Study on preparation and release behavior of chitosan-fucoidan nanoparticles for oral drug delivery

學生姓名: 許馨勻
指導教授: 黃意真
學  號: 10432029
學期: 104上
摘  要: Fucoidan (FD) is a negatively charged polysaccharide. There have been various in-vivo and in-vitro studies on the anticarcinogenic effects of FD, which has been known to induce the apoptosis or to inhibit the angiogenic activity of some cancer cells. Chitosan (CS) have been reported that the surface charge affects cellular uptake and intracellular trafficking. Positively-charged nanoparticles (NPs) preferring to contact with negatively-charged cell surface with their electrostatic interaction. Therefore, a smaller-positively charged CS NP is believed optimized to promote the intestinal uptake greater. The aim of this study is to investigate on preparation and applications of CS-FD NPs by correlating characteristics and their charge density. The first study was preparation conditions for both a high yield without aggregation and a small mean-size of CS-FD NPs. The optimum conditions of pH 5 and 1 : 1 CS-FD mass ratio were suggested to prepare CS-FD NPs. Second, CS-FD hollow multilayer nanocapsules were successfully prepared through layer-by-layer assembly of CS and FD by correlating each other. CS/FD nanocapsules is a promising delivery system for water soluble bioactive compounds, showing a great potential of application in food and pharmaceutical industries. Third, an oversulfation reaction of fucoidan (OFD) has been performed to enhance its antiangiogenic activities. NPs composed of CS and OFD were prepared by a polycation–polyanion complex method. Evaluation of test NPs in enhancing the intestinal paracellular transport of OFD suggested that the NPs with a positive surface charge could transiently open the tight junctions between Caco-2 cells and thus increase the paracellular permeability. In conclusion, these findings of the work suggested that CS/OFD NPs may be a suitable carrier to transport OFD across the Caco-2 monolayer for the purpose of antiangiogenic therapy.