Development and In Vitro Evaluation of an Innovative “Dietary Flavonoid Supplement” on Osteoarthritis Process

Abstract

The aim of this study was to evaluate the antidegenerative effect in osteoarthritis damage of eriocitrin alone and eriocitrin formulated as innovative “dietary flavonoid supplement.” A complexation between eriocitrin and hydroxypropyl β-cyclodextrin by solubilization/freeze-drying method was performed. The complex in solution was evaluated by phase solubility studies and the optimal 1 : 2 flavanone/cyclodextrin molar ratio was selected. Hydroxypropyl β-cyclodextrin was able to complex eriocitrin as confirmed by UV-Vis absorption, DSC, and FTIR studies. The complex formed increased the eriocitrin water solubility (from 4.1 ± 0.2 g·L−1 to 11.0 ± 0.1 g·L−1) and dissolution rate (from 37.0% to 100%) in 30 min. The in vitro studies exhibit the notion that eriocitrin and its complex inhibit AGEs in a similar manner because hydroxypropyl β-cyclodextrin does not interfere with the flavanone intrinsic property. Instead, the presence of cyclodextrin improves eriocitrin antioxidant stability maintaining a high fluorescence value until 8 hours with respect to the pure materials. Moreover, hydroxypropyl β-cyclodextrin showed moderate GAGs restoration acting synergistically with the complexed compound to maintain the structural chondrocytes integrity. The results point out that ERT/HP-betaCD complex possesses technological and biological characteristics able to obtain an easily soluble nutraceutical product, which reduces the degenerative and oxidative damage which occurs in osteoarthritis, and improve the patient compliance.

Solid Lipid Nanoparticles Loading Idebenone Ester with Pyroglutamic Acid: In Vitro Antioxidant Activity and In Vivo Topical Efficacy

“…The ORAC assay has emerged as a valuable analytical method to determine the antioxidant potential of a range of substances [49,50], representing a reaction mechanism relevant to human biology [51]. This assay evaluates the fluorescence decrease of a fluorescent probe (fluorescein) due to the action of peroxyl radicals generated by thermal decomposition of 2,2′-azobis(2-methylpropionamidine) dihydrochloride (AAPH) [33].…”

Recycling of Almond By-Products for Intestinal Inflammation: Improvement of Physical-Chemical, Technological and Biological Characteristics of a Dried Almond Skins Extract

“…Sicilian almond skin acetonic extract contains polyphenols, well-known for their antioxidant activity [ 10 , 11 , 12 , 13 , 14 , 15 , 16 , 17 ]. Unfortunately, it was characterized by a low water solubility and a consequent slow and incomplete in vitro dissolution rate that affects in vivo bioavailability.…”

“…In addition, it is able to mask unpleasant flavors, thus also improving the organoleptic characteristics of the active ingredients [ 8 ]. CD is inserted in the “GRAS list”, it is already widely used in the food field and to ameliorate the chemical–physical, technological and biological characteristics of herbal extract and natural compounds [ 9 , 10 ]. Moreover, in the literature, it was reported that CD was able to complex (+) catechin, once of the most abundant components of almond skins [ 11 ], with optimal results in term of complexation and improvement in technological, biological and stability characteristics [ 12 , 13 , 14 , 15 , 16 ].…”

Application of Spray Drying Particle Engineering to a High-Functionality/Low-Solubility Milk Thistle Extract: Powders Production and Characterization

“…A way to enhance the absorption after the oral administration as well as, targeted biological efficacy is to produce technological delivery systems able to improve dissolution and permeation rate of the active ingredient [ 2 , 3 ]. Numerous delivery systems had been developed and studied extensively in oral drug delivery [ 4 , 5 , 6 ], but the application of this research area to nutraceuticals only is emerging very recently [ 7 , 8 , 9 , 10 , 11 , 12 ]. The milk thistle ( Silybum marianum (L.) Gaertn, Asteraceae), extract is an essential source of silymarin; it is a well-known complex of flavonolignans (silybin A and B, isosilybin A and B, silydianin, and silychristin) and flavonoids (taxifolin and quercetin) used to treat a variety of ailments like liver (hepatitis, cirrhosis, and icterus), kidney, and gallbladder problems [ 13 , 14 ].…”