Sinigrin (SNG) and curcumin(CCM) have been known to provide a range of health benefits, such as anti-cancer, anti-inflammatory, and antioxidant activities. However, the use of these compounds is limited due to their poor stability and bioavailability. For instance, SNG is prone to decomposition in acidic gastric environment before reaching to the lower part of intestine where SNG could be absorbed and exerts its biological functions. On the other hand, CCM is reported to be poorly absorbed in the gastrointestinal tract due to its low solubility. Therefore, an effective carrier system that can deliver SNG and CCM to the target site without losing its activity is needed. In this study, we prepared hollow silica particles (HSP) sized to around 100nm, of which its surface was coated with amylose (AM@HSP) for oral delivery of SNG and CCM. The hollow structure of HSP provided a huge reservoir that could encapsulate large amounts of active ingredients. The amylose coating on the surface of HSP was found to control the release rate of encapsulated SNG and CCM as well as turning the surface of HSP biocompatible. The bioavailability of encapsulated compounds could be enhanced by incorporating chitosan to the surface of AM@HSP, which increases the retention time of the carrier in the lower part of the intestine. The physicochemical characteristics of AM@HSP were analyzed with dynamic light scattering (DLS), transmission electron microscopy (TEM), scanning electron microscopy (SEM), fourier transform infrared spectroscopy(FTIR) and X-ray diffraction(XRD). The encapsulation efficiency of SNG and CCM were 74.0% and 33.3%, respectively, whereas, total drug loading capacity was 22.0%. Furthermore, the released profile indicates that 80% of SNG and CCM were released over 10h in simulated intestinal fluid(SIF), whereas the release of SNG and CCM in simulated gastric fluid (SGF) was negligible. The stability of encapsulated SNG and CCM against environmental stresses, such as photo-degradation and chemical oxidation, was significantly enhanced upon encapsulation in AM@HSP. These results suggest that the starch based carrier system proposed in this study would be effective in delivering bioactive compounds that are vulnerable to highly acidic environment to the lower part of gastrointestinal tract.

Amylose coated hollow silica particle for oral delivery of antioxidants to the lower part of gastrointestinal tract

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