Comparison of the effect of different chitosan salts and N-trimethyl chitosan chloride on the permeability of intestinal epithelial cells (Caco-2)

Journal of Controlled Release

Volumn 51, Issue 1, 1998, Pages 35-46

  Kotzé, Awie F ^a   Lueßen, Henrik L ^b   De Leeuw, Bas J ^b   De Boer, Bert G ^c   Coos Verhoef, J ^b   Junginger, Hans E ^b  

^a NORTH WEST UNIVERSITY   (South Africa)

^b LEIDEN UNIVERSITY   (Netherlands)

^c LEIDEN UNIVERSITY   (Netherlands)

Author keywords

Absorption enhancers; Chitosan; Confocal laser scanning microscopy; N trimethyl chitosan chloride; Paracellular transport; Transepithelial electrical resistance

Indexed keywords

BIOCHEMICAL MARKER; CHITOSAN DERIVATIVE; N TRIMETHYLCHITOSAN CHLORIDE; UNCLASSIFIED DRUG;

ARTICLE; CELL TRANSPORT; CONTROLLED DRUG RELEASE; CONTROLLED STUDY; DRUG ABSORPTION; DRUG SOLUBILITY; DRUG SYNTHESIS; ELECTRIC RESISTANCE; HUMAN; HUMAN CELL; INTESTINE EPITHELIUM CELL; INTESTINE MUCOSA PERMEABILITY; LASER MICROSCOPY; PERMEABILITY; PRIORITY JOURNAL; PROTEIN QUATERNARY STRUCTURE; TIGHT JUNCTION;

BIOLOGICAL TRANSPORT; CACO-2 CELLS; CARBON RADIOISOTOPES; CELL MEMBRANE PERMEABILITY; CHITIN; CHITOSAN; ELECTRIC IMPEDANCE; EPITHELIAL CELLS; GLUTAMATES; HUMANS; INTESTINAL ABSORPTION; MANNITOL; MICROSCOPY, CONFOCAL; POLYETHYLENE GLYCOLS;

EID: 0345055299     PISSN: 01683659     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0168-3659(97)00154-5     Document Type: Article

References (22)

1. Fix J.A. Absorption enhancing systems for the GI system. J. Control. Release. 6:1987;151-156.
2. J.L. Madara, J.S. Trier, Functional morphology of the mucosa of the small intestine, in: L.R. Johnson (Ed.), Physiology of the Gastrointestinal Tract, 2nd. ed., Raven Press, New York, 1987, pp. 1251-1266.
3. Hochman J., Artursson P. Mechanisms of absorption enhancement and tight junction regulation. J. Control. Release. 29:1994;253-267.
4. Gumbiner B. Structure, biochemistry and essembly of epithelial tight junctions. Am. J. Physiol. 253:1987;749-758.
5. Madara J.L. Loosening tight junctions. Lessons from the intestine. J. Clin. Invest. 83:1989;1089-1094.
6. Lueßen H.L., de Leeuw B.J., Langemeÿer M.W.E., de Boer A.G., Verhoef J.C., Junginger H.E. Mucoadhesive polymers in peroral drug delivery. VI. Carbomer and chitosan improve the intestinal absorption of the peptide drug Buserelin In vivo. Pharm. Res. 13:1996;1666-1670.
7. Artursson P., Magnusson C. Epithelial transport of drugs in cell culture. II. Effect of extracellular calcium concentration on the paracellular transport of drugs of different lipophilicities across monolayers of intestinal eptihelial (Caco-2) cells. J. Pharm. Sci. 79:1990;595-600.
8. Tomita M., Hayashi M., Awazu S. Absorption-enhancing mechanism of EDTA, caprate and decanoylcarnitine in Caco-2 cells. J. Pharm. Sci. 85:1996;608-611.
9. Boulenc X., Roques C., Joyeux H., Berger Y., Fabre G. Bisphophonates increase tight junction permeability in the human intestinal epithelial (Caco-2) model. Int. J. Pharm. 123:1995;13-24.
10. Kriwet B., Kissel T. Poly(acrylic) acid microparticles widen the intercellular spaces of Caco-2 cell monolayers: an examination by confocal laser scanning microscopy. Eur. J. Pharm. Biopharm. 76:1996;233-240.
11. Illum L., Farraj N.F., Davis S.S. Chitosan as a novel nasal delivery system for peptide drugs. Pharm. Res. 11:1994;1186-1189.
12. Lueßen H.L., Rentel C.-O., Kotzé A.F., Lehr C.-M., de Boer A.G., Verhoef J.C., Junginger H.E. Mucoadhesive polymers in peroral peptide drug delivery. IV. Polycarbophil and chitosan are potent enhancers of peptide transport across intestinal mucosae in vitro. J. Control. Release. 45:1997;15-23.
13. Artursson P., Lindmark T., Davis S.S., Illum L. Effect of chitosan on the permeability of monolayers of intestinal epithelial cells (Caco-2). Pharm. Res. 11:1994;1358-1361.
14. Schipper N.G.M., Varum K.M., 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.
15. A.F. Kotze, H.L. Lueßen, B.J. de Leeuw, A.G. de Boer, J.C. Verhoef, H.E. Junginger, N-trimethyl chitosan chloride as a potential absorption enhancers across mucosal surfaces: in vitro evaluation in intestinal epithelial cells (Caco-2), Pharm. Res., submitted for publication.
16. Domard A., Rinaudo M., Terrassin C. New method for the quaternization of chitosan. Int. J. Macromol. 8:1986;105-107.
17. Borchard G., Lueßen H.L., de Boer A.G., Verhoef J.C., Lehr C.-M., Junginger H.E. The potential of mucoadhesive polymers in enhancing intestinal peptide drug absorption. III. Effects of chitosan glutamate and carbomer on epithelial tight junctions in vitro. J. Control. Release. 39:1996;131-138.
18. Noach A.B.J., Kurosaki Y., Blom-Roosemalen M.C.M., de Boer A.G., Breimer D.D. Cell-polarity dependent effect of chelation on the paracellular permeabilty of confluent Caco-2 cell monolayers. Int. J. Pharm. 90:1993;229-237.
19. Hurni M.A., Noach A.B.J., Blom-Roosemalen M.C.M., de Boer A.G., Nagelkerke J.F., Breimer D.D. Permeability enhancement in Caco-2 cell monolayers by sodium salicylate and sodium taurodihydrofusidate: Assessment of effect reversibility and imaging of transepithelial transport routes by confocal laser scanning microscopy. J. Pharmacol. Exp. Ther. 267:1993;942-950.
20. Lehr C.-M., Bouwstra J.A., Schacht E.H., Junginger H.E. In vitro evaluation of mucoadhesive proeperties of chitosan and some other natural polymers. Int. J. Pharm. 78:1992;43-48.
21. Meza I., Sabanero M., Stefani E., Cereijido M. Occluding junctions in MDCK cells: Modulation of transepithelial permeability by the cytoskeleton. J. Cell Biochem. 18:1982;407-421.
22. Madara J.L. Intestinal absorptive cell tight junctions are linked to cytoskeleton. Am. J. Physiol. 253:1987;C171-C175.