Gastrointestinal distribution and absorption behavior of Eudragit-coated chitosan-prednisolone conjugate microspheres in rats with TNBS-induced colitis

International Journal of Pharmaceutics

Volumn 348, Issue 1-2, 2008, Pages 80-88

  Oosegi, Tomoko ^a   Onishi, Hiraku ^a   Machida, Yoshiharu ^a  

^a HOSHI UNIVERSITY   (Japan)

Author keywords

Drug release; Eudragit L100 coated chitosan prednisolone conjugate microspheres; Gastrointestinal distribution; Plasma concentration; TNBS induced colitis

Indexed keywords

CHITOSAN; EUDRAGIT; MICROSPHERE; PREDNISOLONE; TRINITROBENZENESULFONIC ACID;

ANALYTIC METHOD; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; COLITIS; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG CONJUGATION; DRUG DELIVERY SYSTEM; DRUG DISTRIBUTION; DRUG RELEASE; DRUG SYNTHESIS; GASTROINTESTINAL ABSORPTION; MALE; NONHUMAN; PARTICLE SIZE; PH; PRIORITY JOURNAL; RAT;

ACRYLATES; ADMINISTRATION, ORAL; ANIMALS; ANTI-INFLAMMATORY AGENTS; AREA UNDER CURVE; BIOLOGICAL AVAILABILITY; CECUM; CHITOSAN; COLITIS; COLON; HYDROGEN-ION CONCENTRATION; INTESTINAL ABSORPTION; INTESTINE, SMALL; MALE; MICROSCOPY, ELECTRON, SCANNING; MICROSPHERES; PARTICLE SIZE; POLYMERS; PREDNISOLONE; RATS; RATS, WISTAR; STOMACH; SURFACE PROPERTIES; TISSUE DISTRIBUTION; TRINITROBENZENESULFONIC ACID; VEHICLES;

EID: 37249092895     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2007.07.007     Document Type: Article

References (36)

1. Akhgari A., Afrasiabi Garekani H., Sadeghi F., and Azimaie M. Statistical optimization of indomethacin pellets coated with pH-dependent methacrylic polymers for possible colonic drug delivery. Int. J. Pharm. 305 (2005) 22-30
2. Ardizzone S., and Bianchi P.G. A practical guide to the management of distal ulcerative colitis. Drugs 55 (1998) 519-542
3. Brzezinski A., Rankin G.B., Seidner D.L., and Lashner B.A. Use of old and new oral 5-aminosalicylic acid formulations in inflammatory bowel disease. Cleve. Clin. J. Med. 62 (1995) 317-323
4. Campieri M., Ferguson A., Doe W., Persson T., and Nilsson L.G. Oral budesonide is as effective as oral prednisolone in active Crohn's disease. The Global Budesonide Study Group. Gut 41 (1997) 209-214
5. Desai M.P., Labhasetwar V., Amidon G.L., and Levy R.J. Gastrointestinal uptake of biodegradable microparticles: effect of particle size. Pharm. Res. 13 (1996) 1838-1845
6. Fiocchi C. Inflammatory bowel disease. Current concepts of pathogenesis and implications for therapy. Minerva Gastroenterol. Dietol. 48 (2002) 215-226
7. Friend D.R. New oral delivery systems for treatment of inflammatory bowel disease. Adv. Drug Deliv. Rev. 57 (2005) 247-265
8. Gionchetti P., Rizzello F., Habal F., Morselli C., Amadini C., Romagnoli R., and Campieri M. Standard treatment of ulcerative colitis. Dig. Dis. 21 (2003) 157-167
9. Jani P., Halbert G.W., Langridge J., and Florence A.T. The uptake and translocation of latex nanospheres and microspheres after oral administration to rats. J. Pharm. Pharmacol. 41 (1989) 809-812
10. Kesisoglou F., and Zimmermann E.M. Novel drug delivery strategies for the treatment of inflammatory bowel disease. Expert Opin. Drug Deliv. 2 (2005) 451-463
11. Khan M.Z., Stedul H.P., and Kurjakovic N. A pH-dependent colon-targeted oral drug delivery system using methacrylic acid copolymers. II. Manipulation of drug release using Eudragit L100 and Eudragit S100 combinations. Drug Dev. Ind. Pharm. 26 (2000) 549-554
12. Klotz U. Clinical pharmacokinetics of sulphasalazine, its metabolites and other prodrugs of 5-aminosalicylic acid. Clin. Pharmacokinet. 10 (1985) 285-302
13. Lamprecht A., Schafer U., and Lehr C.M. Microparticle targeting to the inflamed colonic mucosa for the treatment of inflammatory bowel disease: in vivo results from rat. AAPS PharmSci 2 (2000) 1930 (abstract)
14. Lamprecht A., Schafer U., and Lehr C.M. Size-dependent bioadhesion of micro- and nanoparticulate carriers to the inflamed colonic mucosa. Pharm. Res. 18 (2001) 788-793
15. Lamprecht A., Ubrich N., Yamamoto H., Schafer U., Takeuchi H., Maincent P., Kawashima Y., and Lehr C.M. Biodegradable nanoparticles for targeted drug delivery in treatment of inflammatory bowel disease. J. Pharmacol. Exp. Ther. 299 (2001) 775-781
16. Larouche J., Morais J., Picard M., Lambert C., Spenard J., Landriault H., Kennedy G., and Poitras P. Release of 5-ASA from Pentasa in patients with Crohn's disease of the small intestine. Aliment. Pharmacol. Ther. 9 (1995) 315-320
17. McLeod A.D., Friend D.R., and Tozer T.N. Synthesis and chemical stability of glucocorticoid-dextran esters: potential prodrugs for colon-specific delivery. In. J. Pharm. 92 (1993) 105-114
18. McLeod A.D., Friend D.R., and Tozer T.N. Glucocorticoid-dextran conjugates as potential prodrugs for colon-specific delivery: hydrolysis in rat gastrointestinal tract contents. J. Pharm. Sci. 83 (1994) 1284-1288
19. Morris G.P., Beck P.L., Herridge M.S., Depew W.T., Szewczuk M.R., and Wallace J.L. Hapten-induced model of chronic inflammation and ulceration in the rat colon. Gastroenterology 96 (1989) 795-803
20. Nakase H., Okazaki K., Tabata Y., Uose S., Ohana M., Uchida K., Matsushima Y., Kawanami C., Oshima C., Ikada Y., and Chiba T. Development of an oral drug delivery system targeting immune-regulating cells in experimental inflammatory bowel disease: a new therapeutic strategy. J. Pharmacol. Exp. Ther. 292 (2000) 15-21
21. Onishi H., Oosegi T., Machida Y., and McGinity J.W. Preparation and in vitro evaluation of chitosan microspheres containing prednisolone: comparison of simple and conjugate microspheres. Drug Dev. Ind. Pharm. 31 (2005) 597-605
22. Oosegi, T., Onishi, H., Machida, Y., in press. In vitro evaluation of enteric-coated chitosan-prednisolone conjugate microspheres as a delivery system for the treatment of inflammatory bowel disease: particle characteristics, morphological features and release behaviors. Eur. J. Pharm. Biopharm.
23. Rutgeerts P. The use of oral topically acting glucocorticosteroids in the treatment of inflammatory bowel disease. Mediators Inflamm. 7 (1998) 137-140
24. Sakuma S., Sudo R., Suzuki N., Kikuchi H., Akashi M., and Hayashi M. Mucoadhesion of polystyrene nanoparticles having surface hydrophilic polymeric chains in the gastrointestinal tract. Int. J. Pharm. 177 (1999) 161-172
25. Shimoda J., Onishi H., and Machida Y. Bioadhesive characteristics of chitosan microspheres to the mucosa of rat small intestine. Drug Dev. Ind. Pharm. 27 (2001) 567-576
26. Sinha V.R., and Kumria R. Coating polymers for colon specific drug delivery: a comparative in vitro evaluation. Acta Pharm. 53 (2003) 41-47
27. Sugimoto K., Yoshida M., Yata T., Higaki K., and Kimura T. Evaluation of poly(vinyl alcohol)-gel spheres containing chitosan as dosage form to control gastrointestinal transit time of drugs. Biol. Pharm. Bull. 21 (1998) 1202-1206
28. Tabata Y., and Ikada Y. Effect of the size and surface charge of polymer microspheres on their phagocytosis by macrophage. Biomaterials 9 (1988) 356-362
29. Tabata Y., Inoue Y., and Ikada Y. Size effect on systemic and mucosal immune responses induced by oral administration of biodegradable microspheres. Vaccine 14 (1996) 1677-1685
30. Tozaki H., Fujita T., Odoriba T., Terabe A., Okabe S., Muranishi S., and Yamamoto A. Validation of a pharmacokinetic model of colon-specific drug delivery and the therapeutic effects of chitosan capsules containing 5-aminosalicylic acid on 2,4,6-trinitrobenzenesulphonic acid-induced colitis in rats. J. Pharm. Pharmacol. 51 (1999) 1107-1112
31. Tozaki H., Odoriba T., Okada N., Fujita T., Terabe A., Suzuki T., Okabe S., Muranishi S., and Yamamoto A. Chitosan capsules for colon-specific drug deliver: 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
32. Van Der Lubben I.M., Konings F.A., Borchard G., Verhoef J.C., and Junginger H.E. In vivo uptake of chitosan microparticles by murine Peyer's patches: visualization studies using confocal laser scanning microscopy and immunohistochemistry. J. Drug Target. 9 (2001) 39-47
33. Watts P.J., Barrow L., Steed K.P., Wilson C.G., Spiller R.C., Melia C.D., and Davies M.C. The transit rate of different-sized model dosage forms through the human colon and the effects of a lactulose-induced catharsis. Int. J. Pharm. 87 (1992) 215-221
34. Wiwattanapatapee R., Lomlim L., and Saramunee K. Dendrimers conjugates for colonic delivery of 5-aminosalicylic acid. J. Control. Release. 88 (2003) 1-9
35. Yamaoka K., Tanigawara Y., Nakagawa T., and Uno T. A pharmacokinetic analysis program (multi) for microcomputer. J. Pharmacobiodyn. 4 (1981) 879-885
36. Yano H., Hirayama F., Kamada M., Arima H., and Uekama K. Colon-specific delivery of prednisolone-appended alpha-cyclodextrin conjugate: alleviation of systemic side effect after oral administration. J. Control. Release 79 (2002) 103-112