Development and evaluation of a novel nanofibersolosome for enhancing the stability, in vitro bioaccessibility, and colonic delivery of cyanidin-3-O-glucoside.

ABSTRACT

The development of colon-specific carrier systems using polysaccharides for oral delivery of nutraceuticals is of great importance for the treatment and/or prevention of inflammatory bowel diseases. In this study, self-assembly with the assistance of vortexing and pulsed-ultrasonication was employed to develop a Fibersol®-2 (a digestion-resistant polysaccharide) and lipoid S75 based novel nanocarrier (denoted as nanofibersolosome) for the colonic delivery of cyanidin-3-O-glucoside (C3G). A series of nanofibersolosome formulations (CFS-0.5-4, 0.5-4 represent the ratios of Fibersol®-2lipoid S75) were developed and their performance was compared with Fibersol®-2-free reference lipid formulation (CFS-0). The nanofibersolosomes (<150 nm) were spherical and unilamellar with high negative surface charge (-38 to -51 mV) and good encapsulation efficiency (EE > 90%). They performed much better than CFS-0 in retaining their physical properties during freeze drying, preventing particle aggregation, and retaining C3G during storage (4 and 25 ℃) and thermal treatments (40, 60, and 80 ℃). They also exhibited significantly higher stability during simulated gastrointestinal digestion than CFS-0. These desirable features of the nanofibersolosomes (especially CFS-0.5 and CFS-1) led to the efficient delivery of higher concentrations of C3G to the colon than CFS-0. Moreover, gastrointestinal-digested and colonic-fermented nanofibersolosome samples exhibited significantly higher DPPH radical scavenging activity and stronger promoting effect on short-chain fatty acid generation than CFS-0. These in vitro findings indicate that the novel nanofibersolosome possesses great potential for the colonic delivery of C3G and likely other hydrophilic labile phytochemicals that merits further evaluation in in vivo models.