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Ligand-Mediated Gastrointestinal Targeting

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Biomedical Aspects of Drug Targeting
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Abstract

This chapter will describe the rationale for drug targeting to the gastrointestinal (GI) tract, why it is important, and what the objectives of such targeting are. The approaches used to achieve these targeting objectives using ligands will be considered and discussed in detail. It it is important to consider some of the pharmaceutical issues involved, such as the type of vehicles to which ligands can be usefully attached. It should be stressed that at the current time, much of the work in this area is theoretical and experimental, with studies in cell culture systems or animals, and has yet to be transferred to man, let alone into pharmaceutical products on the market. In many cases, costs and regulatory considerations may make it prohibitive for the pharmaceutical industry to adopt some of the most interesting ideas emanating from the research laboratories.

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References

  1. J. Pappo, T.H. Ermak and H.J. Steger. Monoclonal antibody-directed targeting of fluorescent polystyrene microspheres to Peyer’s patch M cells. Immunology 73: 277–280 (1991).

    Google Scholar 

  2. J.F. Woodley and B. Naisbett. The potential of lectins for delaying the intestinal transit of drugs. Proc. Int. Symp. Contr. Rel. Bioact. Mater. 15: 125–126 (1988).

    Google Scholar 

  3. B. Naisbett and J. Woodley. The potential use of tomato lectin for oral drug delivery. 3. Bioadhesion in vivo. Int. J. Pharm. 114: 227–236 (1995).

    Article  Google Scholar 

  4. M.J. Montisci, A. Dembri, G. Giovannuci, H. Chacun, D. Duchene and G. Ponchel. Gastrointestinal transit and mucoadhesion of colloidal suspensions of Lycopersicon esculentum L. and Lotus tetragonolobus lectin-PLA microsphere conjugates in rats. Pharm. Res. 18: 829–837 (2001).

    Article  Google Scholar 

  5. Lehr, C.-M,. A. Pustzai. “The potential of bioadhesive lectins for the delivery of

    Google Scholar 

  6. peptide and protein drugs to the gastrointestinal tract.“ In Lectins:Biomedicalperspectives,A.Pusztai, S.Bardocz, ed. London and Bristol: Taylor and Francis, 1995.

    Google Scholar 

  7. C.-M. Lehr, F.G.J. Poelma, H.E. Junginger and J.J. Tukker. An estimate of turnover time of intestinal mucus gel layer in the rat in situ loop. Int. J. Pharm. 70: 235–240 (1991).

    Article  Google Scholar 

  8. N. Hussain, P.U. Jani and A.T. Florence. Enhanced oral uptake of tomato lectin- conjugated nanoparticles in the rat. Pharm. Res. 14: 613–618 (1997).

    Article  Google Scholar 

  9. N. Foster, M.A. Clark, M.A. Jepson and B.H. Hirst. Ulex europaeus 1 lectin targets microspheres to mouse Peyer’s patch M- cells in vivo. Vaccine 16: 536–541 (1998).

    Article  Google Scholar 

  10. M.A. Clark, B.H. Hirst and M.A. Jepson. Lectin-mediated mucosal delivery of drugs and microparticles. Adv. Drug Deliv. Rev. 43: 207–223 (2000).

    Article  Google Scholar 

  11. H. Chen, V. Torchilin and R. Langer. Polymerized liposomes as potential oral vaccine carriers: stability and bioavailability. J. Cont. Rel. 42: 263–272 (1996).

    Article  Google Scholar 

  12. S. Wrôblewski, P. Kopéckova, B. Rihovâ and J. Kope6ek. Lectin-HPMA copolymer conjugates-drug carriers for gastrointestinal tract targeting. Proc. Int. Symp. Contr. Rel. Bioact. Mater. 25: 768–769 (1998).

    Google Scholar 

  13. M. Wirth, A. Fuchs, M. Wolf, B. Ertl and F. Gabor. Lectin-mediated drug targeting: preparation, binding characteristics, and antiproliferative activity of wheat germ agglutinin conjugated doxorubicin on Caco-2 cells. Pharm. Res. 15: 1031–1037 (1998).

    Article  Google Scholar 

  14. S. Wroblewski, M. Berenson, P. Kopeckova and J. Kopecek. Potential of lectin-N-(2- hydroxypropyl)methacrylamide copolymer-drug conjugates for the treatment of pre-cancerous conditions. J. Cont. Rel. 74: 283–293 (2001).

    Article  Google Scholar 

  15. E.C. Lavelle. Targeted delivery of drugs to the gastrointestinal tract. Crit. Rev. Ther. Drug Car. Syst. 18: 341–386 (2001).

    Google Scholar 

  16. N. Hussain and A.T. Florence. Utilizing bacterial mechanisms of epithelial cell entry: invasin-induced oral uptake of latex nanoparticles. Pharm. Res. 15: 153–156 (1998).

    Article  Google Scholar 

  17. D. Ayelet, P. Kopeckovâ, T. Minko, A. Rubinstein and J. Kope6ek. The involvement of endogenous lectins in mediating the antitumor activity of targetable HPMA copolymer-doxorubicin conjugates in human colon adenocarcinoma and hepatoma cells. Pharm. Res. In press: (2002).

    Google Scholar 

  18. J. Alsenz, G.J. Russell-Jones, S. Westwood, B. Levet-Trafit and P.C. de Smidt. Oral absorption of peptides through the cobalamin (vitamin B 12) pathway in the rat intestine. J. Cont. Rel. 17: 825–832 (2000).

    Google Scholar 

  19. A. Bernkop-Schnürch, V. Schwarz and S. Steininger. Polymers with thiol groups: a new generation of mucoadhesive polymers? Pharm. Res. 16: 876–881 (1999).

    Article  Google Scholar 

  20. M.K. Marschütz, P. Caliceti and A. Bernkop-Schnürch. Design and in vitro evaluation of an oral delivery system for insulin. Pharm. Res. 17: 1468–1474 (2000).

    Article  Google Scholar 

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© 2002 Springer Science+Business Media New York

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Woodley, J. (2002). Ligand-Mediated Gastrointestinal Targeting. In: Muzykantov, V., Torchilin, V. (eds) Biomedical Aspects of Drug Targeting. Springer, Boston, MA. https://doi.org/10.1007/978-1-4757-4627-3_22

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  • DOI: https://doi.org/10.1007/978-1-4757-4627-3_22

  • Publisher Name: Springer, Boston, MA

  • Print ISBN: 978-1-4419-5312-4

  • Online ISBN: 978-1-4757-4627-3

  • eBook Packages: Springer Book Archive

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