151. Wheat germ agglutinin-functionalised crosslinked polyelectrolyte microparticles for local colon delivery of 5-FU:in vitroefficacy andin vivogastrointestinal distribution
- Author
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Maja Simonoska Crcarevska, Bente Steffansen, Katerina Goracinova, Simona Dimchevska, Marija Glavas-Dodov, Sonja Kuzmanovska, and Nikola Geskovski
- Subjects
Male ,Antimetabolites, Antineoplastic ,Materials science ,Alginates ,Colon ,Wheat Germ Agglutinins ,Cell ,Pharmaceutical Science ,Bioengineering ,chemistry.chemical_compound ,Colloid and Surface Chemistry ,Glucuronic Acid ,In vivo ,medicine ,Animals ,Humans ,Distribution (pharmacology) ,Rats, Wistar ,Physical and Theoretical Chemistry ,Triticum ,Chitosan ,Drug Carriers ,Hexuronic Acids ,Organic Chemistry ,Molecular biology ,Wheat germ agglutinin ,In vitro ,Rats ,medicine.anatomical_structure ,Biochemistry ,chemistry ,Caco-2 ,Colonic Neoplasms ,Fluorouracil ,Caco-2 Cells ,Thymidine ,Conjugate - Abstract
We have previously reported the development and characterisation of wheat germ agglutinin (WGA)-functionalised chitosan-Ca-alginate (CTS-Ca-ALG) microparticles (MPs) loaded with acid-resistant particles of 5-fluorouracil (5-FU). In the present work, our goal was to evaluate the potential of these carriers for efficient treatment of colon cancer by studying in vitro permeability and cell association of 5-FU and [methyl-³H]thymidine uptake in Caco-2 cells, as well as in vivo gastrointestinal distribution. The amount of 5-FU permeated through Caco-2 cells was 15.1, 7.7 and 6.5% for 5-FU solution, CTS-Ca-ALG MPs and WGA conjugates. The concentration of 5-FU associated with Caco-2 cells was significantly greater when delivered from MPs. By incorporation of 5-FU into MPs and further decoration with WGA, an increased [methyl-³H]thymidine uptake was observed few hours after continuous drug treatment followed by significantly reduced uptake after 6 h. Gastrointestinal distribution was in favour of increased localisation and concentration of the particles in colon region.
- Published
- 2013