Bioavailability Of Nutraceuticals Research Articles

Synergistic effects of superfine grinding and high hydrostatic pressure on the contents, distribution, digestive behaviors and antioxidant activities of polyphenols in barley leaves

Barley leaves (BLs) naturally contained abundant phenolics, most of which are hardly completely released from food matrix during gastrointestinal digestion. Superfine grinding (SFG) and high hydrostatic pressure (HHP) are generally used to treat the functional plants due to their effectiveness to cell wall-breaking and improvement of nutraceutical bioavailability. Thus, this study investigated the synergistic effects of SFG and HHP (100, 300, 500 MPa/20 min) on the bioaccessbility of typical phenolics in BLs during the simulated in-vitro digestion. The results demonstrated that the highest bioaccessbility (40.98%) was found in the ultrafine sample with HHP at 500 MPa. CLSM and SEM confirmed SFG led to microstructurally rapture of BLs. Moreover, the recovery index of ABTS radical scavenging activity and FRAP of HHP-treated ultrafine and fine BLs samples maximumly increased by 53.62% and 9.61%, respectively. This study is expecting to provide the theoretical basis to improve the consumer acceptance of BLs.

Lipid Nanoparticles: An Effective Tool to Improve the Bioavailability of Nutraceuticals.

Nano-range bioactive colloidal carrier systems are envisaged to overcome the challenges associated with treatments of numerous diseases. Lipid nanoparticles (LNPs), one of the extensively investigated drug delivery systems, not only improve pharmacokinetic parameters, transportation, and chemical stability of encapsulated compounds but also provide efficient targeting and reduce the risk of toxicity. Over the last decades, nature-derived polyphenols, vitamins, antioxidants, dietary supplements, and herbs have received more attention due to their remarkable biological and pharmacological health and medical benefits. However, their poor aqueous solubility, compromised stability, insufficient absorption, and accelerated elimination impede research in the nutraceutical sector. Owing to the possibilities offered by various LNPs, their ability to accommodate both hydrophilic and hydrophobic molecules and the availability of various preparation methods suitable for sensitive molecules, loading natural fragile molecules into LNPs offers a promising solution. The primary objective of this work is to explore the synergy between nature and nanotechnology, encompassing a wide range of research aimed at encapsulating natural therapeutic molecules within LNPs.

Metabolomics of ethnic fermented foods and beverages: understanding new aspects through Omic techniques

In the era of Omics, metabolomics and metaproteomics have emerged as powerful tools for the deep analysis of the fermentation of various foods. These two are relatively new in the field of science. However, they are already proven to be crucial for a more proper understanding of microbes, their interactions with hosts and surrounding environments, metabolic activity, and intracellular biochemical reactions. Metabolomics is a quantitative and qualitative determination study of metabolites of participated microbes in the process of fermentation that helps to analyze several biochemical pathways concerning chemical changes that occur during different stages of fermentation. Hence, it provides a deep insight into the microscopic world as well as helps to significantly enhance the available nutraceuticals and probiotic characterizations in fermented foods. Evaluating the possible pathways of microbes in generating particular compounds of interest is proven to be beneficial for increasing the bioavailability of nutraceuticals and nutrients. It can be utilized to reshape the general process of fermentation in a more improved and optimized way for better yielding of nutritive components while decreasing the antinutrient components in the specific product. Metabolomics studies can be used to modify strains based on specific needs, for example, different stress-tolerant microbial strains for the optimal production of desired metabolites in stressed conditions, modulation in metabolic pathways to naturally increase the bioavailability of beneficial compounds, etc. These “Omics” methods are paving the way for a more thorough understanding of microbial life, metabolism systems, and genetic characteristics regarding protein synthesis and are undoubtedly becoming a potent weapon or a universal key in modulating fermented food products in a more advanced and sustainable approach possible. This present review aims to constitute a relevant approach for understanding the metabolic processes that can occur or are currently occurring in a given system and for implementing novel strategies focused on solving production problems or improving sustainability.

The Anticancer Potential of Plant-Derived Nutraceuticals via the Modulation of Gene Expression.

Current studies show that approximately one-third of all cancer-related deaths are linked to diet and several cancer forms are preventable with balanced nutrition, due to dietary compounds being able to reverse epigenetic abnormalities. An appropriate diet in cancer patients can lead to changes in gene expression and enhance the efficacy of therapy. It has been demonstrated that nutraceuticals can act as powerful antioxidants at the cellular level as well as anticarcinogenic agents. This review is focused on the best studies on worldwide-available plant-derived nutraceuticals: curcumin, resveratrol, sulforaphane, indole-3-carbinol, quercetin, astaxanthin, epigallocatechin-3-gallate, and lycopene. These compounds have an enhanced effect on epigenetic changes such as histone modification via HDAC (histone deacetylase), HAT (histone acetyltransferase) inhibition, DNMT (DNA methyltransferase) inhibition, and non-coding RNA expression. All of these nutraceuticals are reported to positively modulate the epigenome, reducing cancer incidence. Furthermore, the current review addresses the issue of the low bioavailability of nutraceuticals and how to overcome the drawbacks related to their oral administration. Understanding the mechanisms by which nutraceuticals influence gene expression will allow their incorporation into an “epigenetic diet” that could be further capitalized on in the therapy of cancer.

A review of recent progress in improving the bioavailability of nutraceutical-loaded emulsions after oral intake.

Increasing awareness of the health benefits of specific constituents in fruits, vegetables, cereals, and other whole foods has sparked a broader interest in the potential health benefits of nutraceuticals. Many nutraceuticals are hydrophobic substances, which means they must be encapsulated in colloidal delivery systems. Oil-in-water emulsions are one of the most widely used delivery systems for improving the bioavailability and bioactivity of these nutraceuticals. The composition and structure of emulsions can be designed to improve the water dispersibility, physicochemical stability, and bioavailability of the encapsulated nutraceuticals. The nature of the emulsion used influences the interfacial area and properties of the nutraceutical-loaded oil droplets in the gastrointestinal tract, which influences their digestion, as well as the bioaccessibility, metabolism, and absorption of the nutraceuticals. In this article, we review recent in vitro and in vivo studies on the utilization of emulsions to improve the bioavailability of nutraceuticals. The findings from this review should facilitate the design of more efficacious nutraceutical-loaded emulsions with increased bioactivity.

Recent Advances in the Gastrointestinal Fate of Organic and Inorganic Nanoparticles in Foods.

Inorganic or organic nanoparticles are often incorporated into foods to enhance their quality, stability, nutrition, or safety. When they pass through the gastrointestinal environment, the properties of these nanoparticles are altered, which impacts their biological effects and potential toxicity. Consequently, there is a need to understand how different kinds of nanoparticles behave within the gastrointestinal tract. In this article, the current understanding of the gastrointestinal fate of nanoparticles in foods is reviewed. Initially, the fundamental physicochemical and structural properties of nanoparticles are discussed, including their compositions, sizes, shapes, and surface chemistries. Then, the impact of food matrix effects and gastrointestinal environments on the fate of ingested nanoparticles is discussed. In particular, the influence of nanoparticle properties on food digestion and nutraceutical bioavailability is highlighted. Finally, future research directions are highlighted that will enable the successful utilization of nanotechnology in foods while also ensuring they are safe.

Mucoadhesive Delivery System: A Smart Way to Improve Bioavailability of Nutraceuticals.

The conventional oral administration of many nutraceuticals exhibits poor oral bioavailability due to the harsh gastric conditions and first-pass metabolism. Oral mucosa has been recognized as a potential site for the delivery of therapeutic compounds. The mucoadhesive formulation can adhere to the mucosal membrane through various interaction mechanisms and enhance the retention and permeability of bioactive compounds. Absorption of bioactive compounds from the mucosa can improve bioavailability, as this route bypasses the hepatic first-pass metabolism and transit through the gastrointestinal tract. The mucosal administration is convenient, simple to access, and reported for increasing the bioactive concentration in plasma. Many mucoadhesive polymers, emulsifiers, thickeners used for the pharmaceutical formulation are accepted in the food sector. Introducing mucoadhesive formulations specific to the nutraceutical sector will be a game-changer as we are still looking for different ways to improve the bioavailability of many bioactive compounds. This article describes the overview of buccal mucosa, the concept of mucoadhesion and related theories, and different techniques of mucoadhesive formulations. Finally, the classification of mucoadhesive polymers and the mucoadhesive systems designed for the effective delivery of bioactive compounds are presented.

Bioavailability of quercetin in zein-based colloidal particles-stabilized Pickering emulsions investigated by the in vitro digestion coupled with Caco-2 cell monolayer model

Protein-based Pickering emulsions have received considerable attention as nutraceutical vehicles. However, the oral bioavailability of nutraceuticals encapsulated in Pickering emulsions was not well established. In this work, a simulated gastrointestinal tract/Caco-2 cell culture model was applied to investigate the oral bioavailability of quercetin encapsulated in zein-based Pickering emulsions with quercetin in zein particles as the control. Pickering emulsions with shell (ZCP-QE) and core quercetin (ZCPE-Q) were constructed, and quercetin bioaccessibility, cell uptake and secretion, and the overall bioavailability were evaluated and compared. The overall oral bioavailability of quercetin was increased from 2.71% (bulk oil) to 38.18% (ZCPs-Q) and 18.97% (ZCPE-Q), particularly reached 41.22% for ZCP-QE. This work took new insights into the contributions of bioaccessibility and absorption (cell uptake plus secretion) to the overall oral bioavailability of quercetin. A schematic representation is proposed to relate the types of colloidal nanostructures in the digesta to the uptake, cell absorption, and overall oral bioavailability of quercetin. This study provided an attractive basis for identifying effective strategies to improve the oral bioavailability of hydrophobic nutraceuticals.

Nanotechnology in Food Systems: A Review

Recent developments of nanotechnology find its way into various fields of food production in our days. Nanotechnology could offer benefits in development of food products with enhanced functionality for health promotion, or modified texture convenient for elderly, and in quality and safety issues in the food supply chain. Nanoencapsulated bioactive components such as vitamins, antibacterial agents contribute to production of enriched food stuffs with the required appearance, flavour, taste, and texture. Nanomaterials can protect the sensitive compounds from environmental attack, release them in a programmed way, and provide favourable improvement in the bioavailability of nutraceuticals. The innovative approach in food packaging, including the detection, indication, and control of food products, serves the quality and safety improvements.

Bioavailability and bioaccessibility of food bioactive compounds; overview and assessment by in vitro methods.

Oral bioavailability is the key to the bioefficiency of food bioactive ingredients; it evaluates the relationship between foods and their health benefits. The analysis of the main factors limiting the oral bioavailability (bioaccessibility, absorption, and transformation) has led to the proposal of classification systems for pharmaceuticals and nutraceuticals (Biopharmaceuticals Classification System and Nutraceutical Bioavailability Classification Scheme). Based on the relevant studies published in the last decade, this review presents the essential aspects regarding the factors limiting the oral bioavailability of the biocomponents and different in vitro methods used to investigate the mechanisms involved in the digestion, absorption, and metabolism of biocomponents, particularly encapsulated bioactive compounds. Oral bioavailability investigated by in vitro studies provides the food and drug manufacturers with information to formulate delivery systems more efficiently and to determine the dosage of biocomponents for increase the health benefits and avoid or reduce the risk of toxicity.

Impact of Pesticide Type and Emulsion Fat Content on the Bioaccessibility of Pesticides in Natural Products.

There is interest in incorporating nanoemulsions into certain foods and beverages, including dips, dressings, drinks, spreads, and sauces, due to their potentially beneficial attributes. In particular, excipient nanoemulsions can enhance the bioavailability of nutraceuticals in fruit- and vegetable-containing products consumed with them. There is, however, potential for them to also raise the bioavailability of undesirable substances found in these products, such as pesticides. In this research, we studied the impact of excipient nanoemulsions on the bioaccessibility of pesticide-treated tomatoes. We hypothesized that the propensity for nanoemulsions to raise pesticide bioaccessibility would depend on the polarity of the pesticide molecules. Bendiocarb, parathion, and chlorpyrifos were therefore selected because they have Log P values of 1.7, 3.8, and 5.3, respectively. Nanoemulsions with different oil contents (0%, 4%, and 8%) were fabricated to study their impact on pesticide uptake. In the absence of oil, the bioaccessibility increased with increasing pesticide polarity (decreasing Log P): bendiocarb (92.9%) > parathion (16.4%) > chlorpyrifos (2.8%). Bendiocarb bioaccessibility did not depend on the oil content of the nanoemulsions, which was attributed to its relatively high water-solubility. Conversely, the bioaccessibility of the more hydrophobic pesticides (parathion and chlorpyrifos) increased with increasing oil content. For instance, for chlorpyrifos, the bioaccessibility was 2.8%, 47.0%, and 70.7% at 0%, 4%, and 8% oil content, respectively. Our findings have repercussions for the utilization of nanoemulsions as excipient foods in products that may have high levels of undesirable non-polar substances, such as pesticides.

Bioavailability of nutraceuticals: Role of the food matrix, processing conditions, the gastrointestinal tract, and nanodelivery systems.

Nowadays, many consumers prefer foods with a high content of nutraceuticals that contribute to the prevention or healing of chronic diseases. Therefore, in recent years, more and more researchers have studied the bioefficiency, safety, and toxicity of nutraceutical-enriched foods. The key stage of nutraceutical bioefficiency is oral bioavailability, which involves the following processes: the release of nutraceuticals from food matrices or nanocarriers in gastrointestinal fluids, the solubilization of nutraceuticals and their interaction with other components of gastrointestinal fluids, the absorption of nutraceuticals by the epithelial layer, and the chemical and biochemical transformations into epithelial cells. These processes are endogenous factors that greatly influence the bioavailability of nutraceuticals. In addition to endogenous factors, the bioavailability of nutraceuticals is also affected by exogenous factors, such as: physicochemical properties of nutraceuticals, food matrix, food processing and storage, and so forth. Both the endogenous and exogenous factors are comprehensively analyzed in this review. Thus, the physicochemical and enzymatic processes involved in food digestion are described, highlighting the role of each stage of gastrointestinal tract (mouth, stomach, and intestine) in nutraceuticals bioaccessibility. The structure and functions of the mucus and epithelial layers, the mechanisms involved in the active and passive transport of nutraceuticals through the cell membrane, and phase I and phase II metabolism reactions are also discussed. Finally, this review focuses on several types of bioactive-loaded nanocarriers such as lipid-based, surfactant-based, and biopolymeric nanocarriers that improve the bioavailability of nutraceuticals.

Impact of plant extract on the gastrointestinal fate of nutraceutical-loaded nanoemulsions: phytic acid inhibits lipid digestion but enhances curcumin bioaccessibility.

The impact of phytic acid on lipid digestion and curcumin bioaccessibility in oil-in-water nanoemulsions was investigated using a simulated gastrointestinal tract (GIT). The size, charge, and structural organization of the colloidal particles in the system were measured as the curcumin-loaded emulsions (7 mg curcumin per g lipid) were passed through simulated mouth (pH 6.8, 2 min), stomach (pH 2.5, 2 hours), and small intestine (pH 7.0, 2 hours) stages. After the small intestine stage, the level of free fatty acids (FFAs) generated and the bioaccessibility of curcumin were measured. The total amount of FFAs released significantly decreased with increasing phytic acid level, from 105.7 ± 5.9% (control) to 78.4 ± 6.4% (0.5% phytic acid). Conversely, curcumin bioaccessibility significantly increased from 39.4 ± 3.5% (control) to 74.7 ± 2.6% (0.5% phytic acid). The inverse relationship between lipolysis and curcumin bioaccessibility was ascribed to the impact of phytic acid on droplet flocculation and the level of free calcium ions present, which affected the production of mixed micelles capable of solubilizing the nutraceutical. The knowledge obtained here might prove beneficial for the employment of phytic acid as a multifunctional ingredient that inhibits lipid digestion while boosting nutraceutical bioavailability.

The gastrointestinal behavior of emulsifiers used to formulate excipient emulsions impact the bioavailability of β-carotene from spinach

The impact of the type of emulsifier used to formulate excipient emulsions on the degradation (D*) and bioaccessibility (B*) of β-carotene in spinach was investigated using a simulated gastrointestinal tract (GIT). Emulsions stabilized by sodium caseinate (SC) were more prone to droplet aggregation than those stabilized by either Tween 20 or octenyl succinic anhydride (OSA)-modified starch. The fraction of β-carotene available for absorption (D* × B*) was also affected by emulsifier type: SC (12.0%) > Tween 20 (5.0%) ≈ OSA stabilized (2.6%) (p < 0.05). This effect was mainly attributed to differences in the digestive characteristics of the emulsifiers, which affected the transfer efficiency of β-carotene from the plant tissues to the lipid phase, lipid digestion, and mixed micelle formation. These results show the importance of selecting an appropriate emulsifier when designing excipient emulsions to enhance the bioavailability of nutraceuticals in fruits and vegetables.

Pectin and chitosan microparticles as controlled release systems of nutraceuticals

Introduction: The nutraceuticals are nutrients present in natural food with functions of drugs, which may provide health benefits, such as prevention and treatment of diseases. However, when we eat the food, only a small concentration of nutraceuticals is still active. In addition, the residence time gastric and the low permeability in the intestine also lead to the degradation of these bioactive compounds, decreasing the bioavailability of nutraceuticals. With this, several strategies were formulated to isolate and protect these bioactive molecules. Outstanding among them the microencapsulation which consists in the isolation and protection of these molecules from the microparticles obtained polymers; bioactive and biodegradable such as Pectin and Chitosan. Objectives: To analyse from recent studies microparticles of Pectin and Chitosan have a potential significant release of nutraceuticals. Methodology: Were searched for articles that examined the microencapsulacao of nutraceuticals from Pectin and Chitosan, and the effects on the bioavailability of the same. Results and Discussion: The reviewed studies showed a potential release of nutraceuticals significant using microparticles of Pectin and Chitosan. The studies showed the benefits of nutraceuticals in the human organism. The nutraceuticals are found mainly in the form of peptides bioactive, vitamins and antioxidants, and they are of extreme importance in the prevention of chronic diseases such as cancer, cardiovascular diseases and processes associated with aging. In addition, it also showed the feasibility of the use of Pectin and Chitosan as release systems for nutraceuticals. Conclusion: When analyzing the articles, it was possible to conclude that the microparticles have a potential in release significant, with perspective to administration by the oral route, and also with use potential of Pectin and Chitosan as release systems for nutraceuticals and can be used to production of pharmaceuticals and new functional foods.

Designing food structure and composition to enhance nutraceutical bioactivity to support cancer inhibition.

Many types of bioactive molecules found in foods ("nutraceuticals") have been shown to exert anticancer activities, including curcumin, resveratrol, polyphenols, sulforaphane, anthocyanins, genistein, quercetin and lycopene. The potential health benefits of nutraceuticals are often not realized because of their poor water solubility, chemical instability, adverse taste profile, and low oral bioavailability. Carefully designed food matrices are being developed to overcome these problems. Nutraceuticals can be isolated from their natural environment, and then incorporated into functional foods, often with the help of delivery systems (such as emulsions, nanoemulsions, liposomes, biopolymer nanoparticles, and microgels). Alternatively, the stability and bioavailability of nutraceuticals can be improved by leaving them in their natural environment, but ingesting them with a specially designed "excipient food". The structure and composition of an excipient food is controlled so as to enhance the bioaccessibilty, stability, and absorption of the nutraceuticals in the gastrointestinal tract. This review article provides an overview of some of the most important anticancer nutraceuticals found in foods, then highlights the main factors impacting their bioaccessibility, absorption and transformation. Finally, it describes different types of delivery systems and excipient systems that can be used to improve the overall bioavailability of anticancer nutraceuticals.

Photo-protection and controlled release of folic acid using edible alginate/chitosan nanolaminates

The formation, characterization, photo-protective properties and release profiles of folic acid-loaded nanolaminated films were investigated by UV–visible spectroscopy, FTIR, Raman and SEM microscopy. Food-grade alginate/chitosan nanolaminates were obtained by the layer-by-layer technique and folic acid (FA) was incorporated by post-diffusion. The FA concentration of loading solutions and immersion time significantly affected the FA content in nanolaminates. The maximum FA loading was reached using FA solutions at 10 mg/mL for 30 min (54.4 μg/cm2), or 12.5 mg/mL for 120 min (≈70 μg/cm2). Nanolaminates containing FA were more stable under ultraviolet light exposure than non-encapsulated FA. The rate and concentration of FA released from nanolaminates were greater at buffer pH 7 than at pH 3, which might play a key role in the delivery and bioavailability of nutraceuticals. These results provide important information for the design of nanolaminates containing hydrophilic active compounds for food applications.

Potential physicochemical basis of Mediterranean diet effect: Ability of emulsified olive oil to increase carotenoid bioaccessibility in raw and cooked tomatoes

Excipient emulsions have compositions and structures specifically designed to increase the bioavailability of nutraceuticals in foods that they are co-ingested with. In this study, olive oil excipient emulsions were shown to significantly increase the bioaccessibility of carotenoids from tomatoes using a simulated gastrointestinal tract (GIT) model (p<0.05): being 8.18±0.93%, 11.85±1.76% for raw tomato-buffer mixture, and cooked tomato-buffer mixture; While being 32.3±2.60%, 55.7±3.28% and 42.6±3.75% for raw tomato-emulsion mixture, cooked tomato-emulsion mixture (boiled together) and cooked tomato- emulsion mixture (tomato boiled alone). These effects were attributed to: (i) the ability of digested olive oil droplets to form mixed micelles in the small intestine that solubilized the carotenoids; and, (ii) the ability of natural antioxidants (phenolics) in the olive oil to protect the carotenoids from oxidation. Thermal treatment (boiling) significantly increased carotenoid bioaccessibility from the tomatoes digested with emulsion, which was attributed to plant tissue disruption at elevated temperatures facilitating carotenoid release (p<0.05). Carotenoid bioaccessibility was higher when the tomatoes were boiled with emulsions (55.7±3.28%) than when they were boiled alone and then added to emulsions (42.6±3.75%). In conclusion, this study indicates that olive oil emulsions boost the bioaccessibility and chemical stability of lipophilic nutraceuticals in tomatoes, which may make an important contribution to the potential health benefits of the Mediterranean diet.

Enhancing nutraceutical bioavailability by controlling the composition and structure of gastrointestinal contents: Emulsion-based delivery and excipient systems

Abstract The oral bioavailability of hydrophobic bioactives can be improved using food matrices that breakdown within the gastrointestinal tract to form colloidal structures capable of altering bioaccessibility, absorption, and/or transformation. Emulsions are particularly suitable for this purpose because their compositions, structures, and properties can be controlled, and they are already widely used in foods. The bioavailability of isolated bioactives can be improved by incorporating them within emulsion-based delivery systems (EDS), while the bioavailability of bioactives in whole foods can be improved by ingesting them with emulsion-based excipient systems (EES). This review discusses the design, fabrication, and utilization of EDS and EES.

Recent progress in hydrogel delivery systems for improving nutraceutical bioavailability

Nutraceuticals are bioactive molecules found in foods that may improve human performance, wellbeing, or health. The potential health benefits of many nutraceuticals are not fully realized because they are chemically degraded during storage or within the gastrointestinal tract. Consequently, there is a need to develop food-grade delivery systems to encapsulate and protect nutraceuticals until they reach an appropriate location within the human body, e.g., mouth, stomach, small intestine, or colon. Hydrogel beads (“microgels”) assembled from proteins and/or polysaccharides can improve nutraceutical performance by protecting them from chemical degradation. These beads can be fabricated using simple and inexpensive processing operations that typically involve two steps: (i) formation of biopolymer-enriched particles; (ii) cross-linking of the biopolymers. Hydrophilic nutraceuticals are usually mixed directly with the biopolymer solution prior to formation of the hydrogel beads, whereas hydrophobic nutraceuticals are typically incorporated into lipid droplets (emulsions or nanoemulsions) prior to mixing with the biopolymer solution. Common particle-formation methods include injection, shearing, templating, and phase separation, whereas common cross-linking methods include changes in solvent quality, counter-ion addition, enzyme addition, heating, and cooling. This article provides an overview of recent progress in the design and fabrication of food-grade hydrogel beads to encapsulate and protect nutraceuticals, including some examples of their potential applications.