Improvement of intestinal absorption of insulin and water-soluble macromolecular compounds by chitosan oligomers in rats

International Journal of Pharmaceutics

Volumn 359, Issue 1-2, 2008, Pages 70-78

  Gao, Yang ^a   He, Lin ^a,b   Katsumi, Hidemasa ^a   Sakane, Toshiyasu ^a   Fujita, Takuya ^c   Yamamoto, Akira ^a  

^a KYOTO PHARMACEUTICAL UNIVERSITY   (Japan)

^b SICHUAN PROVINCIAL PEOPLE'S HOSPITAL   (China)

^c RITSUMEIKAN UNIVERSITY   (Japan)

Author keywords

Absorption enhancer; Chitosan oligomer; Insulin; Intestinal absorption; Membrane toxicity; Tight junction

Indexed keywords

CHITOSAN; DIMER; FLUORESCEIN ISOTHIOCYANATE DEXTRAN; INSULIN; LACTATE DEHYDROGENASE; OLIGOMER;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; COLON ABSORPTION; CONTROLLED STUDY; DRUG ABSORPTION; DRUG BLOOD LEVEL; ELECTRIC RESISTANCE; ENZYME ACTIVITY; HYDROPHILICITY; HYPOGLYCEMIA; INSULIN BLOOD LEVEL; INTESTINE ABSORPTION; INTESTINE EPITHELIUM; JEJUNUM; MALE; MOLECULAR WEIGHT; NONHUMAN; PRIORITY JOURNAL; PROTEIN SECRETION; RAT; STATISTICAL SIGNIFICANCE;

ADMINISTRATION, ORAL; ANIMALS; CHITOSAN; DEXTRANS; ELECTRIC IMPEDANCE; EXCIPIENTS; FLUORESCEIN-5-ISOTHIOCYANATE; INSULIN; INTESTINAL ABSORPTION; INTESTINAL MUCOSA; JEJUNUM; L-LACTATE DEHYDROGENASE; MALE; MOLECULAR WEIGHT; PERMEABILITY; RATS; RATS, WISTAR; SOLUBILITY; TIGHT JUNCTIONS;

EID: 44749091974     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2008.03.016     Document Type: Article

References (43)

1. Artursson P., Lindmark T., Davis S.S., and Illum L. Effect of chitosan on the permeability of monolayers of intestinal epithelial cells (Caco-2). Pharm. Res. 11 (1994) 1358-1361
2. Asada H., Douen T., Mizokoshi Y., Fujita T., Murakami M., Yamamoto A., and Muranishi S. Stability of acyl derivatives of insulin in the small intestine: relative importance of insulin association characteristics in aqueous solution. Pharm. Res. 11 (1994) 1115-1120
3. Asada H., Douen T., Waki M., Adachi S., Fujita T., Yamamoto A., and Muranishi S. Absorption characteristics of chemically modified-insulin derivatives with various fatty acids in the small and large intestine. J. Pharm. Sci. 84 (1995) 682-687
4. Bernkop-Schnurch A., and Krajicek M.E. Mucoadhesive polymers as platforms for peroral peptide delivery and absorption: synthesis and evaluation of different chitosan-EDTA conjugates. J. Control Release 50 (1998) 215-223
5. Carreno-Gomez B., and Duncan R. Evaluation of the biological properties of soluble chitosan and chitosan microspheres. Int. J. Pharm. 148 (1997) 231-240
6. Chandy T., and Sharma C.P. Chitosan as a biomaterial. Biomater. Art. Cells Art. Org. 18 (1990) 1-24
7. 1,7]-eel calcitonin in rats. J. Control Release 106 (2005) 287-297
8. 1,7]-eel calcitonin using chitosan capsules containing various additives in rats. J. Drug Target 14 (2006) 165-172
9. Gao Y., Lin H., Katsumi H., Sakane T., Fujita T., and Yamamoto A. Improvement of intestinal absorption of water-soluble macromolecules by various polyamines: intestinal mucosal toxicity and absorption-enhancing mechanism of spermine. Int. J. Pharm. 354 (2008) 126-134
10. Hamman J.H., Stander M., and Kotze A.F. Effect of the degree of quaternisation of N-trimethyl chitosan chloride on absorption enhancement: in vivo evaluation in rat nasal epithelia. Int. J. Pharm. 232 (2002) 235-242
11. Hirano S., Seino H., Akiyama Y., and Nonaka I. Biocompatibility of chitosan by oral and intravenous administrations. Polym. Eng. Sci. 59 (1988) 897-901
12. Illum L., Farraj N.F., and Davis S.S. Chitosan as a novel nasal delivery system for peptide drugs. Pharm. Res. 11 (1994) 1186-1189
13. Imai T., Shiraishi S., Saito H., and Otagiri M. Interaction of indomethacin with low molecular weight chitosan and improvements of some pharmaceutical properties of indomethacin by low molecular weight chitosans. Int. J. Pharm. 67 (1991) 11-20
14. Kotze A.F., de Leeuw B.J., Luessen H.L., de Boer A.G., Verhoef J.C., and Junginger H.E. Chitosans for enhanced delivery of therapeutic peptides across intestinal epithelia: in vitro evaluation in Caco-2 cell monolayers. Int. J. Pharm. 159 (1997) 243-253
15. Kotze A.F., Luessen H.L., de Leeuw B.J., de Boer B.G., Verhoef J.C., and Junginger H.E. N-trimethyl chitosan chloride as a potential absorption enhancer across mucosal surfaces: in vitro evaluation in intestinal epithelial cells (Caco-2). Pharm. Res. 14 (1997) 1197-1202
16. Lee V.H.L., and Yamamoto A. Penetration and enzymatic barriers to peptide and protein absorption. Adv. Drug Deliv. Rev. 4 (1989) 171-207
17. Lee V.H.L., Yamamoto A., and Kompella U.B. Mucosal penetration enhancers for facilitation of peptide and protein drug absorption. Crit. Rev. Ther. Drug Carrier Syst. 8 (1991) 91-192
18. Lehr C.M., Bouwstra J.A., Schacht E.H., and Junginger H.E. In vitro evaluation of mucoadhesive properties of chitosan and some other natural polymers. Int. J. Pharm. 78 (1992) 43-48
19. Miyake M., Minami T., Hirota M., Toguchi H., Odomi M., Ogawara K., Higaki K., and Kimura T. Novel oral formulation safely improving intestinal absorption of poorly absorbable drugs: utilization of polyamines and bile acids. J. Control Release 111 (2006) 27-34
20. Miyazaki S., Ishii K., and Nadai T. The use of chitin and chitosan as drug carriers. Chem. Pharm. Bull. 29 (1981) 3067-3069
21. Miyazaki S., Yamaguchi H., Yokouchi C., Takada M., and Hou W.-M. Sustained release and intragastric-floating granules of indomethacin using chitosan in rabbits. Chem. Pharm. Bull. 36 (1988) 4033-4038
22. 2EDTA, sodium glycocholate on intestinal absorption of insulin. Biol. Pharm. Bull. 16 (1993) 68-72
23. Sawayanagi Y., Nambu N., and Nagai T. Use of chitosan for sustained release preparations of water soluble drugs. Chem. Pharm. Bull. 30 (1982) 4213-4215
24. Sawayanagi Y., Nambu N., and Nagai T. Directly compressed tablets containing chitin or chitosan in addition to mannitol. Chem. Pharm. Bull. 30 (1982) 4216-4218
25. Schipper N.G., Olsson S., Hoogstraate J.A., de Boer A.G., Varum K.M., and Artursson P. Chitosans as absorption enhancers for poorly absorbable drugs 2: mechanism of absorption enhancement. Pharm. Res. 14 (1997) 923-929
26. Schipper N.G., Varum K.M., and Artursson P. Chitosans as absorption enhancers for poorly absorbable drugs: 1: influence of molecular weight and degree of acetylation on drug transport across human intestinal epithelial (Caco-2) cells. Pharm. Res. 13 (1996) 1686-1692
27. Smith J.M., Dornish M., and Wood E.J. Involvement of protein kinase C in chitosan glutamate-mediated tight junction disruption. Biomaterials 26 (2005) 3269-3276
28. Smith J., Wood E., and Dornish M. Effect of chitosan on epithelial cell tight junctions. Pharm. Res. 21 (2004) 43-49
29. Takayama K., Hirata M., Machida Y., Masada T., Sannan T., and Nagai T. Effect of interpolymer complex formation on bioadhesive property and drug release phenomenon of compressed tablet consisting of chitosan and sodium hyaluronate. Chem. Pharm. Bull. 38 (1990) 1993-1997
30. Thanou M.M., Kotze A.F., Scharringhausen T., Luessen H.L., de Boer A.G., Verhoef J.C., and Junginger H.E. Effect of degree of quaternizaiton of N-trimethyl chitosan chloride for enhanced transport of hydrophilic compounds across intestinal Caco-2 cell monolayers. J. Control Release 64 (2000) 15-25
31. Thanou M.M., Verhoef J.C., Romeijn S.G., Nagelkerke J.F., Merkus F.W., and Junginger H.E. Effects of N-trimethyl chitosan chloride, a novel absorption enhancer, on Caco-2 intestinal epithelia and the ciliary beat frequency of chicken embryo trachea. Int. J. Pharm. 185 (1999) 73-82
32. Tozaki H., Komoike J., Tada C., Maruyama T., Terabe A., Suzuki T., Yamamoto A., and Muranishi S. Chitosan capsules for colon-specific drug delivery: improvement of insulin absorption from the rat colon. J. Pharm. Sci. 86 (1997) 1016-1021
33. Uchiyama T., Yamamoto A., Hatano H., Fujita T., and Muranishi S. Effectiveness and toxicity screening of various absorption enhancers in the large intestine: intestinal absorption of phenol red and protein and phospholipids release from the intestinal membrane. Biol. Pharm. Bull. 19 (1996) 1618-1621
34. Uchiyama T., Sugiyama T., Quan Y.-S., Kotani A., Okada N., Fujita T., Muranishi S., and Yamamoto A. Enhanced permeability of insulin across the rat intestinal membrane by various absorption enhancers: their intestinal mucosal toxicity and absorption-enhancing mechanism of n-lauryl-β-d-maltopyranoside. J. Pharm. Pharmacol. 51 (1999) 1241-1250
35. Utoguchi N., Watanabe Y., Shida T., and Matsumoto M. Nitric oxide donors enhance rectal absorption of macromolecules in rabbits. Pharm. Res. 15 (1998) 870-876
36. Yamada K., Odomi M., Okada N., Fujita T., and Yamamoto A. Chitosan oligomers as potential and safe absorption enhancers for improving the pulmonary absorption of interferon-α in rats. J. Pharm. Sci. 94 (2005) 2432-2440
37. Yamamoto A., Hayakawa E., Kato Y., Nishiura A., and Lee V.H.L. A mechanistic study on enhancement of rectal permeability to insulin in the albino rabbit. J. Pharmacol. Exp. Ther. 263 (1992) 25-31
38. Yamamoto A., Taniguchi T., Rikyuu K., Tsuji T., Fujita T., Murakami M., and Muranishi S. Effects of various protease inhibitors on the intestinal absorption and degradation of insulin in rats. Pharm. Res. 11 (1994) 1496-1500
39. Yamamoto A., Umemori S., and Muranishi S. Absorption enhancement of intrapulmonary administered insulin by various absorption enhancers and protease inihibitors in rats. J. Pharm. Pharmacol. 46 (1994) 14-18
40. Yamamoto A., Uchiyama T., Nishikawa R., Fujita T., and Muranishi S. Effectiveness and toxicity screening of various absorption enhancers in the rat small intestine: effects of absorption enhancers on the intestinal absorption of phenol red and the release of protein and phospholipids from the intestinal membrane. J. Pharm. Pharmacol. 48 (1996) 1285-1289
41. Yamamoto A., Okagawa T., Kotani A., Uchiyama T., Shimura T., Tabata S., Kondo S., and Muranishi S. Effects of different absorption enhancers on the permeation of ebiratide, an ACTH analogue, across intestinal membranes. J. Pharm. Pharmacol. 49 (1997) 1057-1061
42. Yamamoto A., Tatsumi H., Maruyama M., Uchiyama T., Okada N., and Fujita T. Modulation of intestinal permeability by nitric oxide donors: implications in intestinal delivery of poorly absorbable drugs. J. Pharmacol. Exp. Ther. 296 (2001) 84-90
43. Yodoya E., Uemura K., Tenma T., Fujita T., Murakami M., Yamamoto A., and Muranishi S. Enhanced permeability of tetragastrin across the rat intestinal membrane and its reduced degradation by acylation with various fatty acids. J. Pharmacol. Exp. Ther. 271 (1994) 1509-1513