Influence of autoclave treatment and enzymatic hydrolysis on the antioxidant activity of Opuntia ficus-indica fruit extract.

The objectives of this study were to obtain Opuntia ficus-indica fruit (OFIF) extract by autoclave treatment, to convert the flavonoid glycosides in the autoclave extract (AE) to aglycones by enzymatic hydrolysis, and to compare the antioxidant activity of AE and OFIF extracts obtained by other conventional methods. It was revealed that the total polyphenol and flavonoid content and antioxidant activity of AE were higher than those of water extract but were a slightly lower than those of ethanol extract, which indicates that autoclave treatment might be an efficient extraction method for OFIF. Moreover, it was confirmed that the conversion of various flavonoid glycosides to aglycones in all the OFIF extracts does not significantly affect the antioxidant activities. Therefore, it is extrapolated that the antioxidant activity might be correlated to the intestinal absorption rates and metabolic pathway induction upon oral administration rather than the structure of compound itself.

Improving the encapsulation efficiency and sustained release behaviour of chitosan/ß-lactoglobulin double-coated microparticles by palmitic acid grafting.

Chitosan (CS) was grafted with 0.1 and 0.5% (w/v) palmitic acid (PA) to improve its encapsulation efficiency (EE) and sustained release characteristics when forming CS microparticles. Thereafter, PA-grafted CS (PA-CS) microparticles were coated with denatured ß-lactoglobulin (ßlg), which forms an outer protective layer. The possibility of hydrophobic interaction with the hydrophobic substances in the CS microparticles increased as the proportion of the grafted PA increased. EE was measured as 64.79, 83.72, and 85.00% for the non-grafted, 0.1, and 0.5% PA-CS microparticles, respectively. In simulated small intestinal conditions, 4.66 and 17.55% of the core material release in the PA-CS microparticles were sustained after 180min by 0.1, and 0.5% PA grafting, respectively. PA grafting enables the sustained release in simulated gastrointestinal fluids by enhancing the hydrophobic interaction between CS and the hydrophobic core material.

Synthesis and controlled-release properties of chitosan/ß-Lactoglobulin nanoparticles as carriers for oral administration of epigallocatechin gallate.

A nano-sized double-walled carrier composed of chitosan and ß-lactoglobulin (ß-Lg) for oral administration of epigallocatechin gallate (EGCG) was developed to achieve a prolonged release of EGCG in the gastrointestinal tract. Carboxymethyl chitosan (CMC) solution was added dropwise to chitosan hydrochloride (CHC) containing EGCG to form a primary coating by ionic complexation. Subsequently, ß-Lg was added to create a secondary layer by ionic gelation. The obtained EGCG-loaded chitosan/ß-Lg nanoparticles had sizes between 100 and 500 nm and zeta potentials ranging from 10 to 35mV. FT-IR spectroscopy revealed a high number of hydrogen-bonding sites in the nanoparticles, which could incorporate EGCG, resulting in high encapsulation efficiency. EGCG incorporated in the primary coating was released slowly over time by diffusion from the swollen CMC-CHC matrix after the outer layer of ß-Lg was degraded in the intestinal fluid. The sustained-release property makes chitosan/ß-Lg nanoparticles an attractive candidate for effective delivery of EGCG.

Fabrication of amorphous curcumin nanosuspensions using ß-lactoglobulin to enhance solubility, stability, and bioavailability.

Curcumin has low aqueous stability and solubility in its native form. It also has a low bioavailability which presents a major barrier to its use in fortifying food products. The aim of this work was to reduce the size of curcumin crystals to the nanoscale and subsequently stabilize them in an amorphous form. To this end, amorphous curcumin nanosuspensions were fabricated using the antisolvent precipitation method with ß-lactoglobulin (ß-lg) as a stabilizer. The resulting amorphous curcumin nanosuspensions were in the size range of 150-175 nm with unimodal size distribution. The curcumin particles were amorphous and were molecularly dispersed within the ß-lg as confirmed by differential scanning calorimetry (DSC) and X-ray diffraction (XRD) studies. The solubility of the amorphous curcumin nanosuspension was enhanced ∼35-fold due to the reduced size and lower crystallinity. Among the formulations, the amorphous curcumin nanosuspensions stabilized with ß-lg and prepared at pH 3.4 (ß-lg-cur 3.4), showed maximum aqueous stability which was >90% after 30 days. An in vitro study using Caco-2 cell lines showed a significant increase in curcumin bioavailability after stabilization with ß-lg.

Co-delivery of hydrophobic curcumin and hydrophilic catechin by a water-in-oil-in-water double emulsion.

Curcumin and catechin are naturally occurring phytochemicals with extreme sensitivity to oxidation and low bioavailability. We fabricated a water-in-oil-in-water (W/O/W) double emulsion encapsulating hydrophilic catechin and hydrophobic curcumin simultaneously. The co-loaded emulsion was fabricated using a two-step emulsification method, and its physicochemical properties were characterised. Volume-weighted mean size (d43) of emulsion droplets was ≈3.88 µm for blank emulsions, whereas it decreased to ≈2.8-3.0 µm for curcumin and/or catechin-loaded emulsions, which was attributed to their capacity to act as emulsifiers. High entrapment efficiency was observed for curcumin and/or catechin-loaded emulsions (88-97%). Encapsulation of catechin and curcumin within an emulsion increased their stability significantly in simulated gastrointestinal fluid, which resulted in a four-fold augmentation in their bioaccessibility compared to that of freely suspended curcumin and catechin solutions. Co-loading of curcumin and catechin did not have adverse effects on either compound's stability or bioaccessibility.