Chitosan as a pore former in coated beads for colon specific drug delivery of 5-ASA

International Journal of Pharmaceutics

Volumn 441, Issue 1-2, 2013, Pages 343-351

  Omwancha, Wycliffe S ^a,b   Mallipeddi, Rama ^c   Valle, Brenda L ^a   Neau, Steven H ^a  

^a UNIVERSITY OF THE SCIENCES   (United States)

^b MERCK RESEARCH LABORATORIES   (United States)

^c DEPARTMENT OF MEDICINE   (United States)

Author keywords

Biodegradable polymer; Chitosan; Colonic drug delivery; Controlled delivery; Excipients; Extrusion; Formulation; Site specific delivery; Spheronization

Indexed keywords

CHITOSAN; ETHYL CELLULOSE; MESALAZINE; POLYMER;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG COATING; DRUG DELIVERY SYSTEM; DRUG DIFFUSION; DRUG FORMULATION; DRUG RELEASE; FACTORIAL DESIGN; INTESTINE FLUID; MALE; NONHUMAN; PRIORITY JOURNAL; RAT; SPHERONIZATION; STOMACH JUICE;

ANIMALS; ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; CELLULOSE; CHITOSAN; COLON; DRUG CARRIERS; DRUG DELIVERY SYSTEMS; EXCIPIENTS; MALE; MESALAMINE; RATS; RATS, SPRAGUE-DAWLEY; TISSUE DISTRIBUTION;

EID: 84872790266     PISSN: 03785173     EISSN: 18733476     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2012.11.022     Document Type: Article

References (83)

1. D. Blok, J. Arndt, F. De Haan, P. Vermeij, H. Junginger, and E. Pauwels Scintigraphic investigation of the gastric emptying of 3 mm pellets in human volunteers Int. J. Pharm. 73 1991 171 176
2. J.T. Carstensen Pharmaceutical Principles of Solid Dosage Forms 1993 Technomic Lancaster
3. M. Chourasia, and S. Jain Pharmaceutical approaches to colon targeted drug delivery systems J. Pharm. Pharm. Sci. 6 2003 33 66
4. J. Christensen Motility in the colon L.R. Johnson, Physiology of the Gastrointestinal Tract 1st ed. 1981 Raven Press New York 445 471
5. J. Cummings, J. Banwell, I. Segal, N. Coleman, H. Englyst, and G. Macfarlane The amount and composition of large bowel contents in man J. Gastroenterol. 98 1990 A408
6. S.S. Davis, J.G. Hardy, M.J. Taylor, D.R. Whalley, and C.G. Wilson The effect of food on the gastrointestinal transit of pellets and an osmotic device (Osmet) Int. J. Pharm. 21 1984 331 340
7. V. Dodane, and V.D. Vilivalam Pharmaceutical applications of chitosan Pharm. Sci. Technol. Today 1 1998 246 253
8. A. Domard Determination of N-acetyl content in chitosan samples by cd measurements Int. J. Biol. Macromol. 9 1987 333 336
9. D. Evans, G. Pye, R. Bramley, A. Clark, T. Dyson, and J. Hardcastle Measurement of gastrointestinal pH profiles in normal ambulant human subjects Gut 29 1988 1035 1041
10. J. Fallingborg, L.A. Christensen, B.A. Jacobsen, and S.N. Rasmussen Very low intraluminal colonic pH in patients with active ulcerative colitis Dig. Dis. Sci. 38 1993 1989 1993
11. J. Fara Colonic drug absorption and metabolism L.F. Prescott, W.S. Nimmo, Novel Drug Delivery and its Therapeutic Application 1989 Wiley Chichester 103 112
12. I. Furda Aminopolysaccharides-their potential as dietary fiber I. Furda, Unconventional Sources of Dietary Fiber 1983 ACS Washington, DC 105 122
13. S.Q. Gao, Y. Sun, P. Kopečková, C.M. Peterson, and J. Kopeček Antitumor efficacy of colon specific HPMA copolymer/9 aminocamptothecin conjugates in mice bearing human colon carcinoma xenografts Macromol. Biosci. 9 2009 1135 1142
14. P. Goldman, and M. Peppercorn Drug therapy: sulfasalazine N. Engl. J. Med. 293 1975 20 23
15. R. Goodacre, M. Ali, B. Vanderlinden, J. Hamilton, M. Castelli, and T. Seaton Hemolytic anemia in patients receiving sulfasalazine Digestion 17 1978 503 508
16. R. Gulley, A. Mirza, and C. Kelly Hepatotoxicity of salicylazosulfapyridine: a case report and review of the literature Am. J. Gastroenterol. 72 1979 561 564
17. J. Hardy, C. Wilson, and E. Wood Drug delivery to the proximal colon J. Pharm. Pharmacol. 37 1985 874 877
18. G. Hawksworth, B. Drasar, and M. Hill Intestinal bacteria and the hydrolysis of glycosidic bonds J. Med. Microbiol. 4 1971 451 459
19. F. Hussain, R. Ajjan, M. Moustafa, J. Anderson, and S. Riley Simple method for the determination of 5-aminosalicylic and N-acetyl-5-aminosalicylic acid in rectal tissue biopsies J. Chromatogr. B: Biomed. Appl. 716 1998 257 266
20. D. Hutchings, B. Kuzmak, and A. Sakr Processing considerations for an EC latex coating system: influence of curing time and temperature Pharm. Res. 11 1994 1474 1478
21. Y. Karrout, C. Neut, F. Siepmann, D. Wils, P. Ravaux, L. Deremaux, M.P. Flament, L. Dubreuil, M. Lemdani, P. Desreumaux, and J. Siepmann Enzymatically degraded Eurylon 6 HP-PG: ethylcellulose film coatings for colon targeting in inflammatory bowel disease patients J. Pharm. Pharmacol. 62 2010 1676 1684
22. D. Kaushik, S. Sardana, and D.N. Mishra Implications of biodegradable and bioadhesive systems in colon delivery Int. J. Pharm. Sci. Drug Res. 1 2009 55 62
23. A. Kramar, S. Turk, and F. Vrecer Statistical optimisation of diclofenac sustained release pellets coated with polymethacrylic films Int. J. Pharm. 256 2003 43 52
24. P. Kumar, and B. Mishra Colon targeted drug delivery systems-an overview Curr. Drug Deliver. 5 2008 186 198
25. A. Lamprecht Multiparticulate systems in the treatment of inflammatory bowel disease Curr. Drug Target. Inflamm. Allergy 2 2003 137 144
26. H. Laroui, G. Dalmasso, H.T.T. Nguyen, Y. Yan, S.V. Sitaraman, and D. Merlin Drug-loaded nanoparticles targeted to the colon with polysaccharide hydrogel reduce colitis in a mouse model J. Gastroenterol. 138 2010 843 853
27. C. Leong, J. Newton, A. Basit, F. Podczeck, J. Cummings, and S. Ring The formation of colonic digestible films of amylose and ethylcellulose from aqueous dispersions at temperatures below 37°C Eur. J. Pharm. Biopharm. 54 2002 291 297
28. A. Levi, A. Fisher, L. Hughes, and W. Hendry Male infertility due to sulphasalazine Lancet 314 1979 276 278
29. Y. Liao, and D. Lee Slow release from a coated sphere with slight deformations of coating film and drug matrix J. Pharm. Sci. 86 1997 92 100
30. H. Liu, X.-G. Yang, S.-F. Nie, L.-L. Wei, L.-L. Zhou, H. Liu, R. Tang, and W.-S. Pan Chitosan-based controlled porosity osmotic pump for colon-specific delivery system: screening of formulation variables and in vitro investigation Int. J. Pharm. 332 2007 115 124
31. H.Y. Liu, X.T. Pi, X.L. Zheng, W.S. Hou, and J.G. Cui Pharmacokinetics of aminophylline delivered to the small intestine and colon using remote controlled capsules Chin. Med. J. (Engl.) 123 2010 320 325
32. W. Liu, S. Sun, Z. Cao, X. Zhang, K. Yao, W.W. Lu, and K. Luk An investigation on the physicochemical properties of chitosan/DNA polyelectrolyte complexes Biomaterials 26 2005 2705 2711
33. M.C. Madamba, W.M. Mullett, S. Debnath, and E. Kwong Characterization of tablet film coatings using a laser-induced breakdown spectroscopic technique AAPS PharmSciTech 8 2007 184 190
34. M. Mayo Pedrosa, C. Alvarez Lorenzo, I. Lacík, R. Martinez Pacheco, and A. Concheiro Sustained release pellets based on poly(N isopropyl acrylamide): matrix and in situ photopolymerization coated systems J. Pharm. Sci. 96 2007 93 105
35. E.L. McConnell, S. Murdan, and A.W. Basit An investigation into the digestion of chitosan (noncrosslinked and crosslinked) by human colonic bacteria J. Pharm. Sci. 97 2008 3820 3829
36. E.L. McConnell, J. Tutas, M.A.M. Mohamed, D. Banning, and A.W. Basit Colonic drug delivery using amylose films: the role of aqueous ethylcellulose dispersions in controlling drug release Cellulose 14 2007 25 34
37. J. Meyer, J. Elashoff, V. Porter-Fink, J. Dressman, and G. Amidon Human postprandial gastric emptying of 1-3-millimeter spheres J. Gastroenterol. 94 1988 1315 1325
38. A.A. Mihas, D.J. Goldenberg, and R.L. Slaughter Sulfasalazine toxic reactions J. Am. Med. Assoc. 239 1978 2590 2591
39. S. Milojevic, J.M. Newton, J.H. Cummings, G.R. Gibson, R. Louise Botham, S.G. Ring, M. Stockham, and M.C. Allwood Amylose as a coating for drug delivery to the colon: preparation and in vitro evaluation using 5-aminosalicylic acid pellets J. Control. Release 38 1996 75 84
40. H. Natsume, K. Sugibayashi, and Y. Morimoto In vitro release profile of mitomycin C from albumin microspheres: extrapolation from macrospheres to microspheres Pharm. Res. 8 1991 185 190
41. J. Nunthanid, M. Luangtana-anan, P. Sriamornsak, S. Limmatvapirat, K. Huanbutta, and S. Puttipipatkhachorn Use of spray-dried chitosan acetate and ethylcellulose as compression coats for colonic drug delivery: effect of swelling on triggering in vitro drug release Eur. J. Pharm. Biopharm. 71 2009 356 361
42. H. Nurulaini, and T.W. Wong Design of in situ dispersible and calcium cross-linked alginate pellets as intestinal-specific drug carrier by melt pelletization technique J. Pharm. Sci. 100 2011 2248 2257
43. W. Omwancha, C. Kouba, S. Yelamanchili, and S.H. Neau Colon-specific drug delivery using ethylcellulose and chitosan in the coat of compression-coated tablets Drug Dev. Ind. Pharm. 37 2011 945 953
44. D.J. Ormrod, C.C. Holmes, and T.E. Miller Dietary chitosan inhibits hypercholesterolaemia and atherogenesis in the apolipoprotein E-deficient mouse model of atherosclerosis Atherosclerosis 138 1998 329 334
45. M.G. Paoletti, L. Norberto, R. Damini, and S. Musumeci Human gastric juice contains chitinase that can degrade chitin Ann. Nutr. Metab. 51 2007 244 251
46. N.A. Peppas, and J.J. Sahlin A simple equation for the description of solute release. III. Coupling of diffusion and relaxation Int. J. Pharm. 57 1989 169 172
47. M.A. Peppercorn, and P. Goldman The role of intestinal bacteria in the metabolism of salicylazosulfapyridine J. Pharmacol. Exp. Ther. 181 1972 555 562
48. A. Press, I. Hauptmann, L. Hauptmann, B. Fuchs, M. Fuchs, K. Ewe, and G. Ramadori Gastrointestinal pH profiles in patients with inflammatory bowel disease Aliment. Pharmacol. Ther. 12 1998 673 678
49. R. Prizont, and N. Konigsberg Identification of bacterial glycosidases in rat cecal contents Dig. Dis. Sci. 26 1981 773 777
50. I.R. Rowland, A.K. Mallett, and A. Wise A comparison of the activity of five microbial enzymes in cecal content from rats, mice, and hamsters, and response to dietary pectin Toxicol. Appl. Pharmacol. 69 1983 143 148
51. P. Roy, and A. Shahiwala Multiparticulate formulation approach to pulsatile drug delivery: current perspectives J. Control. Release 134 2009 74 80
52. A. Rubinstein Approaches and opportunities in colon-specific drug delivery Crit. Rev. Ther. Drug Carrier Syst. 12 1995 101 149
53. A. Rubinstein, and R. Radai In vitro and in vivo analysis of colon specificity of calcium pectinate formulations Eur. J. Pharm. Biopharm. 41 1995 291 295
54. M. Sadeghi Synthesis and swelling behaviors of graft copolymer based on chitosan-g-poly (AA-co-HEMA) Int. J. Chem. Eng. Appl. 1 2010 354 358
55. M. Saffran, G.S. Kumar, C. Savariar, J.C. Burnham, F. Williams, and D.C. Neckers A new approach to the oral administration of insulin and other peptide drugs Science 233 1986 1081 1084
56. S. Sangekar, W.A. Vadino, I. Chaudry, A. Parr, R. Beihn, and G.A. Digenis Evaluation of the effect of food and specific gravity of tablets on gastric retention time Int. J. Pharm. 35 1987 187 191
57. R. Semdé, K. Amighi, M.J. Devleeschouwer, and A.J. Moës Effect of pectinolytic enzymes on the theophylline release from pellets coated with water insoluble polymers containing pectin HM or calcium pectinate Int. J. Pharm. 197 2000 169 179
58. Z.J. Shao, L. Morales, S. Diaz, and N.A. Muhammad Drug release from Kollicoat SR 30 D-coated nonpareil beads: evaluation of coating level, plasticizer type, and curing condition AAPS PharmSciTech 3 2002 87 96
59. S.J.K. Shirsagar, M.R. Bhalekar, G.N. Shukla, and S.K. Mohapatra Development and evaluation of multiparticulate colon targeted drug delivery system by combined approach of pH and bacteria Int. J. Pharm. Tech. Res. 3 2011 1139 1149
60. J. Siepmann, and N.A. Peppas Mathematical modeling of controlled drug delivery Adv. Drug Deliv. Rev. 48 2001 137 138
61. J. Siepmann, and N.A. Peppas Modeling of drug release from delivery systems based on hydroxypropyl methylcellulose (HPMC) Adv. Drug Deliv. Rev 48 2001 139 157
62. L.F. Siew, A.W. Basit, and J.M. Newton The properties of amylose-ethylcellulose films cast from organic-based solvents as potential coatings for colonic drug delivery Eur. J. Pharm. Sci. 11 2000 133 139
63. L.F. Siew, S.M. Man, J.M. Newton, and A.W. Basit Amylose formulations for drug delivery to the colon: a comparison of two fermentation models to assess colonic targeting performance in vitro Int. J. Pharm. 273 2004 129 134
64. G.L. Simon, and S.L. Gorbach The human intestinal microflora Dig. Dis. Sci. 31 1986 147 162
65. V. Sinha, and R. Kumria Microbially triggered drug delivery to the colon Eur. J. Pharm. Sci. 18 2003 3 18
66. O. Stoilova, N. Koseva, N. Manolova, and I. Rashkov Polyelectrolyte complex between chitosan and poly (2-acryloylamido-2-methylpropanesulfonic acid) Polym. Bull. 43 1999 67 73
67. P.O. Stotzer, and H. Abrahamsson Human postprandial gastric emptying of indigestible solids can occur unrelated to antral phase III Neurogastroenterol. Motil. 12 2000 415 419
68. M. Thanou, and H. Junginger Pharmaceutical applications of chitosan and derivatives S. Dimitriu, Polysaccharides: Structural Diversity and Functional Versatility 2nd ed. 2005 Marcel Dekker New York 661 677
69. H. Tozaki, T. Odoriba, N. Okada, T. Fujita, A. Terabe, T. Suzuki, S. Okabe, S. Muranishi, and A. Yamamoto Chitosan capsules for colon-specific drug delivery: enhanced localization of 5-aminosalicylic acid in the large intestine accelerates healing of TNBS-induced colitis in rats J. Control. Release 82 2002 51 61
70. T. Uchiyama, T. Sugiyama, Y.S. Quan, A. Kotani, N. Okada, T. Fujita, S. Muranishi, and A. Yamamoto Enhanced permeability of insulin across the rat intestinal membrane by various absorption enhancers: their intestinal mucosal toxicity and absorption-enhancing mechanism of n-lauryl-beta-d-maltopyranoside J. Pharm. Pharmacol. 51 1999 1241 1250
71. S.K. Umadevi, R. Thiruganesh, S. Suresh, and K.B. Reddy Formulation and evaluation of chitosan microspheres of aceclofenac for colon-targeted drug delivery Biopharm. Drug Dispos. 31 2010 407 427
72. K. Umprayn, P. Chitropas, and S. Amarekajorn Development of terbutaline sulfate sustained-release coated pellets Drug Dev. Ind. Pharm. 25 1999 477 491
73. G. Van den Mooter Colon drug delivery Expert Opin. Drug Deliv. 3 2006 111 125
74. Z. Wakerly, J. Fell, D. Attwood, and D. Parkins Studies on drug release from pectin/ethylcellulose film-coated tablets: a potential colonic delivery system Int. J. Pharm. 153 1997 219 224
75. S.L. Waller Differential measurement of small and large bowel transit times in constipation and diarrhoea: a new approach Gut 16 1975 372 378
76. W. Wang, S. Bo, S. Li, and W. Qin Determination of the Mark-Houwink equation for chitosans with different degrees of deacetylation Int. J. Biol. Macromol. 13 1991 281 285
77. H. Wei, F. Li Fang, B. Min, C. Yong Zhen, X. Bai, D. Qing, W. Feng, Q. Min, and C. De Ying Chitosan/Kollicoat SR 30D film coated pellets of aminosalicylates for colonic drug delivery J. Pharm. Sci. 99 2010 186 195
78. H. Wei, D. Qing, C. De Ying, X. Bai, and F. Li Fang In vitro and in vivo studies of pectin/ethylcellulose film coated pellets of 5 fluorouracil for colonic targeting J. Pharm. Pharmacol. 60 2008 35 44
79. H. Wei, D. Qing, C. De-Ying, and X. Bai Pectin/ethylcellulose as film coatings for colon-specific drug delivery: preparation and in vitro evaluation using 5-fluorouracil pellets J. Pharm. Sci. Technol. 61 2007 121 130
80. L. Yang Biorelevant dissolution testing of colon-specific delivery systems activated by colonic microflora J. Control. Release 125 2008 77 86
81. H. Zhang, and S.H. Neau In vitro degradation of chitosan by a commercial enzyme preparation: effect of molecular weight and degree of deacetylation Biomaterials 22 2001 1653 1658
82. H. Zhang, and S.H. Neau In vitro degradation of chitosan by bacterial enzymes from rat cecal and colonic contents Biomaterials 23 2002 2761 2766
83. X.L. Zhao, K.X. Li, X.F. Zhao, D.H. Pang, and D.W. Chen Study on colon-specific 5-Fu pH-enzyme di-dependent chitosan microspheres Chem. Pharm. Bull. (Tokyo) 56 2008 963 968