Pectin-Based Formulations for Controlled Release of an Ellagic Acid Salt with High Solubility Profile in Physiological Media
Metadata
Show full item recordEditorial
MDPI
Materia
Ellagic acid lysine salt Pectin-based formulations Controlled release Gut microbiota
Date
2021Referencia bibliográfica
Ortenzi, M.A.; Antenucci, S.; Marzorati, S.; Panzella, L.; Molino, S.; Rufián-Henares, J.Á.; Napolitano, A.; Verotta, L. Pectin-Based Formulations for Controlled Release of an Ellagic Acid Salt with High Solubility Profile in Physiological Media. Molecules 2021, 26, 433. https://doi.org/10.3390/molecules26020433
Sponsorship
European Union’s Horizon 2020 research and innovation program through the Stance4Health project (Grant No. 816303)Abstract
Among 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.