Colon-Targeted Oral Drug Delivery Systems: Design Trends and Approaches

AAPS PharmSciTech

Volumn 16, Issue 4, 2015, Pages 731-741

  Amidon, Seth ^a   Brown, Jack E ^a   Dave, Vivek S ^a  

^a ST JOHN FISHER COLLEGE   (United States)

Author keywords

colon targeting; factors affecting colon delivery; future trends; novel approaches; traditional approaches

Indexed keywords

ENZYME; POLYSACCHARIDE; PRODRUG;

ANATOMICAL VARIATION; ARTICLE; BIOADHESIVE SYSTEM; BIOAVAILABILITY; COLON; COLON SPECIFIC BIODEGRADABLE DELIVERY SYSTEM; COLON SPECIFIC DRUG DELIVERY SYSTEM; DRUG DELIVERY SYSTEM; HUMAN; INTESTINAL COLONIC TRANSIT TIME; INTESTINE TRANSIT TIME; MATRIX BASED SYSTEM; MULTIPARTICULATE SYSTEM; OSMOTIC CONTROLLED DELIVERY; OSMOTIC PRESSURE; PHYSICAL PHENOMENA; PHYSIOLOGY; POLYSACCHARIDE BASED DELIVERY SYSTEM; PRESSURE CONTROLLED DELIVERY; PRIORITY JOURNAL; PULSINCAP SYSTEM; TIMED RELEASE SYSTEM; VISCOSITY; DRUG EFFECTS; INTESTINE ABSORPTION; ORAL DRUG ADMINISTRATION;

ADMINISTRATION, ORAL; BIOLOGICAL AVAILABILITY; COLON; DRUG DELIVERY SYSTEMS; HUMANS; INTESTINAL ABSORPTION;

EID: 84937816427     PISSN: None     EISSN: 15309932     Source Type: Journal    
DOI: 10.1208/s12249-015-0350-9     Document Type: Article

References (84)

1. Das S, Deshmukh R, Jha A. Role of natural polymers in the development of multiparticulate systems for colon drug targeting. Syst Rev Pharmacy. 2010;1(1):79–85.
2. Leuva VR, Patel BG, Chaudhary DJ, Patel JN, Modasiya MMK. Oral colon-specific drug delivery system. J Pharm Res. 2012;5(4):2293–7.
3. Kumar M, Ali A, Kaldhone P, Shirode A, Kadam VJ. Report on pharmaceutical approaches to colon targeted drug delivery systems. J Pharm Res. 2010;3(3).
4. Philip AK, Philip B. Colon targeted drug delivery systems: a review on primary and novel approaches. Oman Med J. 2010;25(2):79–87.
5. Kumar P, Mishra B. Colon targeted drug delivery systems—an overview. Curr Drug Deliv. 2008;5(3):186–98.
6. Malayandi R, Kondamudi P, Ruby PK, Aggarwal D. Biopharmaceutical considerations and characterizations in development of colon targeted dosage forms for inflammatory bowel disease. Drug Deliv Transl Res. 2014;4(2):187–202.
7. Coupe AJ, Davis SS, Wilding IR. Variation in gastrointestinal transit of pharmaceutical dosage forms in healthy subjects. Pharm Res. 1991;8(3):360–4.
8. Dressman JB, Berardi RR, Dermentzoglou LC, Russell TL, Schmaltz SP, Barnett JL, et al. Upper gastrointestinal (GI) pH in young, healthy men and women. Pharm Res. 1990;7(7):756–61.
9. Ibekwe VC, Fadda HM, McConnell EL, Khela MK, Evans DF, Basit AW. Interplay between intestinal pH, transit time and feed status on the in vivo performance of pH responsive ileo-colonic release systems. Pharm Res. 2008;25(8):1828–35.
10. Rubinstein A. Microbially controlled drug delivery to the colon. Biopharm Drug Dispos. 1990;11(6):465–75.
11. Hebden JM, Blackshaw PE, Perkins AC, Wilson CG, Spiller RC. Limited exposure of the healthy distal colon to orally-dosed formulation is further exaggerated in active left-sided ulcerative colitis. Aliment Pharmacol Ther. 2000;14(2):155–61.
12. Rana SV, Sharma S, Malik A, Kaur J, Prasad KK, Sinha SK, et al. Small intestinal bacterial overgrowth and orocecal transit time in patients of inflammatory bowel disease. Dig Dis Sci. 2013;58(9):2594–8.
13. Stubbs JB, Valenzuela GA, Stubbs CC, Croft BY, Teates CD, Plankey MW, et al. A noninvasive scintigraphic assessment of the colonic transit of nondigestible solids in man. J Nucl Med. 1991;32(7):1375–81.
14. Christl SU, Scheppach W. Metabolic consequences of total colectomy. Scand J Gastroenterol Suppl. 1997;222:20–4.
15. Sandle GI. Salt and water absorption in the human colon: a modern appraisal. Gut. 1998;43(2):294–9.
16. Schiller C, Frohlich CP, Giessmann T, Siegmund W, Monnikes H, Hosten N, et al. Intestinal fluid volumes and transit of dosage forms as assessed by magnetic resonance imaging. Aliment Pharmacol Ther. 2005;22(10):971–9.
17. Shameem M, Katori N, Aoyagi N, Kojima S. Oral solid controlled release dosage forms: role of GI-mechanical destructive forces and colonic release in drug absorption under fasted and fed conditions in humans. Pharm Res. 1995;12(7):1049–54.
18. Pijper A, Discombe G. Shape and motility of bacteria. J Pathol Bacteriol. 1946;58(3):325–42.
19. Evans DF, Pye G, Bramley R, Clark AG, Dyson TJ, Hardcastle JD. Measurement of gastrointestinal pH profiles in normal ambulant human subjects. Gut. 1988;29(8):1035–41.
20. Fallingborg J, Christensen LA, Ingeman-Nielsen M, Jacobsen BA, Abildgaard K, Rasmussen HH. pH-profile and regional transit times of the normal gut measured by a radiotelemetry device. Aliment Pharmacol Ther. 1989;3(6):605–13.
21. Macfarlane GT, Gibson GR, Cummings JH. Comparison of fermentation reactions in different regions of the human colon. J Appl Bacteriol. 1992;72(1):57–64.
22. Bown RL, Gibson JA, Sladen GE, Hicks B, Dawson AM. Effects of lactulose and other laxatives on ileal and colonic pH as measured by a radiotelemetry device. Gut. 1974;15(12):999–1004.
23. Nugent SG, Kumar D, Rampton DS, Evans DF. Intestinal luminal pH in inflammatory bowel disease: possible determinants and implications for therapy with aminosalicylates and other drugs. Gut. 2001;48(4):571–7.
24. Gibson SA, McFarlan C, Hay S, MacFarlane GT. Significance of microflora in proteolysis in the colon. Appl Environ Microbiol. 1989;55(3):679–83.
25. Rowland IR. Factors affecting metabolic activity of the intestinal microflora. Drug Metab Rev. 1988;19(3–4):243–61.
26. Chung KT, Fulk GE, Egan M. Reduction of azo dyes by intestinal anaerobes. Appl Environ Microbiol. 1978;35(3):558–62.
27. Hejazi R, Amiji M. Chitosan-based gastrointestinal delivery systems. J Control Release. 2003;89(2):151–65.
28. Ratner BD, Gladhill KW, Horbett TA. Analysis of in vitro enzymatic and oxidative degradation of polyurethanes. J Biomed Mater Res. 1988;22(6):509–27.
29. Sinha VR, Kumria R. Polysaccharides in colon-specific drug delivery. Int J Pharm. 2001;224(1–2):19–38.
30. Kang M, Khanal T, Kim H, Lee D, Yeo H, Lee Y, et al. Role of metabolism by human intestinal microflora in geniposide-induced toxicity in HepG2 cells. Arch Pharm Res. 2012;35(4):733–8.
31. Nutt JG, Fellman JH. Pharmacokinetics of levodopa. Clin Neuropharmacol. 1984;7(1):35–49.
32. Azadkhan AK, Truelove SC, Aronson JK. The disposition and metabolism of sulphasalazine (salicylazosulphapyridine) in man. Br J Clin Pharmacol. 1982;13(4):523–8.
33. Hamedani R, Feldman RD, Feagan BG. Drug development in inflammatory bowel disease: budesonide-a model of targeted therapy. Aliment Pharmacol Ther. 1997;3:98–107.
34. French DL, Mauger JW. Evaluation of the physicochemical properties and dissolution characteristics of mesalamine: relevance to controlled intestinal drug delivery. Pharm Res. 1993;10(9):1285–90.
35. Nicholls A, Harris-Collazo R, Huang M, Hardiman Y, Jones R, Moro L. Bioavailability profile of Uceris MMX extended-release tablets compared with Entocort EC capsules in healthy volunteers. J Int Med Res. 2013;41(2):386–94.
36. Rabito MF, Reis AV, Freitas Ados R, Tambourgi EB, Cavalcanti OA. A pH/enzyme-responsive polymer film consisting of Eudragit® FS 30 D and arabinoxylane as a potential material formulation for colon-specific drug delivery system. Pharm Dev Technol. 2012;17(4):429–36.
37. Friend DR, Chang GW. A colon-specific drug-delivery system based on drug glycosides and the glycosidases of colonic bacteria. J Med Chem. 1984;27(3):261–6.
38. Friend DR, Chang GW. Drug glycosides: potential prodrugs for colon-specific drug delivery. J Med Chem. 1985;28(1):51–7.
39. Kim D, Hong S, Jung S, Jung Y, Kim YM. Synthesis and evaluation of N-nicotinoyl-2-{2-(2-methyl-5-nitroimidazol-1-yl)ethyloxy}-D,L-glycine as a colon-specific prodrug of metronidazole. J Pharm Sci. 2009;98(11):4161–9.
40. Kim H, Lee Y, Yoo H, Kim J, Kong H, Yoon JH, et al. Synthesis and evaluation of sulfate conjugated metronidazole as a colon-specific prodrug of metronidazole. J Drug Target. 2012;20(3):255–63.
41. Vaidya A, Jain S, Agrawal RK, Jain SK. Pectin-metronidazole prodrug bearing microspheres for colon targeting. J Saudi Chem Soc. 2012
42. Modasiya MK, Patel VM. Design of colon specific drug delivery using sodium alginate and HPMC. J Pharm Res. 2012;5(4):2253–8.
43. Cummings JH, Englyst HN. Fermentation in the human large intestine and the available substrates. Am J Clin Nutr. 1987;45(5 Suppl):1243–55.
44. Scheline RR. Metabolism of foreign compounds by gastrointestinal microorganisms. Pharmacol Rev. 1973;25(4):451–523.
45. Basit A, Bloor J. Perspectives on colonic drug delivery business briefing. Pharmatech. 2003:185–9.
46. Roos AA, Edlund U, Sjoberg J, Albertsson AC, Stalbrand H. Protein release from galactoglucomannan hydrogels: influence of substitutions and enzymatic hydrolysis by beta-mannanase. Biomacromolecules. 2008;9(8):2104–10.
47. Hita V, Singh R, Jain SK. Colonic targeting of metronidazole using azo aromatic polymers: development and characterization. Drug Deliv. 1997;4(1):19–22.
48. Ahmad MZ, Akhter S, Ahmad I, Singh A, Anwar M, Shamim M, et al. In vitro and in vivo evaluation of Assam Bora rice starch-based bioadhesive microsphere as a drug carrier for colon targeting. Expert Opin Drug Deliv. 2012;9(2):141–9.
49. Alvarez-Fuentes J, Fernández-Arévalo M, González-Rodríguez ML, Cirri M, Mura P. Development of enteric-coated timed-release matrix tablets for colon targeting. J Drug Target. 2004;12(9/10):607–12.
50. Fukui E, Miyamura N, Uemura K, Kobayashi M. Preparation of enteric coated timed-release press-coated tablets and evaluation of their function by in vitro and in vivo tests for colon targeting. Int J Pharm. 2000;204(1–2):7–15.
51. Gazzaniga A, Iamartino P, Maffione G, Sangalli ME. Oral delayed-release system for colonic specific delivery. Int J Pharm. 1994;108(1):77–83.
52. Chourasia MK, Jain SK. Design and development of multiparticulate system for targeted drug delivery to colon. Drug Deliv. 2004;11(3):201–7.
53. Hardy JG, Wilson CG, Wood E. Drug delivery to the proximal colon. J Pharm Pharmacol. 1985;37(12):874–7.
54. Vaidya A, Jain A, Khare P, Agrawal RK, Jain SK. Metronidazole loaded pectin microspheres for colon targeting. J Pharm Sci. 2009;98(11):4229–36.
55. Perera G, Barthelmes J, Bernkop-Schnurch A. Novel pectin-4-aminothiophenole conjugate microparticles for colon-specific drug delivery. J Control Release. 2010;145(3):240–6.
56. Ye L, Hong Z. Budesonide-loaded guar gum microspheres for colon delivery: preparation, characterization and in vitro/in vivo evaluation. Int J Mol Sci. 2015;16(2):2693–704.
57. Beckert T, Petereit HU, Dressman J, Rudolph M. Multi-particulate form of medicament, comprising at least two differently coated forms of pellet. Google Patents; 2005.
58. Agarwal T, Narayana SNGH, Pal K, Pramanik K, Giri S, Banerjee I. Calcium alginate-carboxymethyl cellulose beads for colon-targeted drug delivery. Int J Biol Macromol. 2015;75:409–17.
59. Beloqui A, Coco R, Memvanga PB, Ucakar B, des Rieux A, Preat V. pH-sensitive nanoparticles for colonic delivery of curcumin in inflammatory bowel disease. Int J Pharm. 2014;473(1–2):203–12.
60. Calabrese I, Cavallaro G, Scialabba C, Licciardi M, Merli M, Sciascia L, et al. Montmorillonite nanodevices for the colon metronidazole delivery. Int J Pharm. 2013;457(1):224–36.
61. Spada G, Gavini E, Cossu M, Rassu G, Giunchedi P. Solid lipid nanoparticles with and without hydroxypropyl-beta-cyclodextrin: a comparative study of nanoparticles designed for colonic drug delivery. Nanotechnology. 2012;23(9).
62. Mundargi RC, Patil SA, Agnihotri SA, Aminabhavi TM. Development of polysaccharide-based colon targeted drug delivery systems for the treatment of amoebiasis. Drug Dev Ind Pharm. 2007;33(3):255–64.
63. Gauri B, Singh SK, Mishra D. Formulation and evaluation of colon targeted oral drug delivery systems for metronidazole in treatment of amoebiasis. Int J Drug Del. 2011;3(3).
64. Shukla RK, Tiwari A. Carbohydrate polymers: applications and recent advances in delivering drugs to the colon. Carbohydr Polym. 2012;88(2):399–416.
65. Bassi P, Kaur G. pH modulation: a mechanism to obtain pH-independent drug release. Expert Opin Drug Deliv. 2010;7(7):845–57.
66. Kosaraju SL. Colon targeted delivery systems: review of polysaccharides for encapsulation and delivery. Crit Rev Food Sci Nutr. 2005;45(4):251–8.
67. Liu L, Fishman ML, Kost J, Hicks KB. Pectin-based systems for colon-specific drug delivery via oral route. Biomaterials. 2003;24(19):3333–43.
68. Wakerly Z, Fell JT, Attwood D, Parkins D. Studies on drug release from pectin/ethylcellulose film-coated tablets: a potential colonic delivery system. Int J Pharm. 1997;153(2):219–24.
69. Maroni A, Zema L, Loreti G, Palugan L, Gazzaniga A. Film coatings for oral pulsatile release. Int J Pharm. 2013;457(2):362–71.
70. Obitte N, Chukwu A. The synergistic effect of Landolphia owariensis latex and Eudragit L-100-coated capsules on the in vitro controlled release of metronidazole for possible colon targeting. Asian J Pharm. 2011;5(2):75–83.
71. Leopold CS, Eikeler D. Eudragit E as coating material for the pH-controlled drug release in the topical treatment of inflammatory bowel disease (IBD). J Drug Target. 1998;6(2):85–94.
72. Yassin AE, Alsarra IA, Alanazi FK, Al-Mohizea AM, Al-Robayan AA, Al-Obeed OA. New targeted-colon delivery system: in vitro and in vivo evaluation using X-ray imaging. J Drug Target. 2010;18(1):59–66.
73. Kadiyam R, Muzib YI. Colon specific drug delivery of tramadol HCl for chronotherapeutics of arthritis. Int J Pharm Investig. 2015;5(1):43–9.
74. Maroni A, Del Curto MD, Cerea M, Zema L, Foppoli A, Gazzaniga A. Polymeric coatings for a multiple-unit pulsatile delivery system: preliminary study on free and applied films. Int J Pharm. 2013;440(2):256–63.
75. Santus G, Baker RW. Osmotic drug delivery: a review of the patent literature. J Control Release. 1995;35(1):1–21.
76. Verma RK, Krishna DM, Garg S. Formulation aspects in the development of osmotically controlled oral drug delivery systems. J Control Release. 2002;79(1–3):7–27.
77. Sethi S, Harikumar SL, Nirmala. Review on advances in colon targeted drug delivery system. Int J Pharm Sci Res. 2012;3(9):2989–3000.
78. Takaya T, Niwa K, Muraoka M, Ogita I, Nagai N, Yano R-i, et al. Importance of dissolution process on systemic availability of drugs delivered by colon delivery system. J Control Release. 1998;50(1–3):111–22.
79. Hay DJ, Sharma H, Irving MH. Spread of steroid-containing foam after intrarectal administration. Br Med J. 1979;1(6180):1751–3.
80. Philip AK, Pathak K. Osmotic flow through asymmetric membrane: a means for controlled delivery of drugs with varying solubility. AAPS PharmSciTech. 2006;7(3):56.
81. Abraham S, Srinath M. Development of modified pulsincap drug delivery system of metronidazole for drug targeting. Indian J Pharm Sci. 2007;69(1):24–7.
82. Krogel I, Bodmeier R. Pulsatile drug release from an insoluble capsule body controlled by an erodible plug. Pharm Res. 1998;15(3):474–81.
83. Huanbutta K, Sriamornsak P, Luangtana-Anan M, Limmatvapirat S, Puttipipatkhachorn S, Lim LY, et al. Application of multiple stepwise spinning disk processing for the synthesis of poly(methyl acrylates) coated chitosan-diclofenac sodium nanoparticles for colonic drug delivery. Eur J Pharm Sci. 2013;50(3–4):303–11.
84. Marieb EN, Hoehn K. Human anatomy and physiology. 7th ed. San Francisco: Pearson Benjamin Cummings; 2007.