The cellular uptake and simulated intestinal wall transportation of resveratrol-loaded zein/pectin nanoparticles were assessed using Caco-2 cells and monolayers, respectively. The oral bioavailabilities of encapsulated (En-RES) and free (RES) resveratrol were evaluated by monitoring the resveratrol concentration in rat plasma after oral administration. The impact of encapsulation on the anti-inflammatory activity of the resveratrol was determined using lipopolysaccharide (LPS)-treated RAW 264.7 macrophages. The cellular uptake of encapsulated resveratrol increased appreciably with observation time (1–4 h), reaching a maximum value (≈1.06 μg mL⁻¹) after 2 h, whereas that of free resveratrol (in DMSO) only increased slightly, reaching 0.62 μg mL⁻¹ after 4 h. The transmembrane transport of En-RES was significantly higher than that of RES (p < 0.05): the resveratrol concentration in the receiving compartment of Costar trans-wells was 4.7-fold higher for the encapsulated resveratrol. The resveratrol concentration in the plasma of rats was measured after they were fed formulations containing a resveratrol equivalent of 20 mg per kg bodyweight. The plasma level reached a maximum value of 1.35 ± 0.26 μg mL⁻¹ at 4 h after feeding the En-RES formulation, and then decreased to 0.19 ± 0.04 μg mL⁻¹ after 48 h. Conversely, the plasma level only reached a maximum value of 0.31 ± 0.05 μg mL⁻¹ at 0.5 h after feeding the free resveratrol formulation (an aqueous PEG 400 solution), and was totally cleared after 8 h. Cell culture studies suggested that En-RES exhibited a strong anti-inflammatory activity by inhibiting the production of NO, PGE₂, IL-1β, IL-6, TNF-α, promoting IL-10 release, inhibiting expression of TLR4, and inhibiting phosphorylation of JNK, ERK1/2, p38 and MAPK. Overall, this research suggests that zein-pectin core/shell nanoparticles are a highly effective delivery system for resveratrol, significantly increasing its bioavailability and anti-inflammation activity. These oral delivery systems may be particularly suitable for applications in functional foods or pharmaceuticals.

Background: Pure 1, 3-diacylglycerols (1, 3-DAG) have been considered to be significant surfactants in food, cosmetics and pharmaceutical industries, as well as the effect on obesity prevention. Methods: In this study, a vacuum-driven air bubbling operation mode was developed and evaluated for the enzymatic synthesis of 1, 3-DAG of saturated fatty acids, by direct esterification of glycerol with fatty acids in a solvent-free system. The employed vacuum-driven air bubbling operation mode was comparable to vacuum-driven N₂ bubbling protocol, in terms of lauric acid conversion and 1, 3-dilaurin content. Results: Some operation parameters were optimized, and 95.3% of lauric acid conversion and 80.3% of 1, 3-dilaurin content was obtained after 3-h reaction at 50°C, with 5 wt% of Lipozyme RM IM (based on reactants) amount. Of the lipases studied, both Lipozyme RM IM and Novozym 435 exhibited good performance in terms of lauric acid conversion. Lipozyme TL IM, however, showed low activity. Lipozyme RM IM showed good operational stability in this operation protocol, 80.2% of the original catalytic activity remained after 10 consecutive batch applications. Some other 1, 3-DAG were prepared and high content was obtained after purification: 98.5% for 1, 3-dicaprylin, 99.2% for 1, 3-dicaprin, 99.1% for 1, 3-dilaurin, 99.5 for 1, 3-dipalmitin and 99.4% for 1, 3-disterin. Conclusion: The established vacuum-driven air bubbling operation protocol had been demonstrated to be a simple-operating, cost-effective, application practical and efficient methodology for 1, 3-DAG preparation.