title: 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 hydroxypropylβ-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. Hydroxypropylβ-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-1to 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 hydroxypropylβ-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, hydroxypropylβ-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.
authors.affiliation: Department of Pharmacy, University of Salerno, Via Giovanni Paolo II, 84084 Fisciano, Italy.
authors.forename: Maria Rosaria
authors.identifier: 0000-0001-7362-826X
authors.initials: MR
authors.lastname: Lauro
authors.affiliation: Department of Drug Science, University of Catania, Viale A. Doria, 95100 Catania, Italy.
authors.forename: Lucia
authors.identifier: 0000-0002-9175-0223
authors.initials: L
authors.lastname: Crascí
authors.affiliation: Department of Pharmacy, University of Salerno, Via Giovanni Paolo II, 84084 Fisciano, Italy.
authors.forename: Francesca
authors.identifier: 0000-0002-3589-5196
authors.initials: F
authors.lastname: Sansone
authors.affiliation: Department of Biomedical and Biotechnological Sciences, Section of Physiology, University of Catania, Via Santa Sofia 64, 95125 Catania, Italy.
authors.forename: Venera
authors.identifier: 0000-0001-9902-3736
authors.initials: V
authors.lastname: Cardile
authors.affiliation: Department of Drug Science, University of Catania, Viale A. Doria, 95100 Catania, Italy.
authors.forename: Anna Maria
authors.initials: AM
authors.lastname: Panico
authors.affiliation: Department of Drug Science, University of Catania, Viale A. Doria, 95100 Catania, Italy.
authors.forename: Giovanni
authors.initials: G
authors.lastname: Puglisi
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000328:Adult; D002152:Calorimetry, Differential Scanning; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D019902:Chondrocytes / Q000166:cytology / Q000378:metabolism; D019587:Dietary Supplements; D004339:Drug Compounding; D044950:Flavanones / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D005419:Flavonoids / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D010003:Osteoarthritis / Q000378:metabolism / Q000473:pathology / Q000517:prevention & control; D018384:Oxidative Stress / Q000187:drug effects*; D012995:Solubility; D013056:Spectrophotometry, Ultraviolet; D017550:Spectroscopy, Fourier Transform Infrared; D047392:beta-Cyclodextrins / Q000737:chemistry
chemical_list: D044950:Flavanones; D005419:Flavonoids; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; C114706:eriocitrin