Zonula occludens toxin synthetic peptide derivative AT1002 enhances in vitro and in vivo intestinal absorption of low molecular weight heparin

Journal of Drug Targeting

Volumn 14, Issue 5, 2006, Pages 321-329

  Motlekar, Nusrat A ^a   Fasano, Alessio ^b   Wachtel, Mitchell S ^c   Youan, Bi Botti C ^a  

^a TEXAS TECH UNIVERSITY HEALTH SCIENCES CENTER   (United States)

^b UNIVERSITY OF MARYLAND SCHOOL OF MEDICINE   (United States)

^c TEXAS TECH UNIVERSITY HEALTH SCIENCES CENTER SCHOOL OF MEDICINE   (United States)

Author keywords

AT1002; Enhancer; Low molecular weight heparin; Oral delivery; Zonula occludens toxin

Indexed keywords

ARDEPARIN; AT 1002; BLOOD CLOTTING FACTOR 10A; ENTEROTOXIN; LOW MOLECULAR WEIGHT HEPARIN; PROTEIN ANTIBODY; SYNTHETIC PEPTIDE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; AREA UNDER THE CURVE; ARTICLE; CELL STRAIN CACO 2; CELL VIABILITY; CONTROLLED STUDY; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG PENETRATION; DRUG TRANSPORT; HUMAN; HUMAN CELL; IMMUNOASSAY; IN VITRO STUDY; IN VIVO STUDY; INTESTINE ABSORPTION; INTESTINE EPITHELIUM; INTESTINE MUCOSA; MALE; MONOLAYER CULTURE; NONHUMAN; PRIORITY JOURNAL; RAT;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; CACO-2 CELLS; CELL MEMBRANE PERMEABILITY; CHOLERA TOXIN; DRUG INTERACTIONS; GASTROINTESTINAL TRACT; HEPARIN, LOW-MOLECULAR-WEIGHT; HUMANS; INTESTINAL ABSORPTION; MALE; OLIGOPEPTIDES; RATS; RATS, SPRAGUE-DAWLEY;

EID: 33746790243     PISSN: 1061186X     EISSN: 10292330     Source Type: Journal    
DOI: 10.1080/10611860600613316     Document Type: Article

References (28)

1. Anderson, JM and Van Itallie, CM. (1995) Tight junctions and the molecular basis for regulation of paracellular permeability Am J Physiol, 269(4 Pt 1), pp. G467-G475.
2. Asada, H and Douen, T and Waki, M and Adachi, S and Fujita, T and Yamamoto, A and Muranishi, S. (1995) Absorption characteristics of chemically modified-insulin derivatives with various fatty acids in the small and large intestine J Pharm Sci, 84(6), pp. 682-687.
3. Aungst, BJ. (2000) Intestinal permeation enhancers J Pharm Sci, 89(4), pp. 429-442.
4. Bernkop-Schnurch, A and Schwarz, V and Steininger, S. (1999) Polymers with thiol groups: A new generation of mucoadhesive polymers? Pharm Res, 16(6), pp. 876-881.
5. Bianchini, P and Bergonzini, GL and Parma, B and Osima, B. (1995) Relationship between plasma antifactor Xa activity and the antithrombotic activity of heparins of different molecular mass Haemostasis, 25(6), pp. 288-298.
6. Clarke, H and Marano, CW and Peralta Soler, A and Mullin, JM. (2000) Modification of tight junction function by protein kinase C isoforms Adv Drug Deliv Rev, 41(3), pp. 283-301.
7. Cox, DS and Gao, H and Raje, S and Scott, KR and Eddington, ND. (2001) Enhancing the permeation of marker compounds and enaminone anticonvulsants across Caco-2 monolayers by modulating tight junctions using zonula occludens toxin Eur J Pharm Biopharm, 52(2), pp. 145-150.
8. Cox, DS and Raje, S and Gao, H and Salama, NN and Eddington, ND. (2002) Enhanced permeability of molecular weight markers and poorly bioavailable compounds across Caco-2 cell monolayers using the absorption enhancer, zonula occludens toxin Pharm Res, 19(11), pp. 1680-1688.
9. Di Pierro, M and Lu, R and Uzzau, SW and Wang, W and Margaretten, K and Pazzani, C and Maimone, F and Fasano, A. (2001) Zonula occludens toxin structure-function analysis. Identification of the fragment biologically active on tight junctions and of the zonulin receptor binding domain J Biol Chem, 276(22), pp. 19160-19165.
10. Dodane, V and Amin Khan, M and Merwin, JR. (1999) Effect of chitosan on epithelial permeability and structure Int J Pharm, 182(1), pp. 21-32.
11. Duizer, E and van der Wulp, C and Versantvoort, CH and Groten, JP. (1998) Absorption enhancement, structural changes in tight junctions and cytotoxicity caused by palmitoyl carnitine in Caco-2 and IEC-18 cells J Pharmacol Exp Ther, 287(1), pp. 395-402.
12. Fasano, A and Uzzau, S. (1997) Modulation of intestinal tight junctions by Zonula occludens toxin permits enteral administration of insulin and other macromolecules in an animal model J Clin Investig, 99(6), pp. 1158-1164.
13. Fasano, A and Baudry, B and Pumplin, DW and Wasserman, SS and Tall, BD and Ketley, JM and Kaper, JB. (1991) Vibrio cholerae produces a second enterotoxin, which affects intestinal tight junctions Proc Natl Acad Sci USA, 88(12), pp. 5242-5246.
14. Fasano, A and Fiorentini, C and Donelli, G and Uzzau, S and Kaper, JB and Margaretten, K and Ding, X and Guandalini, S and Comstock, L and Goldblum, SE. (1995) Zonula occludens toxin modulates tight junctions through protein kinase C-dependent actin reorganization, in vitro J Clin Investig, 96(2), pp. 710-720.
15. Fasano, A and Uzzau, S and Fiore, C and Margaretten, K. (1997) The enterotoxic effect of zonula occludens toxin on rabbit small intestine involves the paracellular pathway Gastroenterology, 112(3), pp. 839-846.
16. Fasano, A and Not, T and Wang, W and Uzzau, S and Berti, I and Tommasini, A and Goldblum, SE. (2000) Zonulin, a newly discovered modulator of intestinal permeability, and its expression in coeliac disease Lancet, 355(9214), pp. 1518-1519.
17. Hirsh, J and Warkentin, TE and Raschke, R and Granger, C and Ohman, EM and Dalen, JE. (1998) Heparin and low-molecular-weight heparin: Mechanisms of action, pharmacokinetics, dosing considerations, monitoring, efficacy, and safety Chest, 114(5), pp. 489S-510S.
18. Karyekar, CS and Fasano, A and Raje, S and Lu, R and Dowling, TC and Eddington, ND. (2003) Zonula occludens toxin increases the permeability of molecular weight markers and chemotherapeutic agents across the bovine brain microvessel endothelial cells J Pharm Sci, 92(2), pp. 414-423.
19. Lee, VH and Yamamoto, A and Kompella, UB. (1991) Mucosal penetration enhancers for facilitation of peptide and protein drug absorption Crit Rev Ther Drug Carrier Syst, 8(2), pp. 91-192.
20. Leone-Bay, A and Paton, DR and Variano, B and Leipold, H and Rivera, T and Miura-Fraboni, J and Baughman, RA and Santiago, N. (1998) Acylated non-alpha-amino acids as novel agents for the oral delivery of heparin sodium, USP J Control Release, 50(1-3), pp. 41-49.
21. Salama, NN and Fasano, A and Lu, R and Eddington, ND. (2003) Effect of the biologically active fragment of zonula occludens toxin, delta G, on the intestinal paracellular transport and oral absorption of mannitol Int J Pharm, 251(1-2), pp. 113-121.
22. Salama, NN and Fasano, A and Thakar, M and Eddington, ND. (2004) The effect of delta G on the transport and oral absorption of macromolecules J Pharm Sci, 93(5), pp. 1310-1319.
23. Sethia, S and Squillante, E. (2004) In vitro-in vivo evaluation of supercritical processed solid dispersions: Permeability and viability assessment in Caco-2 cells J Pharm Sci, 93(12), pp. 2985-2993.
24. Swenson, ES and Milisen, WB and Curatolo, W. (1994) Intestinal permeability enhancement: Efficacy, acute local toxicity, and reversibility Pharm Res, 11(8), pp. 1132-1142.
25. Teien, AN and Lie, M and Abildgaard, U. (1976) Assay of heparin in plasma using a chromogenic substrate for activated factor X Thromb Res, 8(3), pp. 413-416.
26. Thakar, M and Vogel, S and Kao, J and Fasano, A. (2005) The vibrio cholerae-generated zonula occludens toxin (zot) N-terminal cleavage site contains a protease-activated receptor activating peptide (par-Ap) that retains biological activity on intestinal tight junctions Gastroenterology, 128(2), pp. A541-T1742.
27. Thanou, M and Verhoef, JC and Nihot, MT and Verheijden, JH and Junginger, HE. (2001) Enhancement of the intestinal absorption of low molecular weight heparin (LMWH) in rats and pigs using Carbopol 934P Pharm Res, 18(11), pp. 1638-1641.
28. Uzzau, S and Lu, R and Wang, W and Fiore, C and Fasano, A. (2001) Purification and preliminary characterization of the zonula occludens toxin receptor from human (CaCo2) and murine (IEC6) intestinal cell lines FEMS Microbiol Lett, 194(1), pp. 1-5.