Drug Res (Stuttg) 2013; 63(12): 657-662
DOI: 10.1055/s-0033-1349129
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

Influence of Beta-cyclodextrin and Chitosan in the Formulation of a Colon-Specific Drug Delivery System

K. Rehman
1   Centre for Drug Delivery Research, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Kuala Lumpur, Malaysia
M. C. I. M. Amin
1   Centre for Drug Delivery Research, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Kuala Lumpur, Malaysia
S. Muda
1   Centre for Drug Delivery Research, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Kuala Lumpur, Malaysia
› Author Affiliations
Further Information

Publication History

received 14 April 2013

accepted 12 June 2013

Publication Date:
10 July 2013 (online)


The increase in diseases of the colon underscores the need to develop cost-effective site-directed therapies. We formulated a polysaccharide-based matrix system that could release ibuprofen under conditions simulating those in the colon by employing a wet granulation method. Tablets were prepared in a series of formulations containing a polysaccharide (beta-cyclodextrin and chitosan) matrix system along with ethylcellulose. We characterized physicochemical properties and performed an in vitro drug release assay in the absence and presence of digestive enzymes to assess the ability of the polysaccharides to function as a protective barrier against the upper gastrointestinal environment. Fourier transform infrared spectroscopy studies revealed no chemical interaction between ibuprofen and polysaccharides; however, spectrum analysis suggested the formation of an inclusion complex of beta-cyclodextrin with ibuprofen. The formulations contained 50% ethylcellulose and 50% beta-cyclodextrins (1:1) were proven to be the better formulation that slowly released the drug until 24 h (101.04±0.65% maximum drug release in which 83.08±0.89% drug was released in colonic medium) showed better drug release profiles than the formulations containing chitosan. We conclude that a beta-cyclodextrin drug carrier system may represent an effective approach for treatment of diseases of the colon.

  • References

  • 1 Jemal A, Bray F, Center MM et al. Global cancer statistics. CA cancer J Clin 2011; 61: 69-90
  • 2 Ahmed IS, Ayres JW. Comparision of in vitro and in vivo performance of a colonic delivery system. Int J of Pharmaceutics 2011; 409: 169-177
  • 3 Friend DR. New oral delivery systems for treatment of inflammatory bowel disease. Adv Drug Delivery Rev 2005; 57: 247-265
  • 4 Oluwatoyin AO. Potentials of tropical starches as pharmaceutical excipients: A review. Starch 2012; 65: 89-105
  • 5 Yanqing C. A novel pH-sensitive hydrogels for potential colon-specific drug delivery: Characterization and in vitro release studies. Starch 2011; 63: 503-511
  • 6 Sinha VR, Rachna K. Polysaccharides in colon-specific drug delivery. Int J of Pharmaceutics 2001; 224: 19-38
  • 7 Hart AL, Stagg AJ, Frame M et al. The role of the gut flora in health and disease and its modifcation as therapy. Ailment Pharmacol Ther 2002; 16: 1383-1393
  • 8 Houwei T, Yi Q, Xiaohua H et al. Study of the sigmoidal swelling kinetics of carboxymethylchitosan-g-poly (acrylic acid) hydrogels intended for colon-specific drug delivery. Carbohydr Polym 2010; 82: 440-445
  • 9 Glen P, Jan B, Andreas B-S. Novel pectin-4-aminothiophenole conjugate microparticles for colon-specific drug delivery. J Control Release 2010; 145: 240-246
  • 10 Hideki Y, Fumitoshi H, Makoto K et al. Colon-specific delivery of prednisolone-appended α-cyclodextrin conjugate: alleviation of systemic side effect after oral administration. J Control Release 2002; 79: 103-112
  • 11 Mohmmad RS, Roya MT, Abel M et al. Synthesis and in vitro evaluation of carboxymethyl starch-chitosan nanoparticles as drug delivery system to the colon. Int J Biol Macromol 2011; 48: 381-385
  • 12 Marianne H, Terje S, Sverre AS. Immersion coating of pellet cores consisting of chitosan and calcium intended for colon drug delivery. Eur J Pharm Biopharm 2010; 75: 245-253
  • 13 Mennini N, Furlanetto S, Cirri M et al. Quality by design approach for developing chitosan-Ca-alginate microspheres for colon delivery of celecoxib-hydroxypropyl-β-cyclodextrin-PVP complex. Eur J Pharm Biopharm 2012; 80: 67-75
  • 14 Claus-Michael L, Joke AB, Etienne HS et al. In vitro evaluation of mucoadhesive properties of chitosan and some other natural polymers. Int J of Pharmaceutics 1992; 78: 43-48
  • 15 Hideyuki T, Tomokazu O, Naoki O et al. 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 2002; 82: 51-61
  • 16 Tozaki H, Komoike J, Tada C et al. Chitosan capsules for colon-specific drug delivery: improvement of insulin absorption from the rat colon. J Pharm Sci 1997; 86: 1016-1021
  • 17 Panos I, Acosta N, Heras A. New Drug Delivery Systems Based on Chitosan. Curr Drug Discovery Technol 2008; 5: 333-341
  • 18 Hiryama F, Uekama F. Cyclodextrin-based controlled drug release system. Adv Drug Delivery Rev 1999; 36: 125-141
  • 19 Beatriz P-V, Carmen R-T, Jose FRDS et al. Modulating drug release with cyclodextrins in hydroxypropyl methylcellulose gels and tablets. J Control Release 2004; 94: 351-363
  • 20 Zou MJ, Cheng G, Okamoto H et al. Colon-specific drug delivery systems based on cyclodextrin prodrugs: In vivo evaluation of 5-aminosalicylic acid from its cyclodextrin conjugates. World J Gastroenterol 2005; 11: 7457-7460
  • 21 Fetzner A, Bohm S, Schreder S et al. Degradation of raw or film-incorporated β-cyclodextrin by enzymes and colonic bacteria. Eur J Pharm Biopharm 2004; 58: 91-97
  • 22 Hua Z, Ibrahim AA, Steven HN. An in vitro evaluation of a chitosan-containing multiparticulate system for macromolecule delivery to the colon. Int J of Pharmaceutics 2002; 239: 197-205
  • 23 Fan L-F, Hei W, Chang Y-Z et al. Studies of chitosan/Kollicoat SR 30D film-coated tablets for colonic drug delivery. Int J Pharm 2009; 375: 8-15
  • 24 Sameer GL, Banga AK. Response Surface Methodology to Optimize Novel Fast Disintegrating Tablets Using β Cyclodextrin as Diluent. AAPS PharmaSciTech 2010; 11: 1627-1635
  • 25 Pruthvipathy RK, Sathyanarayana MU, Steven HN et al. Ethylcellulose matrix controlled release tablets of a water-soluble drug. Int J of Pharmaceutics 1995; 123: 119-125
  • 26 Monica CC, Mark JC, James WA. New dissolution method for mesalamine tablets and capsules. Dissolut Technol 2008; 15: 7-14
  • 27 Challa R, Ahuja A, Ali J et al. Cyclodextrins in drug delivery: an updated review. AAPS PharmaSciTech 2005; 6: 329-357
  • 28 Wong TW, Colombo G, Sonvico F. Pectin Matrix as Oral Drug Delivery Vehicle for Colon Cancer Treatment. AAPS PharmaSciTech 2011; 1: 201-214
  • 29 Rebecca LC, Lee AM, Imran A. The utility of cyclodextrins for enhancing oral bioavailability. J Control Release 2007; 123: 78-99