Effects of N-trimethyl chitosan chloride, a novel absorption enhancer, on Caco-2 intestinal epithelia and the ciliary beat frequency of chicken embryo trachea

International Journal of Pharmaceutics

Volumn 185, Issue 1, 1999, Pages 73-82

  Thanou, Maya M ^a   Verhoef, J Coos ^a   Romeijn, Stefan G ^a   Nagelkerke, J Fred ^a   Merkus, Frans W H M ^a   Junginger, Hans E ^a  

^a LEIDEN UNIVERSITY   (Netherlands)

Author keywords

Caco 2; Ciliary beat frequency; N trimethyl chitosan chloride; Texas red dextran; Tight junctions

Indexed keywords

CHITOSAN DERIVATIVE; N TRIMETHYLCHITOSAN; PENETRATION ENHANCING AGENT; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL TISSUE; ARTICLE; CELL DAMAGE; CELL STRAIN CACO 2; CHICKEN; CILIARY MOTILITY; CYTOTOXICITY; DRUG SAFETY; EMBRYO; HUMAN; HUMAN CELL; INTESTINE EPITHELIUM CELL; LASER MICROSCOPY; NONHUMAN; PRIORITY JOURNAL; TRACHEA;

ANIMALS; CACO-2 CELLS; CHICK EMBRYO; CHITIN; CHITOSAN; CILIA; DRUG CARRIERS; HUMANS; INTESTINAL MUCOSA; MICROSCOPY, CONFOCAL; POLYMERS; SURFACE-ACTIVE AGENTS; TRACHEA;

EID: 0032815732     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0378-5173(99)00126-X     Document Type: Article

References (28)

1. Ainge G., Bowles J.A.K., Mc Cormick S.G., Richards D.H., Scales M.D.C. Lack of deleterious effects of corticosteroid sprays containing benzalkonium chloride on nasal ciliated epithelium in vivo results in laboratory animals. Drug. Invest. 8:1994;127-133.
2. Anderberg E.K., Nyström C., Artursson P. Epithelial transport of drugs in cell culture. VI: effects of pharmaceutical surfactant excipients and bile acids on transepithelial permeability in monolayers of human intestinal epithelial (Caco-2) cells. J. Pharm. Sci. 81:1992;879-887.
3. 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.
4. Artursson P., Borchardt R.T. Intestinal drug absorption and metabolism in cell cultures: caco-2 and beyond. Pharm. Res. 14:1997;1655-1658.
5. Aspden T.J., Illum L., Skaugrud Ø. Chitosan as a nasal delivery system: evaluation of insulin absorption enhancement and effect on nasal membrane integrity using the rat models. Eur. J. Pharm. Sci. 4:1996;23-31.
6. Aspden T.J., Mason J.D.T., Jones N.S., Lowe J., Skaugrud Ø., Illum L. Chitosan as a nasal delivery system: the effect of chitosan solutions on in vitro and in vivo mucociliary transport rates in human turbinates and volunteers. J. Pharm. Sci. 86:1997;509-513.
7. Aspden T., Illum L., Skaugrud Ø. The effect of chronic nasal application of chitosan solutions on cilia beat frequency in guinea pigs. Int. J. Pharm. 153:1997;137-146.
8. Carreño-Gómez B., Duncan R. Evaluation of the biological properties of soluble chitosan and chitosan microspheres. Int. J. Pharm. 148:1997;231-240.
9. Chandy T., Sharma C.P. Chitosan as a biomaterial. Biomat. Art. Cells Art. Org. 18:1990;1-24.
10. Hariharan D., Peppas N.A. Characterization, dynamic swelling behavior and solute transport in cationic networks with applications to the development of swelling-controlled release systems. Polymer. 37:1996;149-161.
11. Haugland, R.P. 1996. Handbook of fluorescent probes and research chemicals, 6th edition, Molecular Probes, Eugene, OR, USA.
12. Hirano S., Seino H., Akiyama Y., Nonaka I. Biocompatibility of chitosan by oral and intravenous administration. Polym. Eng. Sci. 59:1988;897-901.
13. 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.
14. Illum L., Farray N.F., Davis S.S. Chitosan as a novel nasal delivery system for peptide drugs. Pharm. Res. 11:1994;1186-1189.
15. Kotzé A.F., Lueßen H.L., De Leeuw B.J., De Boer A.G., Verhoef J.C., 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. Kotzé A.F., Lueßen H.L., De Leeuw B.J., De Boer A.G., Verhoef J.C., Junginger H.E. Comparison of the effect of different chitosan salts and N-trimethyl chitosan chloride on the permeability of intestinal epithelial cells (Caco-2). J. Control. Rel. 51:1998;35-46.
17. Kotzé A.F., Thanou M., Verhoef J.C., Junginger H.E. Chitosan and N-trimethyl chitosan chloride as absorption enhancers for nasal and rectal delivery of insulin. Proceed. Intern. Symp. Control. Rel. Bioact. Mater. 25:1998;479-480.
18. Kotzé A.F., Lueßen H.L., De Boer A.G., Verhoef J.C., Junginger H.E. Chitosan for enhanced intestinal permeability: prospects for derivatives soluble in neutral and basic environments. J. Pharm. Sci. 88:1999;253-257.
19. Lueßen H.L., De Leeuw B.J., Langemeijer M.W.E., De Boer A.G., Verhoef J.C., Junginger H.E. Mucoadhesive polymers in peroral peptide delivery. VI. Carbomer and chitosan improve the intestinal absorption of the peptide drug buserelin in vivo. Pharm. Res. 13:1996;1666-1670.
20. 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. Rel. 45:1997;15-23.
21. Madara J.L. Loosening of the tight junctions. J.Clin. Invest. 83:1989;1089-1094.
22. Marttin E., Schipper N.G.M., Verhoef J.C., Merkus F.W.H.M. Nasal mucociliary clearance as a factor in nasal drug delivery. Adv. Drug Deliv. Rev. 29:1998;13-38.
23. Merkus F.W.H.M., Schipper N.G.M., Hermens W.A.J.J., Romeijn S.G., Verhoef J.C. Absorption enhancers in nasal drug delivery: efficacy and safety. J. Control. Rel. 24:1993;201-208.
24. Nagelkerke J.F., De Bont H.J.G.M. Upgrading of a BioRad MRC-600 confocal laser scanning microscopy with a 543-nm and a 633-nm HeNe laser. J. Microsc. 184:1996;58-61.
25. Quinton P.M., Phillpot C.W. A role for anionic sites in epithelial architecture. Effect of cationic polymers on cell membrane structure. J. Cell Biol. 56:1973;787-796.
26. Romeijn, S.G., Verhoef, J.C., Marttin, E., Merkus, F.W.H.M. 1996. The effect of nasal formulations on ciliary beating in vitro. Int. J. Pharm. 135, 137-145.
27. Sieval A.B., Thanou M., Kotzé A.F., Verhoef J.C., Brussee J., Junginger H.E. Preparation and NMR-characterization of highly substituted N-trimethyl chitosan chloride. Carbohydr. Polym. 36:1998;157-165.
28. Thanou, M., Kotzé, A.F., Scharringhausen, T., Lueßen, H.L., De Boer, A.G., Verhoef, J. C., Junginger, H.E., 1999. Effect of degree of quaternization of N-trimethyl chitosan chloride for enhanced transport of hydrophilic compounds across intestinal Caco-2 cell monolayers. J. Control. Rel. (in press).