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.
Access this chapter
Tax calculation will be finalised at checkout
Purchases are for personal use only
Preview
Unable to display preview. Download preview PDF.
References
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).
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).
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).
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).
Lehr, C.-M,. A. Pustzai. “The potential of bioadhesive lectins for the delivery of
peptide and protein drugs to the gastrointestinal tract.“ In Lectins:Biomedicalperspectives,A.Pusztai, S.Bardocz, ed. London and Bristol: Taylor and Francis, 1995.
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).
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).
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).
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).
H. Chen, V. Torchilin and R. Langer. Polymerized liposomes as potential oral vaccine carriers: stability and bioavailability. J. Cont. Rel. 42: 263–272 (1996).
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).
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).
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).
E.C. Lavelle. Targeted delivery of drugs to the gastrointestinal tract. Crit. Rev. Ther. Drug Car. Syst. 18: 341–386 (2001).
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).
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).
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).
A. Bernkop-Schnürch, V. Schwarz and S. Steininger. Polymers with thiol groups: a new generation of mucoadhesive polymers? Pharm. Res. 16: 876–881 (1999).
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).
Author information
Authors and Affiliations
Editor information
Editors and Affiliations
Rights and permissions
Copyright information
© 2002 Springer Science+Business Media New York
About this chapter
Cite this chapter
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
Download citation
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