Functionalization of selenium nanoparticles with olive polyphenols - impact on toxicity and antioxidative activity.

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.

Preparation of astaxanthin/zeaxanthin-loaded nanostructured lipid carriers for enhanced bioavailability: Characterization-, stability-and permeability study.

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 (PDI) 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 % vs. 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 PDI 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 in vitro 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.

Cellular Antioxidant Activity of Olive Pomace Extracts: Impact of Gastrointestinal Digestion and Cyclodextrin Encapsulation.

Olive pomace is a valuable secondary raw material rich in polyphenols, left behind after the production of olive oil. The present study investigated the protective effect of a polyphenolic extract from olive pomace (OPE) on cell viability and antioxidant defense of cultured human HepG2 cells submitted to oxidative stress induced by tert-butylhydroperoxide (tBOOH). The investigation considered possible matrix effects, impact of gastrointestinal digestion and cyclodextrin (CD) encapsulation. Pre-treatment of cells with OPE prevented cell damage and increased intracellular glutathione but did not affect the activity of glutathione peroxidase and superoxide dismutase. OPE matrix significantly enhanced cell protective effects of major antioxidants, such as hydroxytyrosol (HTS), while cyclodextrin encapsulation enhanced activity of OPE against intracellular reactive oxygen species (ROS) accumulation. The obtained results show that OPE is more potent antioxidant in comparison to equivalent dose of main polyphenols (HTS and TS) and that increasing solubility of OPE polyphenols by CD encapsulation or digestion enhances their potential to act as intracellular antioxidants. Antioxidative protection of cells by OPE was primarily achieved through direct radical-scavenging/reducing actions rather than activation of endogenous defense systems in the cell.

The mechanisms of pharmacokinetic food-drug interactions - A perspective from the UNGAP group.

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.

Alpha Lipoic Acid Reduces Symptoms and Inflammation Biomarkers in Patients with Chronic Hemorrhoidal Illness.

Background: Oral dietary supplementation is becoming increasingly popular as an addition to classical approaches for the prevention and treatment of hemorrhoidal disease. Aim: To examine the effect of orally administrated alpha lipoic acid (ALA), known for its antioxidant and anti-inflammatory properties, in the treatment of patients with permanent symptoms of hemorrhoidal disease. Methods: Patients with second- and third-degree hemorrhoids (n = 100) were enrolled into a randomized, open label, single-center trial. The study group (n = 50) was treated with 200 mg of orally administered ALA once a day during the 12-week period, the control group (n = 50) did not receive any treatment. Results: There were no significant differences in demographics, diagnosis, or exposure to major risk factors between the study and placebo group at baseline. ALA significantly improved subjective efficacy variables, such as pain and discomfort (p < 0.01) as well as objective signs of the disease, such as bleeding (p < 0.01), in comparison to the control group. Furthermore, the 3-month treatment significantly reduced the number of patients with positive C-reactive protein (CRP) value (serum CRP > 5 mg/L) from 18% before to only 2% after the treatment (χ2 = 4.65; p < 0.01). Average leukocyte count has also been significantly reduced in the treatment group (p < 0.01) from 7.29 × 109/L before to 6.18 × 109/L after treatment. Conclusions: The obtained results indicate that ALA is effective in the treatment of second- and third-degree hemorrhoids. Larger, double-blind controlled trials are needed to confirm the results and to investigate optimal treatment regimens.

A comparison of the nutritional value and food safety of organically and conventionally produced wheat flours.

Growing interest in organic agriculture has prompted this study aiming to evaluate nutritional content of wheat flours originating from organic and conventional production systems. Obtained results showed that organic samples had significantly lower protein content and lower levels of Ca, Mn and Fe compared to conventional samples. Protein digestibility and levels of K, Zn and Mo were significantly higher in organic than in conventional wheat flours. Regarding undesirable metals, significantly higher levels of As and Cd were found in conventional compared to organic wheat flours. Although the mean concentrations of zearalenone and ochratoxin A were higher in conventional than in organic flours, this difference was not significant. This study revealed that organic agriculture has the potential to yield products with some relevant improvements in terms of high quality proteins and microelements contents, while the reduction in contamination with toxic elements and mycotoxins may be accomplished.