Chitosans for enhanced delivery of therapeutic peptides across intestinal epithelia: In vitro evaluation in Caco-2 cell monolayers

International Journal of Pharmaceutics

Volumn 159, Issue 2, 1997, Pages 243-253

  Kotze A F ^a,b   De Leeuw, B J ^b   Luessen H L ^b,c   De Boer, A G ^b   Verhoef, J C ^b   Junginger, H E ^b  

^a NORTH WEST UNIVERSITY   (South Africa)

^b LEIDEN UNIVERSITY   (Netherlands)

^c LTS Lohmann Therapie Systeme AG   (Germany)

Author keywords

Absorption enhancers; Caco 2 cells; Chitosan; N trimethyl chitosan chloride; Paracellular transport; Peptide transport; Transepithelial electrical resistance

Indexed keywords

ARGIPRESSIN[DEGLYCINAMIDE]; BUSERELIN; CARBOMER; CHITOSAN DERIVATIVE; CHYMOTRYPSIN A; CORBOPOL; INSULIN; N TRIMETHYLCHITOSAN CHLORIDE; PROTEINASE; SEACURE CL 210; SEACURE G 210; UNCLASSIFIED DRUG;

ARTICLE; CELL STRAIN CACO 2; DRUG ABSORPTION; DRUG CONFORMATION; DRUG DEGRADATION; DRUG DELIVERY SYSTEM; DRUG FORMULATION; DRUG PROTEIN BINDING; DRUG SOLUBILITY; DRUG UPTAKE; ENZYME INHIBITION; HUMAN; HUMAN CELL; INTESTINE EPITHELIUM; PRIORITY JOURNAL;

EID: 0031574261     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0378-5173(97)00287-1     Document Type: Article

References (28)

1. Akiyama Y., Lueßen H.L., De Boer A.G., Verhoef J.C., Junginger H.E. Design of fast dissolving poly(acrylate) and controlled drug-releasing capsule formulations with trypsin inhibiting properties. Int. J. Pharm. 138:1996;13-23.
2. Arai K., Kinumaki T., Fujita T. Toxicity of chitosan. Bull. Tokai Reg. Fish Lab. 43:1968;89-94.
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. 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.
5. Cereijido, M., Ruiz, O., Gonzalez-Mariscal, L., Contreras, R.G., Balda, M.S., Garcia-Villegas, M.R., 1993. The paracellular pathway. In: Audas, K.L., Raub, T.J. (Eds.), Biological Barriers to Protein Delivery. Plenum Press, New York, pp. 3-21.
6. Domard A., Rinaudo M., Terrassin C. New method for the quaternization of chitosan. Int. J. Macromol. 8:1986;105-107.
7. Fix J.A. Absorption enhancing systems for the GI system. J. Control. Release. 6:1987;151-156.
8. Gumbiner B. Structure, biochemistry and essembly of epithelial tight junctions. Am. J. Physiol. 253:1987;749-758.
9. Hirano S., Seino H., Akiyama Y., Nonaka I. Biocompatibility of chitosan by oral and intravenous administration. Polym. Eng. Sci. 59:1988;897-901.
10. Hochman J., Artursson P. Mechanisms of absorption enhancement and tight junction regulation. J. Control. Release. 29:1994;253-267.
11. 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.
12. Illum L., Farraj N.F., Davis S.S. Chitosan as a novel nasal delivery system for peptide drugs. Pharm. Res. 11:1994;1186-1189.
13. Kotzé, A.F., Lueßen, H.L., De Leeuw, B.J., De Boer, A.G., Verhoef, J.C., Junginger, H.E., 1997a. N-trimethyl chitosan cloride as a potential absorption enhancers across mucosal surfaces: in vitro evaluation in intestinal epithelial cells (Caco-2). Pharm. Res. 14, 1197-1202.
14. Kotzé, A.F., Lueßen, H.L., De Leeuw, B.J., De Boer, A.G., Verhoef, J.C., Junginger, H.E., 1997b. Comparision of the effect of different chitosan salts and N-trimethyl chitosan chloride on the permeability of intestinal epithelial cells (Caco-2). J. Control. Release 14, 1197-1202.
15. Lee, V.H.L, 1991. Changing needs in drug delivery in the era of peptide and protein drugs. In: Lee, V.H.L (Ed.), Peptide and Protein Drug Delivery. Marcel Dekker, New York, pp. 1-56.
16. Li Q., Dunn E.T., Grandmaison E.W., Goosen M.F.A. Applications and properties of chitosan. J. Boiact. Compat. Polym. 7:1992;370-397.
17. 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.
18. Lueßen H.L., De Leeuw B.J., Pérard D., Lehr C.-M., De boer A.G., Verhoef J.C., Junginger H.E. Mucoadhesive polymers in peroral peptide drug delivery. I. Influence of mucoadhesive excipients on the proteolytic activity of intestinal enzymes. Eur. J. Pharm. Sci. 4:1996;117-128.
19. Lueßen H.L., Bohner V., Pérard D., Langguth P., Verhoef J.C., De Boer A.G., Merkle H.P., Junginger H.E. Mucoadhesive polymers in peroral peptide drug delivery. V. Effect of poly(acrylates) on the enzymatic degradation of peptide drugs by intestinal brush border membrane vesicles. Int. J. Pharm. 141:1996;39-52.
20. Lueßen H.L., Rental 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. Polycarbophyl and chitosan are potent enhancers of peptide transport across intestinal mucosae in vitro. J.Control. Release. 45:1997;15-23.
21. Madara J.L. Intestinal absorptive cell tight junctions are linked to cytoskeleton. Am. J. Physiol. 253:1987;C171-C175.
22. Madara J.L. Loosening tight junctions. Lessons from the intestine. J. Clin. Invest. 83:1989;1089-1094.
23. 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.
24. Muranishi S. Absorption enhancers. Crit. Rev. Ther. Drug Carrier Syst. 7:1990;1-27.
25. 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.
26. Skaugrud O. Chitosan makes the grade. Manuf. Chem. 60:1989;31-35.
27. 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.
28. Wilson, C.G., Washington, N., 1989. Physiological Pharmaceutics: Biological Barriers to Drug Absorption. Ellis Horwood, Chichester, pp. 1-186.