Nutraceutical Delivery Research Articles

The spatial arrangement of astaxanthin in bilayers greatly influenced the structural stability of DPPC liposomes

Liposomes are regarded as the ideal nanocarrier for concurrent or separate delivery of nutraceuticals in the food industries. Precise control of the structural stability is essential for the processing, storage, and nutrition delivery of liposomes. Astaxanthin was found to significantly affect the membrane stability of liposomes by inserting into the phospholipid bilayers in a similar way to cholesterol. Compared with cholesterol, astaxanthin could significantly improve the phase transition temperature, membrane fluidity, and membrane compactness of liposomes. Additionally, the membrane stability was well modulated by controlling the distribution patterns of astaxanthin (monomers, H- and J-aggregates) in bilayers. For instance, astaxanthin H-aggregates could endow the liposomal membrane with highest rigidity and compactness. Additionally, astaxanthin aggregates, especially J-aggregates could greatly improve storage stability of liposomes, thus providing a novel strategy to regulate and optimize the stability of liposomes for their diversified applications.

Application of X-ray Microcomputed Tomography for the Static and Dynamic Characterization of the Microstructure of Oleofoams.

Oleofoams are a novel, versatile, and biocompatible soft material that finds application in drug, cosmetic or nutraceuticals delivery. However, due to their temperature-sensitive and opaque nature, the characterization of oleofoams’ microstructure is challenging. Here, synchrotron X-ray microcomputed tomography and radiography are applied to study the microstructure of a triglyceride-based oleofoam. These techniques enable non-destructive, quantitative, 3D measurements of native samples to determine the thermodynamic and kinetic behavior of oleofoams at different stages of their life cycle. During processing, a constant bubble size distribution is reached after few minutes of shearing, while the number of bubbles incorporated keeps increasing until saturation of the continuous phase. Low amounts of solid triglycerides in oleofoams allow faster aeration and a more homogeneous microstructure but lower thermodynamic stability, with bubble disproportionation and shape relaxation over time. Radiography shows that heating causes Ostwald ripening and coalescence of bubbles, with an increase of their diameter and sphericity.

A CRITICAL REVIEW ON NANOEMULSION: ADVANTAGES, TECHNIQUES AND CHARACTERIZATION

Nanoemulsions have small droplet size and are kinetically stable colloidal systems. These are the thermodynamically stable isotropic system in which two immiscible liquids are mixed to form a single phase by means of appropriate surfactant and cosurfactant. Nanoemulsion droplet sizes fall typically in the range of 20–200 nm and shows narrow size distribution. They have enhanced functional properties in comparison to conventional emulsions. The composition and structure of the nanoemulsions can be controlled for the encapsulation and effective delivery of bioactive lipophilic compounds. Nanoemulsions have potential application in the food industry for the delivery of nutraceuticals, coloring and flavoring agents, and antimicrobials. This review aims to provide consolidated information regarding various formulation and characterization techniques developed for nanoemulsions. Various characterization techniques for nanoemulsions include determination of entrapment efficiency, particle size, polydispersity index, zeta potential as well as characterization through differential scanning calorimetry, Fourier-transform infrared spectroscopy and transmission electron microscopy.

Fabrication and characterization of Pickering high internal phase emulsion stabilized by mung bean flour

Pickering high internal phase emulsion (HIPE) has a broad application prospect in the field of solid fat substitution and nutraceutical delivery, but the safe and available food-derived particle emulsifier is the bottleneck of its practical application. In this study, mung bean flour was used as a particle emulsifier to stabilize oil-in-water Pickering HIPEs. The results showed that the particle size of mung bean flour was suitable (median diameter, 26.41 μm) and had certain wettability. The volume fraction of oil phase (φ) and the concentration of mung bean flour (c) had significant effects on the formation of Pickering HIPEs. When c ≥ 1%, the Pickering HIPE of φ = 80% could be obtained. Mung bean flour not only played an emulsifying role at the oil/water interface, but also prevented the coalescence of oil droplets through its viscosity effect in the aqueous phase. With the increase of c, the droplet size of Pickering HIPEs decreased, the mechanical properties increased gradually, and the ability of HIPEs protecting β-carotene against ultraviolet irradiation was also enhanced.

Tremella polysaccharides-coated zein nanoparticles for enhancing stability and bioaccessibility of curcumin

The purpose of the present research was to examine the ability of Tremella polysaccharide (TP) to stabilize zein nanoparticles (zein NPs) and appraise the performance of zein/Tremella polysaccharide nanoparticles (zein/TP NPs) in terms of encapsulating and delivering curcumin. In this study, the zein/TP NPs were fabricated based on the anti-solvent precipitation method, which were used to protect and deliver curcumin. The results suggested that TP could be deposited on the surface of zein NPs by virtue of electrostatic interaction, so as to improve the hydrophilicity of zein, provide better protection for curcumin and assemble more stable nanoparticles. Compared with zein NPs (54.73%), the zein/TP NPs exhibited higher encapsulation efficiency of curcumin (93.34%) and excellent re-dispersibility. Furthermore, the retention rate of curcumin encapsulated in zein/TP NPs reached 80.78% and 90.74% after UV irradiation and 80 °C heat treatment for 2 h, respectively, which proved that the addition of TP significantly improved the stability of curcumin. Meanwhile, in vitro digestion study demonstrated that the bioaccessibility of curcumin encapsulated in zein/TP NPs increased by 37.36% compared with in zein NPs. Therefore, the zein/TP NPs may be served as an effective and potential carrier for the delivery of nutraceuticals.

Stimuli-responsive polymer-complexed liposome nanocarrier provides controlled release of biomolecules

Smart nanocarriers have recently attracted attention for their effective delivery of biomolecules to the intestine without degradation in the oral delivery field. In this study, we prepared a stimulus-responsive polymer complex containing liposomal nanocarriers, termed capsosomes, and examined their multi-level release properties in the oral delivery of hydrophilic molecules. The capsosomes were constructed as a trilaurin-based solid lipid nanoparticle (SLN) assembly coated with chitosan (CSLNs), with liposomal subcompartments. We investigated the pH sensitivity and behavior of capsosomes in vitro under simulated gastrointestinal (GI) conditions. Positively charged CSLNs with negatively charged liposomal subcompartments were complexed by electrostatic forces, and their thermodynamic characteristics were examined using isothermal titration calorimetry. The optimized formulation was a 1.6 M ratio of liposomes to CSLNs, yielding physically stable capsosomes. The complexed liposomes were released from capsosomes at pH 7.0. We compared the structural integrity and retention times of free liposomes and capsosomes using an in vitro digestion model. The capsosomes showed improved stability and prolonged retention time under small intestinal conditions and bypassed the GI tract. Approximately 87% of the complexed liposomes were released and transferred to the small intestinal membrane. These results demonstrate the potential application of pH-sensitive capsosomes for the oral delivery of food nutraceuticals.

Ultrasonication induced synthesis of TPGS stabilized clove oil nanoemulsions and their synergistic effect against breast cancer cells and harmful bacteria

The present work reports the fabrication of TPGS assisted clove oil in water nanoemulsion for the delivery of polyphenolic nutraceuticals i.e. curcumin and resveratrol and the analysis of their synergetic healing potential. The fabrication procedure was undertaken by the use of high energy ultrasonic cavitation technique. The morphological and rheological properties of the fabricated systems were analyzed and optimized using numerous techniques. The current study throws light on the influence of surfactant type and composition on the mixing stability of oil phase. Both curcumin and resveratrol were effectively loaded in the nanoemulsion, and their loading efficiencies were found to be 99.87 and 99.38%, respectively. The study was undertaken with the aim of exploring the versatile therapeutic potential by elevating the established antimicrobial activity of curcumin and resveratrol and testing their prospects against breast cancer cell lines. The results demonstrated the antimicrobial activity of nanoemulsion (without nutraceuticals) itself against gram-positive and gram-negative bacteria owing to the clove oil which would be an asset in accomplishing better results. In combination with curcumin and resveratrol, it exhibited enhanced effect against different bacterial strains thus showcasing an increase in its efficacy. Furthermore, the anti-tumor activity of prepared formulations has been tested on MDA MB −231 and Hep G2 breast cancer cell lines to broaden the horizons of biological applications of the formulated system.

Polymeric micelles and nanomedicines: Shaping the future of next generation therapeutic strategies for infectious diseases

Despite all the advances in understanding the pathogenesis of infectious diseases and the development of novel treatments to combat them, these pathogenic disorders are among the most common reasons for hospitalizations and death worldwide.Polymeric micelles (PMs) are nano-sized drug delivery systems that in the last few years have raised special attention for optimizing the therapy of many infectious diseases, including those considered as neglected by the World Health Organization. These nanoscopic core/shell structures formed by self-assemblies of amphiphilic block copolymers represent an effective delivery system for poorly water-soluble drugs. In the last few years, many micellar formulations were studied for delivery of drugs, genes and nutraceuticals, and some of them are under clinical trials. This review will focus on the applications of polymeric single and mixed micelles for the treatment of infectious diseases and will discuss how these advancements have contributed to improve their pharmacotherapy, with a special emphasis on neglected tropical diseases. A summary of the nanomaterials used for the preparation of PMs is detailed. The current state of the art of several micellar formulations as nanocarriers of FDA-approved drugs for the therapy of many infectious diseases, including those under pre-clinical or clinical trials is provided. Finally, perspectives in the design of a more efficient pharmacotherapy to overcome the multi-drug resistance phenotype of pathogens or host cells are addressed.

Synthesis and characterization of lotus seed protein-based curcumin microcapsules with enhanced solubility, stability, and sustained release.

Lotus seed protein (LSP) was extracted from lotus seed and used to encapsulate curcumin with or without complexing with pectin. The physicochemical properties of LSP-based microcapsules, including solubility, stability, and in vitro sustained release, were determined. The mechanism of interaction between curcumin, LSP, and pectin was revealed. The encapsulation efficiency of curcumin was found to depend on LSP concentration and was highest (86.32%, w/w) at 50 mg mL-1 . The curcumin in curcumin-LSP and curcumin-LSP-pectin powder particles achieved a solubility of 75.15% and 81.39%, respectively, which was a remarkable enhancement. The microencapsulation with LSP and LSP-pectin matrix showed a significant improvement in the antioxidant activity, photostability, thermostability, and storage stability of free curcumin. The microencapsulated curcumin showed sustained control release at the gastric stage and burst-type release in the subsequent intestinal stage, presenting cumulative release rates of 64.3% and 72.4% from curcumin-LSP and curcumin-LSP-pectin particles after gastrointestinal digestion. The LSP-pectin complex produced microcapsules with higher solubility, smaller particle size, enhanced physicochemical stability, and increased bioaccessibility. Fourier transform infrared, circular dichroism spectra, and differential scanning calorimetry data indicated that the encapsulated curcumin interacted with LSP and pectin mainly through hydrogen bonding, hydrophobic, and electrostatic interactions. This work shows that LSP can be an alternative encapsulant for the delivery of hydrophobic nutraceuticals with enhanced solubility, stability, and sustained release. The results may contribute to the design of novel food-grade delivery systems based on LSP vehicles, thereby broadening the applications of LSP in the fields of functional food. © 2021 Society of Chemical Industry.

Fabrication and characterization of bamboo shoot cellulose/sodium alginate composite aerogels for sustained release of curcumin

The feasibility of using unmodified bamboo shoot cellulose (BSC) to produce composite aerogels with sodium alginate (SA) in a fast and green way for sustained release of curcumin was explored for the first time, in which calcium ion-induced SA cross-linking could effectively retain the structural stability of aerogel skeleton. The aerogels were characterized by scanning electron microscopy, Fourier transform infrared spectroscopy and differential scanning calorimetry. The encapsulation and release of curcumin from aerogels were studied while the antioxidant activity of encapsulated curcumin was investigated. Curcumin was evenly encapsulated in the composite aerogels and showed a sustained release behavior, followed the first-order rate expression. Interpenetrating network structures were built between BSC and SA mainly through hydrogen bonding, which could be further reinforced by the cross-linking of CaCO3 on the SA matrix. The original characteristics of BSC in the composite aerogels were well retained. The thermal stability and mechanical properties of the composite aerogels were improved by Ca2+-induced cross-linking, while the uncross-linked composite aerogels exhibited better encapsulation efficiency and in vitro antioxidant activity. Overall, this study was the first to use cellulose from bamboo shoot to develop aerogels for drug delivery purposes. The cellulose/alginate composite aerogels were promising to be used as biocompatible carriers for drug and nutraceutical delivery.

Nobiletin-loaded composite penetration enhancer vesicles restore the normal miRNA expression and the chief defence antioxidant levels in skin cancer

Skin cancer is one of the most dangerous diseases, leading to massive losses and high death rates worldwide. Topical delivery of nutraceuticals is considered a suitable approach for efficient and safe treatment of skin cancer. Nobiletin; a flavone occurring in citrus fruits has been reported to inhibit proliferation of carcinogenesis since 1990s, is a promising candidate in this regard. Nobiletin was loaded in various vesicular systems to improve its cytotoxicity against skin cancer. Vesicles were prepared using the thin film hydration method, and characterized for particle size, zeta potential, entrapment efficiency, TEM, ex-vivo skin deposition and physical stability. Nobiletin-loaded composite penetration enhancer vesicles (PEVs) and composite transfersomes exhibited particle size 126.70 ± 11.80 nm, 110.10 ± 0.90 nm, zeta potential + 6.10 ± 0.40 mV, + 9.80 ± 2.60 mV, entrapment efficiency 93.50% ± 3.60, 95.60% ± 1.50 and total skin deposition 95.30% ± 3.40, 100.00% ± 2.80, respectively. These formulations were selected for cytotoxicity study on epidermoid carcinoma cell line (A431). Nobiletin-loaded composite PEVs displayed the lowest IC50 value, thus was selected for the in vivo study, where it restored skin condition in DMBA induced skin carcinogenesis mice, as delineated by histological and immuno-histochemical analysis, biochemical assessment of skin oxidative stress biomarkers, in addition to miRNA21 and miRNA29A. The outcomes confirmed that nobiletin- loaded composite PEVs is an efficient delivery system combating skin cancer.

One-step preparation of double emulsions stabilized with amphiphilic and stimuli-responsive block copolymers and nanoparticles for nutraceuticals and drug delivery

One-step emulsification approaches enable prevention of the loss of emulsion droplets associated with two-step emulsification approaches. Stimuli-responsive amphiphilic block copolymers, emulsifiers, and nanoparticles that are responsive to changes in the temperature, pH, presence of CO 2 , or presence of salts, can eliminate the requirement for two hydrophilic and lipophilic emulsifiers in the emulsion system. The amphiphilic block copolymers prepared from naturally occurring amino acids and proteins enable targeted delivery of drugs and nutraceuticals with high cellular uptake. Likewise, the presence of impurities, such as salts and redox reactions driven by the presence of iodine, can result in spontaneous emulsification and formation of double emulsions. This timely review focuses on the application of double emulsions for delivery of drugs and nutraceuticals and will provide insights to scientists in the pharmaceutical industry or food nutritionists who consider fortification of food products with micronutrients. • One-step preparation of double emulsions can prevent the loss of internal emulsion droplets during processing. • Stabilization of double emulsions with amphiphilic copolymers can prevent the need for two various emulsifiers. • The stimuli-responsive copolymers can enable encapsulation and controlled release of nutraceuticals and drugs. • Hydrophilicity or lipophilicity of block copolymers can be tuned by adjusting the length of blocks and oil composition.

Alginate-based delivery systems for food bioactive ingredients: An overview of recent advances and future trends.

Due to its advantagessuch as ionic crosslinking, pH responsiveness, excellent biocompatibility, biodegradability and low price, alginate has become one of the most important natural polysaccharides extensively used in constructing desired delivery systems for food bioactive ingredients. In this review, the fundamental knowledge of alginate as a building block for construction of nutraceutical delivery systems is introduced. Then, various types of alginate-based nutraceutical delivery systems are classified and summarized. Furthermore, the future trends of alginate-based delivery systems are highlighted. Currently, alginate-based delivery systems include hydrogel, emulsion, emulsion-filled alginate hydrogel, nanoparticle, microparticle, core-shell particle, liposome, edible film, and aerogel. Although alginate has been widely used in the fabrication of food bioactive ingredient delivery systems, further efforts and improvements are still needed. For this purpose, the future perspectives of alginate-based delivery systems are discussed. The feasible research trends of alginate-based delivery systems include the development of novel large-scale commercial preparation technology, multifunctional delivery system based on alginate, alginate oligosaccharide-based delivery system and alginate-based oleogel. Overall, the objective of this review is to provide useful guidance for rational design and application of alginate-based nutraceutical delivery systems in the future.

A Critical Reveiw on Nanoemulsion: Advantages, techniques and characterization

Nanoemulsions have small droplet size and are kinetically stable colloidal systems. These are the thermodynamically stable isotropic system in which two immiscible liquids are mixed to form a single phase by means of appropriate surfactant and co-surfactant. Nanoemulsion droplet sizes fall typically in the range of 20-200 nm and shows narrow size distribution. They have enhanced functional properties in comparison to conventional emulsions. The composition and structure of the nanoemulsions can be controlled for the encapsulation and effective delivery of bioactive lipophilic compounds. Nanoemulsions have potential application in the food industry for the delivery of nutraceuticals, coloring and flavoring agents, and antimicrobials. This review aims to provide consolidated information regarding various formulation and characterization techniques developed for nanoemulsions. Various characterization techniques for nanoemulsions include determination of entrapment efficiency, particle size, polydispersity index, zeta potential as well as characterization through differential scanning calorimetry, Fourier-transform infrared spectroscopy and transmission electron microscopy.

Preparation and characterization of β‐carotene nanoemulsions stabilized by complexes of tartary buckwheat bran protein and rutin

Tartary buckwheat bran (TBB), which is rich in proteins, is the main waste of tartary buckwheat processing. To improve the value of TBB, the noncovalent and covalent Tartary buckwheat bran protein (TBBP)/rutin complexes were prepared, and their capacities to fabricate β-carotene nanoemulsions were compared. The results indicated that the covalent complex exhibited the highest emulsifying performance, and the corresponding nanoemulsion had the lowest droplet size and polymer dispersity index (PDI) and the highest absolute value of ζ-potential, which could remain stable for four weeks. The high–temperature–short–time treatment and freeze–thaw processing had little influence on this nanoemulsion. However, it was very sensitive to high salt concentrations. Compared with the nanoemulsion prepared by the noncovalent complex, it had higher protein and rutin concentrations at the oil-water interface, which explained the improved stability of β-carotene against high temperature and UV irradiation. Practical applications In this study, the fabrication and characterization of β-carotene nanoemulsion stabilized by the complexes of tartary buckwheat bran protein and rutin are introduced. It can provide a reference for the utilization of other low-value cereal proteins and prompt the development of nutraceutical delivery systems based on food-derived protein-polyphenol complexes.

Modification of Kutki millet (Panicum sumatrense) starch properties by the addition of amino acids for the preparation of hydrogels and its characterization

Starch is a biopolymer containing hydrophilic groups and is used in hydrogels preparation. Amino acids are multifunctional monomers of proteins that can be used as a cross linker to modify the starch by incorporating new functional groups into its chains. In this study, the Kutki millet starch was isolated and modified with lysine (positively charged), aspartic acid (negatively charged), and threonine (neutral) at varying pH levels. These modified starches were characterized for their various functional, structural, pasting, and textural properties. Hydrogels prepared from Lys9-KMS, Thr9-KMS, and AA11-KMS, possessing less adhesiveness, strong integrity, and hardness were then characterized for their XRD and morphological characterization. The principal component analysis (PCA) biplot showed that the samples modified at higher pH levels are positively correlated with the textural properties, swelling power and amylose content (I and IV quadrants), than those modified at lower pH. It may be inferred that starch modified with amino acid at higher pH have good textural properties than those at lower pH. Results of the overall investigation indicated that among these three amino acids, lysine could be a better cross linker for modification of Kutki millet starch and preparation of their gels for the delivery of nutraceuticals.

Development and evaluation of a novel nanofibersolosome for enhancing the stability, in vitro bioaccessibility, and colonic delivery of cyanidin-3-O-glucoside

The development of colon-specific carrier systems using polysaccharides for oral delivery of nutraceuticals is of great importance for the treatment and/or prevention of inflammatory bowel diseases. In this study, self-assembly with the assistance of vortexing and pulsed-ultrasonication was employed to develop a Fibersol®-2 (a digestion-resistant polysaccharide) and lipoid S75 based novel nanocarrier (denoted as nanofibersolosome) for the colonic delivery of cyanidin-3-O-glucoside (C3G). A series of nanofibersolosome formulations (CFS-0.5–4, 0.5–4 represent the ratios of Fibersol®-2:lipoid S75) were developed and their performance was compared with Fibersol®-2-free reference lipid formulation (CFS-0). The nanofibersolosomes (<150 nm) were spherical and unilamellar with high negative surface charge (−38 to −51 mV) and good encapsulation efficiency (EE > 90%). They performed much better than CFS-0 in retaining their physical properties during freeze drying, preventing particle aggregation, and retaining C3G during storage (4 and 25 ℃) and thermal treatments (40, 60, and 80 ℃). They also exhibited significantly higher stability during simulated gastrointestinal digestion than CFS-0. These desirable features of the nanofibersolosomes (especially CFS-0.5 and CFS-1) led to the efficient delivery of higher concentrations of C3G to the colon than CFS-0. Moreover, gastrointestinal-digested and colonic-fermented nanofibersolosome samples exhibited significantly higher DPPH radical scavenging activity and stronger promoting effect on short-chain fatty acid generation than CFS-0. These in vitro findings indicate that the novel nanofibersolosome possesses great potential for the colonic delivery of C3G and likely other hydrophilic labile phytochemicals that merits further evaluation in in vivo models.

Lipid-Based Nanocarrier System for the Effective Delivery of Nutraceuticals.

Nutraceuticals possess several health benefits and functions; however, most nutraceuticals are prone to degradation in the gastrointestinal environment and have poor bioavailability. Application of a novel carrier system is of increasing importance to overcome obstacles and provide efficient applicability. Lipid-based nanocarriers provide a large surface-to-mass ratio, enhanced intestinal absorption by solubilization in the intestinal milieu, intestinal lymphatic transport, and altering enterocyte-based transport. A critical overview of the current limitation, preparation, and application of lipid-based nanocarriers (liposomes and niosomes) and lipid nanoparticles (SLNs and NLCs) is discussed. Physical and gastrointestinal stability and bioavailability of nanoencapsulated nutraceuticals are considered as well.

Exploration of the Microstructure and Rheological Properties of Sodium Alginate-Pectin-Whey Protein Isolate Stabilized Β-Carotene Emulsions: To Improve Stability and Achieve Gastrointestinal Sustained Release.

Sodium alginate (SA)-pectin (PEC)-whey protein isolate (WPI) complexes were used as an emulsifier to prepare β-carotene emulsions, and the encapsulation efficiency for β-carotene was up to 93.08%. The confocal laser scanning microscope (CLSM) and scanning electron microscope (SEM) images showed that the SA-PEC-WPI emulsion had a compact network structure. The SA-PEC-WPI emulsion exhibited shear-thinning behavior and was in a semi-dilute or weak network state. The SA-PEC-WPI stabilized β-carotene emulsion had better thermal, physical and chemical stability. A small amount of β-carotene (19.46 ± 1.33%) was released from SA-PEC-WPI stabilized β-carotene emulsion in simulated gastric digestion, while a large amount of β-carotene (90.33 ± 1.58%) was released in simulated intestinal digestion. Fourier transform infrared (FTIR) experiments indicated that the formation of SA-PEC-WPI stabilized β-carotene emulsion was attributed to the electrostatic and hydrogen bonding interactions between WPI and SA or PEC, and the hydrophobic interactions between β-carotene and WPI. These results can facilitate the design of polysaccharide-protein stabilized emulsions with high encapsulation efficiency and stability for nutraceutical delivery in food and supplement products.

Technological Potential of a Lupin Protein Concentrate as a Nutraceutical Delivery System in Baked Cookies.

Previous reports have shown that lupin protein extracts (LE) contain a polypeptide named deflamin with a potent matrix metalloproteinase (MMP)-9 inhibitory activity. The aim of our study was to develop an efficient delivery method for incorporating deflamin into cookies using different alternative flours. A lupin protein concentrate (10 g protein/100 g cookie dough) was added to gluten and gluten-free flours to produce savoury cookies, and its impacts on the physical properties of doughs and cookies, as well on the maintenance of deflamin’s anti-MMP-9 activity, were analysed. The results showed that the biochemical compositions of all cookies with LE presented higher protein and ash contents when compared to the control cookies. Rice, buckwheat and oat doughs were firmer than the others, whereas the addition of LE to kamut and buckwheat flours made cookies significantly firmer than the controls. Additionally, strong interactions between LE and several flours were observed, yielding different impacts on the MMP-9 bioactivity. Overall, the only flour that did not interfere with the desired nutraceutical activities was buckwheat, with 60% MMP-9 inhibitory activity and a concomitant reduction of colon cancer migration; hence, buckwheat flour was revealed to be a good vehicle to deliver bioactive deflamin, showing strong potential as a functional food to be used in preventive or curative approaches to gastrointestinal diseases.