Release of adsorbed ferulic acid in simulated gastrointestinal conditions

Abstract

Ferulic acid (FA) is a natural antioxidant with limited absorption when conjugated with biomolecules but whose free form is readily absorbed in the stomach and, to a lesser extent, in the ileum. The latter suffers from inflammation and oxidative stress, so a novel strategy for the delivery of FA in this compartment of the gastrointestinal tract was developed. Using the neutral un-functionalized resin Lewatit® VP OC 1064 MD PH, under optimized conditions, a loading of 144 mg FA/g of dry resin was obtained. By means of an in vitro simulated digestion, an average release of 32 mg FA/g of dry loaded resin (recovery of 22%) was observed in intestinal conditions. The incorporation/release of FA onto/from the resin was confirmed by ATR-FTIR spectroscopy and by HPLC-DAD. This work showed that the free form of FA can effectively be delivered in the small intestine, after immobilization in solid matrices. Keywords Ferulic acid • Adsorption • Release • In vitro digestion simulation • Intestine Abbreviations ATR-FTIR Attenuated total reflectance-Fourier transform infrared C 0 Initial concentration CA Caffeic acid C e Concentration at equilibrium ChA 5-O-Caffeoylquinic acid C r Concentration of released ferulic acid FA Ferulic acid GI Gastrointestinal HCA(s) Hydroxycinnamic acid(s) HPLC-DAD High-performance liquid chromatography with diode-array detection Lewatit Lewatit® VP OC 1064 MD PH m Mass of resin pCA p-Coumaric acid q e Amount of compound adsorbed for unit mass of adsorbent q r Amount of ferulic acid released from the resin SA Sinapic acid V Volume of solution V r Volume of simulated medium Electronic supplementary material The online version of this article (

The intestinal delivery systems of ferulic acid: Absorption, metabolism, influencing factors, and potential applications

“…It was reported that 25% of FA in tomatoes could be effectively absorbed. However, 5‐ O ‐feruloyl‐ l ‐arabinofuranose (FAA), a typical FA sugar ester in cereals, showed a lower absorption rate (Martins et al., 2020). Only 3% of FA from cereals and its metabolites were detected in urine, whereas 50% were tested upon free FA treatments (Lafay & Gil‐Izquierdo, 2007).…”

“…The resin has the ability to selectively adsorb FA from hydrolyzed complex matrices without the need for sugar co‐adsorption. The release of FA from the resin by the resin FA complex under the conditions found in the GI tract (e.g., pH changes) was evaluated (recovery of 22%) (Martins et al., 2020). The acidic medium promoted the adsorption of FA and impeded its release, whereas alkaline media caused the release of FA from the adsorbent and hindered its adsorption.…”

“…Besides, FA has tremendous advantages in protecting intestinal health, including repairing intestinal barrier damage, inhibiting inflammatory reaction, and regulating gut microbiota (GM). FA has been considered a potential prophylactic or therapeutic agent for gastrointestinal (GI) inflammation (Martins et al., 2020), inhibiting intestinal diseases (IDs), such as inflammatory bowel disease (IBD), irritable bowel syndrome, and intestinal cancer.…”

Recent Advances in Biological Activity, New Formulations and Prodrugs of Ferulic Acid

“…The obtained formulation ensures the sustained release of the active substance [ 97 ]. Attempts have also been made to immobilize FA in the solid porous resin Lewatit ® , which provides the nanoparticles with narrow size distributions [ 98 ].…”