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Year: 2013


Type: Article



Title: Wheat germ agglutinin-functionalised crosslinked polyelectrolyte microparticles for local colon delivery of 5-FU: in vitro efficacy and in vivo gastrointestinal distribution


Author: Glavas-Dodov, Marija
Author: Steffansen, Bente
Author: Crcarevska, Maja S
Author: Geskovski, Nikola
Author: Dimchevska, Simona
Author: Sonja Kuzmanovska
Author: Goracinova, Katerina



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.


Publisher:


Relation: Journal of microencapsulation



Identifier: oai:repository.ukim.mk:20.500.12188/8398
Identifier: http://hdl.handle.net/20.500.12188/8398
Identifier: 10.3109/02652048.2013.770099
Identifier: 30
Identifier: 7



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Wheat germ agglutinin-functionalised crosslinked polyelectrolyte microparticles for local colon delivery of 5-FU: in vitro efficacy and in vivo gastrointestinal distribution201315