The simultaneous intake of food and drugs can have a strong impact on drug release, absorption, distribution, metabolism and/or elimination and consequently, on the efficacy and safety of ...pharmacotherapy. As such, food-drug interactions are one of the main challenges in oral drug administration. Whereas pharmacokinetic (PK) food-drug interactions can have a variety of causes, pharmacodynamic (PD) food-drug interactions occur due to specific pharmacological interactions between a drug and particular drinks or food. In recent years, extensive efforts were made to elucidate the mechanisms that drive pharmacokinetic food-drug interactions. Their occurrence depends mainly on the properties of the drug substance, the formulation and a multitude of physiological factors. Every intake of food or drink changes the physiological conditions in the human gastrointestinal tract. Therefore, a precise understanding of how different foods and drinks affect the processes of drug absorption, distribution, metabolism and/or elimination as well as formulation performance is important in order to be able to predict and avoid such interactions. Furthermore, it must be considered that beverages such as milk, grapefruit juice and alcohol can also lead to specific food-drug interactions. In this regard, the growing use of food supplements and functional food requires urgent attention in oral pharmacotherapy. Recently, a new consortium in Understanding Gastrointestinal Absorption-related Processes (UNGAP) was established through COST, a funding organisation of the European Union supporting translational research across Europe. In this review of the UNGAP Working group “Food-Drug Interface”, the different mechanisms that can lead to pharmacokinetic food-drug interactions are discussed and summarised from different expert perspectives.
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Olive pomace extract (OPE) was investigated as a potential surface modifier for the development of the green synthesis process of selenium nanoparticles (SeNPs). In order to evaluate them as ...potential nutraceuticals, the obtained nanosystems were characterized in terms of size distribution, shape, zeta potential, stability in different media, gastrointestinal bioaccessibility and biocompatibility. Systems with a unimodal size distribution of spherical particles were obtained, with average diameters ranging from 53.3 nm to 181.7 nm, depending on the type of coating agent used and the presence of OPE in the reaction mixture. The nanosystems were significantly affected by the gastrointestinal conditions. Bioaccessibility ranged from 33.57% to 56.93% and it was significantly increased by functionalization of with OPE. Biocompatibility was investigated in the HepG2 and Caco2 cell models, proving that they had significantly lower toxicity in comparison to sodium selenite. Significant differences were observed in cellular responses depending on the type of cells used, indicating differences in the mechanisms of toxicity induced by SeNPs. The obtained results provide new insight into the possibilities for the utilization of valuable food-waste extracts in the sustainable development of nanonutraceuticals.
olive pomace extract (OPE) is a rich source of health promoting polyphenols (hydroxytyrosol (HTS) and tyrosol (TS)) and can be used as a nutraceutical ingredient of dietary supplements and functional ...foods. Its adequate bioavailability is a prerequisite for excreting biological activity and can be significantly and specifically affected by different food matrices.
in order to investigate food effects on polyphenol bioaccessibility, OPE was co-digested with different foods according to internationally harmonized in vitro digestibility method. Impact of particular nutrients on HTS and TS permeability was assessed on Caco-2 cell monolayer.
HTS and TS bioaccessibility and transepithelial permeability can be significantly affected by foods (nutrients), especially by casein and certain types of dietary fiber. Those effects are polyphenol-and nutrient-specific and are achieved either through complexation in gastrointestinal lumen and/or through direct effects of nutrients on intestinal monolayer.
obtained results emphasize the significance and complexity of polyphenol interactions within the food matrix and the necessity of individual investigational approaches with respect to particular food/nutrient and interacting phenolic compounds.
Strawberry tree (Arbutus unedo L.) leaves are used in folk medicine for treating inflammation, hypertension, and diabetes. The aims of this study were to evaluate the antimicrobial effects of A. ...unedo leaf extracts on 15 uropathogens and test the extent to which arbutin, as the most abundant bioactive compound in the leaves, is responsible for their antimicrobial activity. Antimicrobial activity of leaf extracts against urinary pathogenic microorganisms was tested by agar well diffusion assay and twofolded microdilution method. Since the polyphenolic content responsible for A. unedo leaves’ antimicrobial activity depends on climate and geolocation, the authors determined the total phenolic, tannin, flavonoid and phenolic acid content using spectrophotometric methods, arbutin and hydroquinone mass fraction using high performance liquid chromatography coupled with a diode array detector (HPLC–DAD) and antioxidative activities by FRAP, ABTS, and DPPH assay. Although methanol was shown to be a more effective solvent for the extraction of polyphenols from leaves, the traditionally used aqueous extract exhibited similar antimicrobial properties. While arbutin did not show direct antimicrobial activity, its metabolite hydroquinone showed strong antimicrobial activity against the tested uropathogens. The strongest antimicrobial activity of leaf extracts was detected for uropathogenic strains of Enterococcus faecalis, which was probably associated with the ability of bacterial β-glucosidase, exerting strong activity in E. faecalis, to convert arbutin to hydroquinone. Our study suggested that the aqueous extract of strawberry tree leaves has the potential for use as a phytotherapeutic in clinical application and should be further investigated.
Selenium nanoparticles (SeNPs) represent novel selenium (Se) formulation characterized by improved biocompatibility and a wider therapeutic range in comparison to inorganic Se. The aim of this work ...was to investigate the possibilities of functionalization of SeNPs with olive pomace extract (OPE), rich in health-promoting polyphenols, and to obtain innovative forms of nutraceuticals. Cytotoxic and antioxidative activities of four types of SeNPs (polyvinylpyrrolidone stabilized (PVP SeNPs), polysorbate stabilized (PS SeNPs), polyvinylpyrrolidone stabilized and functionalized using OPE (f PVP SeNPs) and polysorbate stabilized and functionalized using OPE (f PS SeNPs) were investigated. SeNPs showed lower toxicity on human hepatocellular carcinoma (HepG2) and human colorectal adenocarcinoma (Caco2) cells compared to selenite. Functionalization with polyphenols significantly improved their direct antiradical (f PVP SeNPs: 24.4 ± 1.84 and f PS SeNPs: 30.9 ± 2.47 mg TE/mmol Se) and reducing properties (f PVP SeNPs: 50 ± 3.16 and f PS SeNPs: 53.6 ± 3.22 mg GAE/mmol) compared to non-functionalized SeNPs. The significant impact of tested SeNPs on intracellular antioxidative mechanisms has been observed and it was dependent on both cell type and physico-chemical properties of SeNPs, indicating the complexity of involved mechanisms.
Astaxanthin (ASTA) and zeaxanthin (ZEA) are xanthophyll carotenoids showing a wide spectrum of health-promoting properties. However, their utilization is limited, mostly due to poor water solubility, ...limited bioavailability, and a tendency to oxidate, as well as photo- and thermal instability. The aim of this work was to develop ASTA- and ZEA-loaded nano-structured lipid carriers (NLCs) that would protect them against degradation and improve their intestinal stability/permeability. Obtained NLCs were characterized by an effective diameter of 294 nm for ASTA-NLC and 280 nm for ZEA-NLC; polydispersity index (
) lower than 0.2; and zeta potential of –29.4 mV and –29.0 mV, respectively. Interestingly, despite similar physicochemical characteristics, our investigation revealed differences in the encapsulation efficiency of ASTA-NLC and ZEA-NLC (58.0 %
. 75.5 %, respectively). Obtained NLCs were stable during a 21 day-storage period in the dark at room temperature or at 4 °C. Investigation of gastrointestinal stability showed no change in effective diameter and
under gastric conditions while both parameters significantly changed under intestinal conditions. Our results showed for the first time that both ASTA- and ZEA-NLCs intestinal absorption investigated in the
model is significantly increased (in relation to pure compounds) and is affected by the presence of mucus. This study provides useful data about the advantages of using NLC as a delivery system for ASTA and ZEA that might facilitate their applications in the food and pharmaceutical industry.
Waste remaining after the production of olive oil (olive pomace) is known to contain significant amounts of phenolic compounds that exert different types of biological activities, primarily acting as ...antioxidants. In this work, a sustainable approach that combines ultrasound-assisted extraction with food-grade solvents and encapsulation with different types of cyclodextrins was used to prepare olive pomace-based polyphenol rich extracts that were tested as antioxidants in various chemical, food, and biological model systems. Encapsulation with cyclodextrins had a significant positive impact on the chemical composition of obtained extracts and it positively affected their antioxidant activity. Observed effects can be explained by an increased content of polyphenols in the formulations, specific physical properties of encapsulated compounds improving their antioxidant activity in complex food/physiological environment, and enhanced interaction with natural substrates. Depending on the applied model, the tested samples showed significant antioxidant protection in the concentration range 0.1⁻3%. Among the investigated cyclodextrins, hydroxypropyl-β-cyclodextrin and randomly methylated-β-cyclodextrin encapsulated extracts showed particularly good antioxidant activity and were especially potent in oil-in-water emulsion systems (1242 mg/g and 1422 mg/g of Trolox equivalents, respectively), showing significantly higher antioxidant activity than Trolox (reference antioxidant). In other models, they provided antioxidant protection comparable to commonly used synthetic antioxidants at concentration levels of 2⁻3%.
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