGA/RS nanoparticles for oral delivery of insulin. Int J Pharm, 2012;425:1-8.
72. Yamamoto A, Taniguchi T, Rikyuu K, Tsuji T, Fujita T, Murakami M, Muranishi S. Effects of various protease inhibitors on the intestinal absorption and degradation of insulin in rats. Pharm Res, 1994;11(10):1496-500. (Pubitemid 24339662)
73. Yang SZ, Huang YD, Jie XF, Feng YM, Niu JY. Relationship between insulin A chain regions and insulin biological activities. World J Gastroenterol, 2000;6(3):371-3. (Pubitemid 30392132)
74. Yin L, Ding J, He C, Cui L, Tan C, Yin C. Drug permeability and mucoadhesion properties of thiolated trimethyl chitosan nanoparticles in oral insulin delivery. Biomaterials, 2009;30:5691-700.
75. Zhang X, Sun M, Zheng A, Cao D, Bi Y, Sun J. Preparation and characterization of insulin-loaded bioadhesive PLGA nanoparticles for oral administration. Eur J Pharm Sci, 2012a;45:632-8.
76. Zhang Y, Wei W, Lv P, Wang L, Ma G. Preparation and evaluation of alginate- chitosan microspheres for oral delivery of insulin. Eur J Pharm Biopharm, 2011;77:11-19.
77. Zhang Y, Wu X, Meng L, Zhang Y, Ai R, Qi N, He H, Xu H, Tang X. Thiolated Eudragit nanoparticles for oral insulin delivery: Preparation, characterization and in vivo evaluation. Int J Pharm, 2012b;436:341-50. Biológicas