Abstract
Background: Almond skins are rich in bioactive compounds that undergo oxidation/degradation phenomena and are poorly soluble in water, reducing in vivo absorption and bioavailability, factors that influence the pharmacological activity of an active product. We developed a dried acetonic almond skins extract/cyclodextrin complex to improve extract solubility, dissolution rate and biological activity. Methods: A lyophilized acetonic almond skin extract was produced. To optimize complex formulation, phase solubility studies and complex characterization (absorption studies, differential scanning calorimetry (DSC), morphology, solubility studies) were performed. To evaluate a possible use in healthy products, tumor necrosis factor-α levels and reactive oxygen species release, as well as cicloxygenase-2 and inducible nitric oxide synthase expression in intestinal epithelial cells, were also evaluated. Results: Phase solubility studies showed a Bs-type profile. A 1:1 dried acetonic almond skins extract/cyclodextrin ratio was able to improve extract water solubility and dissolution rate (100% in 45 min). The UV-Vis spectra of complex revealed a hypsochromic and hyperchromic effect, probably due to a partial inclusion of extract in cyclodextrin cavity through weak bonds, confirmed by DSC and morphology studies. The technological improvement in the extract characteristics also led to better biological activity. In fact, the complex effectively reduces tumor necrosis factor-α levels with respect to the pure extract and significantly inhibits the reactive oxygen species release, even if only at the lower concentration of 5 μg/mL. Conclusion: The complex was able to overcome solubility problems and could be used in inflammatory disease.
Highlights
The waste and processing by-products of the agri-food industry have recently become a subject of great interest in scientific research
The trend is to encourage the recycling of by-products to minimize wastes and their disposal costs, employing sophisticate technologies to exploit the bioactive substances of which they are rich in order to produce nutraceutical products with high added value
Considering that polyphenols are able to act on inflammation processes through several mechanisms related to their antioxidative and radical scavenger properties [17], we evaluated the radical scavenging activity and the pharmacological potential of these products in an in vitro model of intestinal inflammation, in intestinal epithelial cells (IEC-6)
Summary
The waste and processing by-products of the agri-food industry have recently become a subject of great interest in scientific research. Despite this information on the nutritional and healthy qualities of the almond nut or its by-products, nothing is reported on their formulation to be administered as a dietary supplement To better use these matrices, it would be appropriate to produce a formulated edible extract in order to improve its physicochemical and technological characteristics (solubility, palatability, manageability, stability) and to make it an ideal candidate for the production of health products with potential nutraceutical activity. This could make it possible to further enhance the value of by-products, maintaining a strong relationship with Mediterranean cultivars, which have great outcomes in terms of product healthiness [7]. Considering that polyphenols are able to act on inflammation processes through several mechanisms related to their antioxidative and radical scavenger properties [17], we evaluated the radical scavenging activity and the pharmacological potential of these products in an in vitro model of intestinal inflammation, in intestinal epithelial cells (IEC-6)
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