期刊
JOURNAL OF MICROENCAPSULATION
卷 30, 期 7, 页码 643-656出版社
TAYLOR & FRANCIS LTD
DOI: 10.3109/02652048.2013.770099
关键词
hydrogel microparticles; 5-fluorouracil; wheat germ agglutinin; Caco-2; gastrointestinal distribution
资金
- TEMPUS [CD_JEP-18016]
- Ministry of Education and Science
- TUBITAK, Turkey [17-364, NATO SfP: 978023]
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-H-3]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-H-3]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.
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