Overcoming paracellular tissue barriers for drug delivery

Pharmaceutical News

Volumn 9, Issue 6, 2002, Pages 381-395

  Paranjpe, Pankaj V ^a   Sinko, Patrick J ^a  

^a RUTGERS UNIVERSITY   (United States)

Author keywords

Absorption; Drug delivery; Oral; Paracellular permeability; Tight junction

Indexed keywords

ACICLOVIR; ACYLCARNITINE; AMOXICILLIN; CARNITINE; CEFMETAZOLE; CHITOSAN; CORTICOSTEROID DERIVATIVE; DODECYL SULFATE SODIUM; GANCICLOVIR; HYDROCORTISONE; IMMUNOGLOBULIN G; INSULIN; MANNITOL; NONSTEROID ANTIINFLAMMATORY AGENT; PREDNISOLONE; SALCATONIN; SALICYLIC ACID; SURFACTANT; TAUROCHOLIC ACID; VALACICLOVIR;

BLOOD BRAIN BARRIER; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG DELIVERY SYSTEM; DRUG EFFICACY; DRUG FORMULATION; DRUG INDUSTRY; DRUG MECHANISM; DRUG PENETRATION; DRUG SAFETY; DRUG TRANSPORT; ENDOCYTOSIS; INTESTINE ABSORPTION; LIPOPHILICITY; MEDICAL LITERATURE; MEMBRANE; MOLECULAR BIOLOGY; NONHUMAN; PINOCYTOSIS; REVIEW; SMALL INTESTINE;

EID: 0042694405     PISSN: 1071894X     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (61)

1. Langer, R. (1998). Drug delivery and targeting. Nature 392(6679suppl), 5-10.
2. Van Hoogdalem, E.J., DeBoer, A.G., Breimer, D.D. (1989). Intestinal drug absorption enhancement: An overview. Pharmac. Ther. 44, 407-443.
3. Fasano, A. (1998). Novel Approaches for oral delivery of macromolecules. J. Pharm. Sci. 87, 1351-1356.
4. Pardridge, W.J. (2002). Drug and gene targeting to the brain with molecular Trojan horses. Nature Reviews Drug Discovery 1, 131-139
5. Miller, G. (2002). Breaking down barriers. Science 297, 1116-18.
6. Daugherty. A.L. and Mrsny, R.J. (1999). Transcellular uptake mechanisms of the intestinal epithelial barrier. Part one. Pharmaceutical. Science and Technology Today 2, 144-151.
7. Shah, D., Shen, W.C. (1996). Transcellular delivery of an insulin-transferrin conjugate in enterocyte-like Caco-2 cells. J Pharm Sci. 85, 1306-11.
8. Wu, D., Yang, J., Pardridge, WM. (1997). Drug targeting of a peptide radiopharmaceutical through the primate blood-brain barrier in vivo with a monoclonal antibody to the human insulin receptor. J Clin Invest. 100, 1804-12.
9. Lutz, K.L., Siahaan, T.J. (1997). Molecular structure of the apical junction complex and its contribution to the paracellular barrier. J. Pharm. Sci. 86, 977-984.
10. Smyth, R.D., Pfeffer, M., Van Harken, D.R., Cohen, A., Holtendorf, G.H. (1981). Human pharmacokinetics and disposition of sarmoxicillin, a lipophillic amoxicillin prodrug. Antimicrob. Agents. Chemother. 19, 1004-1012.
11. Fleisher, D., Johnson, K.C., Stewart, B.H., Amidon, G.L. (1986). Oral absorption of 21-corticosteroid esters: a function of aqueous stability and intestinal enzyme activity and distribution. J Pharm Sci. 75, 934-9.
12. Weller, S., Blum, M.R., Doucelte, M., Burnette, T., Cederberg, D.M., deMirinda, P., Smiley, M.L. (1993). Pharmacokinetics of the acylovir prodrug, valacyclovir after escalating single and multiple-dose administration to normal volunteer. Clin. Pharmacol. Ther. 54, 595-605.
13. Sugawara, M., Huang, W., Fei, Y.J., Leibach, F.H., Ganapathy, V., Ganapathy, M.E. (2000). Transport of valganciclovir, a ganciclovir prodrug, via peptide transporters PEPT1 and PEPT2. J Pharm Sci. 89, 781-9.
14. Hochman, J. and Artursson, P. (1994). Mechanisms of absorption enhancement and tight junction regulation. J. Cont. Rel. 29, 253-267.
15. Madara, J.L. (2000). Modulation of tight junctional permeability. Adv. Drug Del. Rev. 41, 251-253.
16. Farquhar, M.G. and Palade, G.E. (1963). Junctional complexes in various epithelia. J. Cell. Biol. 17, 375-412.
17. Staehlin, L.A. (1974). Structure and function of intercellular junctions. Int. Rev. Cytol. 39, 191-283.
18. Diamond, J.M. (1977). The epithelial junction: Bridge, gate and fence. Physiologist 20, 10-18.
19. Stevenson, B.R. (1999). Understanding tight junction clinical physiology at the molecular level. J. Clin. Invest. 104, 3-4.
20. Lapierre, L.A. (2000). The molecular structure of the tight junction. Adv. Drug Del. Rev. 41, 255-264.
21. Tsukita, S and Furuse, M. (1999). Occludin and claudins in tight junction strands: leading or supporting players? Trends Cell Biol. 9, 268-273.
22. Barry, B.W. Dermatological formulations, percutaneous absorption (Barry, B.W. ed) 127-233, Marcel Dekker.
23. Rege, B.D., Yu, L.X., Hussain, A.S., Polli, J.E. (2001). Effect of common excipients on caco-2 transport of low-permeability drugs. J. Pharm. Sci. 90, 1776-1786.
24. Drewe, J., Fricker, G., Vonderscher, J., Beglinger, C. (1993). Enteral absorption of octreotide: absorption enhancement by polyoxyethylene-24-cholesterol ether. Br. J. Pharmacol. 108, 298-303.
25. Fix, J.A., Engle, K., Porter, P.A., Leppert, P.S., Selk, J.J., Gardner, C.R., Alexander, J. (1986). Acylcarnitines: drug absorption-enhancing agents in the gastrointestinal tract. Am. J. Physiol. 251, G332-G340.
26. Fix, J.A. (1987). Absorption enhancing agents for the GI system. J. Cont. Rel. 6, 151-156.
27. Sinko, P.J., Lee, Yong-Hee, Makhey, V., et al. (1999). Biopharmaceutical approaches for developing and assessing oral peptide delivery strategies and systems: In vitro permeability and in vivo oral absorption of salmon calcitonin (sCT). Pharm. Res. 16, 527-533.
28. Liu, D.Z., Lecluyse, E.L., Thakker, D.R. (1999). Dodecylphosphocholine-mediated enhancement of paracellular permeability and cytotoxicity in Caco-2 cell monolayers. J. Pharm. Sci. 88, 1161-1168.
29. Lindmark, T., Kimura, Y., Artursson, P. (1998). Absorption enhancment through intracellular regulation of tight junction permeability by medium chain fatty acids in Caco-2 cells. J. Pharm. Exp. Ther. 284, 362-369.
30. Muranishi, S. (1990). Absorption enhancers. Crit. Rev. Ther. Drug. Carrier. Sys. 7, 1-33.
31. Meaney, C.M., O'Driscoll, C.M. (2000). A comparison of the permeation enhancement potential of simple bile salt and mixed bile salt:fatty acid miceller systems using Caco-2 cell culture model. Int. J. Pharm. 207, 21-30.
32. Illum, L., Farraj, N.F. Davis, S.S. (1994). Chitosan as a novel nasal delivery system for peptide drugs. Pharm. Res. 11, 1186-1189.
33. Ranaldi, G., Mariguano, I., Vespignani, I., Perozz, G., Sambuy, Y. (2002). The effet of chitosan and other polycations on tight junction permeability in the human intestinal Caco-2 cell line. J. Nutr. Biochem. 13, 157-167.
34. Thanou, M., Verhoef, J.C., Junginger, H.E. (2001). Oral drug absorption enhancement by chitosan and its derivatives. Adv. Drug. Del. Rev. 52, 117-126.
35. Cereijido, M. and Anderson, J. (2001). Tight junctions, 2nd ed. CRC press.
36. Fasano, A., Baudry, B., Pumplin, O.W., et al. (1991). Vibrio cholerae produces a second enterotoxin, which affects intestinal tight junctions. Proc. Natl. Sci. Acad. 88, 5242-5246.
37. Fasano, A., 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. Invest. 99, 1158-1164.
38. Ojakian, G.K. (1981). Tumor promotor-induced changes in the permeability of epithelial cell tight junctions. Cell. 23, 95-103.
39. Hazen-Martin, D.J., Sens, M.A., Detrisac, C.J., Blackburn, J.G., Sens, D.A. (1989). Elevated glucose alters paracellular transport of cultured human proximal tubule cells. Kidney. Intl. 35, 31-39.
40. McRoberts, J.A., Aranda, R., Riley, N., Kang, H. (1990) Insulin regulates the paracellular permeability of cultured intestinal epithelial cell monolayers. J. Clin. Invest. 85, 1127-1134.
41. Yamamoto, A., Tatsumi, H., Maruyama, M., Uchiyama, T., Okada, N., Fujita, T. (2001). Modulation of intestinal permeability by nitric oxide donors: implications in intestinal delivery of poorly absorbable drugs. J. Pharmcol. Exp. Ther. 296, 84-90.
42. Bjork, E., Isaksson, U., Edman, P., Artursson, P. (1995). Starch microspheres induce pulsatile delivery of drugs and peptides across the epithelial barrier by reversible separation of tight junctions. J. Drug. Targeting. 2, 501-507.
43. Wan, H., Winton, H.L., Soeller, C., Tovey, E.R., Gruenert, D.C., Thompson, P.J., et al. (1999). Der p 1 facilitates transepithelial allergen delivery by disruption of tight junctions. J. Clin. Invest. 104, 123-133.
44. Collares-Buzato, C.B., Jepson, M.A., Simmons, N.L., Hirst, B.H. (1998). Increased tyrosin phosphorylation causes redistribution of adherens junction and tight junction proteins and perturbs paracellular barrier function in MDCK epithelia. Eur. J. Cell. Biol. 76, 85-92.
45. Morgado-Diaz, J.A., desouza, W. (2001). Evidence that increased tyrosine phosphorylation causes disassembly of adherens junctions but does not perturb paracellular permeability in Caco-2 cells. Tissue. Cell. 33, 500-513.
46. Salzman, A.L., Menconi, M.J., Unno, N., Ezzell, R.M., Casey, D.M., et al. (1995). Nitric oxide dilates tight junctions and depletes ATP in cultured Caco-2 Bbe intestinal epithelial monolayers. Am. J. Physiol. 268, G361-G373.
47. Utoguchi, N., Watanabe, Y., Shida, T., Matsumoto, M. (1998). Nitric oxide donors enhance rectal absorption of macromolecules in rabbits. Pharm. Res. 15, 870-876.
48. Ward, P.D., Tippin, T.K., Thakker, D.R. (2000). Enhancing paracellular permeability by modulating epithelial tight junctions. Pharm. Sci. Tech. Today. 3, 346-358.
49. Daugherty, A.L., Mrsny, R.J. (1999). Regulation of the intestinal epithelial paracellular barrier. Pharm. Sci. Tech. Today. 2, 281-287.
50. Liu, F., Soares, M.J., Audus, K.L. (1997). Permeability properties of monolayers of the human trophoblast cell line BeWo. Am J Physiol 273, C1596-604.
51. Marrero, J.A., Ostrovskiy, D.A., Matkowskyj, K.A., Koutsouris, S., Hecht, G., Benya, R.V. (1998). Electrophysiological characterization of human distal colon epithelium isolated using a novel technique. Dig Dis Sci 43, 2439-459.
52. Pezron, I., Mitra, R., Pal, D., Mitra, A.K. (2002). Insulin aggregation and asymmetric transport across human bronchial epithelial cell monolayers (Calu-3). J Pharm Sci. 91, 1135-46.
53. Prytz, H., Benoni, C., Tagesson, C. (1989). Does smoking tighten the gut? Scand. J. Gastroenterol. 24, 1084-8.
54. Duizer, E., Gilde, AJ., Versntvoort, CH., Groten, JP. (1999). Effects of cadmium chloride on the paracellular barrier function of intestinal epithelial cell lines. Toxicol. Appl. Pharmacol. 155, 117-26.
55. Elliott, P.J., Hayward, N.J., Dean, R.L., Blunt, D.G., Bartus, R.T. (1996). Intravenous RMP-7 selectively increases uptake of carboplatin into rat brain tumors. Cancer Res. 56, 3998-4005.
56. Elliot, P.J., Bartus, R.T., Mackic, J.B., Zlokovic, B.V. (1997). Intravenous infusion of RMP-7 increases ocular uptake of ganciclovir. Pharm Res. 14, 80-5.
57. Emerich, D.F., Dean, R.L., Osborn, C., Bartus, R.T. (2001). The development of the bradykinin agonist labradimil as a means to increase the permeability of the blood-brain barrier: from concept to clinical evaluation. Clin Pharmacokinet. 40, 105-23.
58. US Patent No. 6346613. Composition and method for enhancing paracellular transport across cell layers.
59. Swenson, E.S., Milisen, W.B., Curatolo, W. (1994). Intestinal permeability enhancement: Efficacy, Acute local toxicity, and Revesibility. Pharm. Res. 11, 1132-1142.
60. Ritschel, W.A. and Kearns, G.L. (1999). Cell Membranes, 27-36, in Handbook of Basic Pharmacokinetics including Clinical Applications. American Pharmaceutical Association.
61. Li, A.P. (2001). Screening of human ADME/Tox drug properties in drug discovery. Drug Discovery Today 6, 357-366.