Ortenzi, Marco AldoAntenucci, StefanoMarzorati, StefaniaPanzella, LuciaMolino, SilviaRufián-Henares, José ÁngelNapolitano, AlessandraVerotta, Luisella2022-12-162022-12-162021-01-15Ortenzi MA, Antenucci S, Marzorati S, Panzella L, Molino S, Rufián-Henares JÁ, et al. Pectin-Based Formulations for Controlled Release of an Ellagic Acid Salt with High Solubility Profile in Physiological Media. Molecules. 2021 Jan 15;26(2):433http://hdl.handle.net/10668/4524Among bioactive phytochemicals, ellagic acid (EA) is one of the most controversial because its high antioxidant and cancer-preventing effects are strongly inhibited by low gastrointestinal absorption and rapid excretion. Strategies toward an increase of solubility in water and bioavailability, while preserving its structural integrity and warranting its controlled release at the physiological targets, are therefore largely pursued. In this work, EA lysine salt at 1:4 molar ratio (EALYS), exhibiting a more than 400 times increase of water solubility with respect to literature reports, was incorporated at 10% in low methoxylated (LM) and high methoxylated (HM) pectin films. The release of EA in PBS at pH 7.4 from both film preparations was comparable and reached 15% of the loaded compound over 2 h. Under simulated gastric conditions, release of EA from HM and LM pectin films was minimal at gastric pH, whereas higher concentrations-up to 300 μM, corresponding to ca. 50% of the overall content-were obtained in the case of the HM pectin film after 2 h incubation at the slightly alkaline pH of small intestine environment, with the enzyme and bile salt components enhancing the release. EALYS pectin films showed a good prebiotic activity as evaluated by determination of short chain fatty acids (SCFAs) levels following microbial fermentation, with a low but significant increase of the effects produced by the pectins themselves. Overall, these results highlight pectin films loaded with EALYS salt as a promising formulation to improve administration and controlled release of the compound.enAtribución 4.0 Internacionalhttp://creativecommons.org/licenses/by/4.0/Ellagic acid lysine saltPectin-based formulationsControlled releaseGastrointestinal digestionGut microbiotaÁcido elágicoLisinaPectinasPreparaciones de acción retardadaDigestiónMicrobioma gastrointestinalMedical Subject Headings::Phenomena and Processes::Metabolic Phenomena::Pharmacokinetics::Biological AvailabilityMedical Subject Headings::Chemicals and Drugs::Pharmaceutical Preparations::Dosage Forms::Delayed-Action PreparationsMedical Subject Headings::Analytical, Diagnostic and Therapeutic Techniques and Equipment::Investigative Techniques::Technology, Pharmaceutical::Drug CompoundingMedical Subject Headings::Chemicals and Drugs::Heterocyclic Compounds::Heterocyclic Compounds, 2-Ring::Benzopyrans::Ellagic AcidMedical Subject Headings::Anatomy::Fluids and Secretions::FecesMedical Subject Headings::Phenomena and Processes::Chemical Phenomena::Biochemical Phenomena::Biochemical Processes::Carbohydrate Metabolism::FermentationMedical Subject Headings::Organisms::Eukaryota::Animals::Chordata::Vertebrates::Mammals::Primates::Haplorhini::Catarrhini::Hominidae::HumansMedical Subject Headings::Phenomena and Processes::Chemical Phenomena::Biochemical Phenomena::Biochemical Processes::HydroxylationMedical Subject Headings::Phenomena and Processes::Metabolic Phenomena::Metabolism::Absorption::Intestinal AbsorptionMedical Subject Headings::Chemicals and Drugs::Carbohydrates::Polysaccharides::PectinsMedical Subject Headings::Phenomena and Processes::Chemical Phenomena::Physicochemical Phenomena::SolubilityMedical Subject Headings::Phenomena and Processes::Microbiological Phenomena::MicrobiotaMedical Subject Headings::Phenomena and Processes::Physiological Phenomena::Physiological Processes::Nutrition Processes::Digestionresearch article33467593Acceso abierto10.3390/molecules260204331420-3049PMC7829853