Nutraceutical Delivery Research Articles

Development of novel pea protein-based nanoemulsions for delivery of nutraceuticals.

A novel pea protein-based emulsifier was used in the production of oil in water (O/W) nanoemulsions. The regions of kinetically stabilized O/W emulsions were individuated in a pseudoternary diagram containing different pea protein, sunflower oil, and water fractions. The stable O/W emulsion region was widened by the addition of NaCl to the aqueous phase or, to a more significant extent, by high pressure homogenization (HPH) processing. The HPH treatment caused the formation of very fine emulsions in the nanometric range (<200 nm), with extremely high stability over time. HPH treatment affected the protein properties, resulting in a reduced water surface tension. Changes in protein structure, which were characterized by light scattering and SDS-PAGE, suggest the occurrence of the disruption of disulfide bonds, thus changing the exposition and availability of hydrophobic groups.

In Vitro Study of the Release Properties of Soy−Zein Protein Microspheres with a Dynamic Artificial Digestive System

The purpose of this work was to study the performance of microspheres of soy protein isolate (SPI), zein, or SPI-zein complex as vehicles of nutraceutical delivery under fasting and prandial conditions in an artificial digestive system (TIM-1). Riboflavin availability for absorption from the small intestine compartments reached 90% of the total load within 4 h, most of it (65-80%) turning up in the jejunum dialysis fluid, suggesting that this segment is the main site of absorption, regardless of the nature of the microspheres. However, the riboflavin concentrations and the availability for absorption profiles depended on microsphere formulation. Release from pure SPI and zein microspheres in the stomach compartment occurred within 15 min. The availability for absorption from both the jejunum and ileum compartment followed first-order kinetics, indicating that the limiting step in nutrient uptake with these two formulations is absorption by passive diffusion. SPI-zein complex microspheres provided sustained release of riboflavin over 4 h and a near-zero-order nutrient availability for absorption profile in both fasting and prandial states. Suspending SPI-zein complex microspheres in yogurt significantly delayed nutrient release, which would increase the likelihood of gastric-sensitive nutrients passing intact into the intestine for absorption. SPI-zein complex microspheres thus show potential for use as nutraceutical delivery vehicles in the creation of novel functional foods.

Bioavailability and Delivery of Nutraceuticals Using Nanotechnology

Nanotechnology is an enable technology that has the potential to revolutionize agriculture and food systems. Driven by increasing consumer demand for healthy food products, researchers have been applying tools and knowledge in nanotechnology to address the issues relevant to food and nutrition. This concise review is mainly focused on nanoemulsions and polymer micelles-based delivery systems which have shown enhanced oral bioavailability and biological efficacies (that is, antiinflammation, anti-cancer, and so on) of different phytochemicals. Nanoemulsions are a class of extremely small droplets that appear to be transparent or translucent with a bluish coloration. They are usually in the range 50 to 200 nm but much smaller than the range (from 1 to 100 mum) for conventional emulsions. Nanoemulsion preparation, characterization, and bioavailability have been discussed. Curcumin nanoemulsions show 85% inhibition of TPA-induced mouse ear inflammation as well as the inhibition of cyclin D1 expression, while dibenzoylmethane (DBM) nanoemulsion shows about 3-fold increase in oral bioavailability compared to the conventional DBM emulsion. Biopolymer micelles show significantly improved water solubility/dispersibility and in vitro anti-cancer activity of phytochemicals. More research efforts are still needed for the understanding of the potential impacts of nanoencapsulated phytochemicals on the human body and environment to address the public concerns.

Elaboration and Characterization of Soy/Zein Protein Microspheres for Controlled Nutraceutical Delivery

Microspheres (15-25 microm) of soy protein isolate (SPI), zein, and SPI/zein blends were prepared using a cold gelation method as possible delivery systems for nutraceutical products. Microsphere matrix crystalline structure, swelling behavior, and nutrient load release kinetics in simulated gastrointestinal fluids were investigated. SPI microspheres showed early burst release of the model nutrient, whereas zein microspheres showed very slow release in both simulated gastric and intestinal fluids. Blending of SPI and zein provides a convenient method of adjusting the hydrophobicity and crystallinity of the protein matrix and hence its swelling behavior and in vivo nutrient release kinetics. Diffusion plays a major role in regulating nutrient release. SPI/zein microspheres blended at ratios of 5:5 and 3:7 showed near zero-order release kinetics over the test period in simulated intestinal buffer and thus have potential as delivery vehicles for nutraceutical products in functional foods.

Formation and Characterization of Ordered Bicontinuous Microemulsions

Ordered bicontinuous microstructures formed in a fully water-dilutable, pseudoternary unique nonionic microemulsion were obtained and characterized. The concentrate contained a mixture of triacetin/d-alpha-tocopherol acetate/ethanol/Tween 60. Upon dilution, the concentrate was transformed from a reversed micellar system to oil-in-water microemulsion droplets. The transformation occurred through an intermediate phase of ordered bicontinuous structures. The factors that governed the construction of this unique phase, and its physical and structural properties, were characterized in detail. The techniques used included small angle X-ray scattering (SAXS), self-diffusion and quantum filtered NMR, differential scanning calorimetry, rheology measurements, electrical conductivity, and dynamic light scattering. This mesophase displays microemulsion properties along with some characteristics of lyotropic liquid crystals (but is not a mixture of the two). Similar to microemulsions, the structures were transparent and spontaneously formed and exhibited thermodynamic stability. Yet, unlike microemulsions, they showed short-range order at room temperature. Additionally, the microstructures exhibited non-Newtonian flow behavior, characteristic of lamellar structures. The bicontinuous ordered microemulsions were obtained upon heating (to 25 degrees C) from the lamellar phase existing at low temperatures (5 degrees C). The main feature governing the bicontinuous mesophase formation was the amphiphilic nature of oil blends composed of d-alpha-tocopherol acetate and triacetin. The oils functioned as cosurfactants, altering the packing parameter of the surfactant and leading to the construction of bicontinuous structures with short-range order. These unique structures might have drug or nutraceutical delivery advantages.

Manufacture of food grade κ-carrageenan microspheres

The objective of this study was to optimise a method for the manufacture of food-grade κ-carrageenan based microgels with a broad range of functionalities such as nutraceutical delivery systems or fat replacers. In order to obtain small and spherical microgels which would not adversely affect the overall mouthfeel or sensory properties of a food product, a special procedure was optimised based on the emulsification of the κ-carrageenan solution in hot rapeseed oil using a high shear rotor–stator mixer, without the aid of surfactants, followed by fast tempering of the emulsion under mild agitation. The influence of emulsion mixing speed, phase volume ratio, oil and aqueous phase viscosity as well as emulsion temperature, on the particle size and size distribution of the spherical microgels was examined. Results show that best operating conditions for a 4% κ-carrageenan solution are a temperature of 68 °C, a phase volume ratio of 5% and a mixing speed above 3000 rpm. Under these optimised conditions, food grade spherical κ-carrageenan microgels were obtained with a Sauter mean diameter (D[3,2] μm) of 25 μm.

Influence of chitosan on stability and lipase digestibility of lecithin-stabilized tuna oil-in-water emulsions

The influence of chitosan concentration (0–0.3 wt%) and molecular weight (120, 250 and 342.5 kDa) on the physical stability and lipase digestibility of lecithin-stabilized tuna oil-in-water emulsions was studied. The ζ-potential, droplet size, creaming stability, free fatty acids and glucosamine released was measured for the emulsions when they were subjected to an in vitro digestion model. The ζ-potential of the oil droplets in lecithin-chitosan stabilized emulsions changed from positive (≈+53 mV) to negative and the emulsions were unstable to droplet aggregation for all chitosan concentrations and molecular weights used after being subjected to the digestion model. The amount of free fatty acid and glucosamine released per unit amount of emulsion was higher when pancreatic lipase was included in the digestion model. These results suggest that lecithin-chitosan coated droplets can be degraded by lipase under simulated gastrointestinal conditions. Consequently, chitosan coated lipid droplets may serve as useful carriers for the delivery of bioactive lipophilic nutraceuticals.

Continuous dual feed homogenization for the production of starch inclusion complexes for controlled release of nutrients

The use of food grade biopolymers, such as starch, has been suggested as a technological solution for the controlled delivery of health promoting ingredients. This staple food carbohydrate may form molecular inclusion complexes, termed V-amylose, with numerous ligands. This study aimed to develop and assess a continuous production process for the formation of such complexes using three starches varying in the amylose:amylopectin ratio. The heart of the technique is the use of dual feed homogenizer for in situ complexation in accord with homogenization, to form micron and sub micron particles. Results show that pre-dissolving high amylose corn starch or corn starch in a hot alkali solution leads to the formation of a bi-modal population of 0.04–20 μm or a mixed population of 0.04–3 μm V-type particles, respectively. These stearic acid-loaded particles exhibit V-type X-ray diffraction and release the stearic acid mainly upon pancreatic amylases treatment. This technology could prospectively be used in numerous applications including as a delivery system for the controlled delivery of bioactives. Introduction of nutraceuticals and bioactive nutrients into foods is a major technological challenge since many of these compounds have low chemical stability during product processing, storage and consumption. One of the industrial approaches to overcome this drawback is the use of encapsulation technologies, mainly with cheap, common and safe food ingredients. This study describes a unique continuous process to exploit starches’ natural and spontaneous tendency to form single helical molecular inclusion complexes, termed V-amylose, as a possible platform for nano and micro-encapsulation. This process involves coupling pH titration, which induces complexation, to a pressurized homogenization which induces rapid complexation and particle size reduction. Thus, it is suggested to help overcome the main drawbacks of current batch processing, i.e. large particle size, particle aggregation and prolonged duration of production. Additionally, the continuity of the process offers the technological possibility of incorporating the process in existing industrial settings of continuous manufacturing. These molecular inclusion complexes could prospectively be used in a wide variety of applications in the food, pharmaceutical and biotechnology industries including as a delivery system for the controlled and targeted delivery of nutrients, nutraceuticals and/or drugs to the lower gastrointestinal tract.

Neurologic disease and vitamin B12 deficiency

Nutraceuticals or functional foods are foods that provide both health benefits to reduce the risk of chronic diseases and basic nutrition. Examples of nutraceuticals are natural foods, including antioxidants, dietary supplements, fortified dairy products, and citrus fruits, and vitamins, minerals, herbals, milk, and cereals. To enhance the efficacy of nutraceuticals, delivery systems are greatly needed to protect nutraceuticals from the harsh conditions of the gastrointestinal (GI) tract. Drug delivery systems using nanotechnology, such as biocompatible polymers, hold promise for the field of pharmaceutical science, as they offer tools and nanostructured materials that deliver therapeutic drugs for treating diseases successfully. Like drug delivery systems, several delivery systems have been designed for nutraceutical delivery, including smart polymers that are stimuli responsive. This chapter will mostly focus on the characteristics of nutraceuticals and discuss strategic designs of nutraceutical delivery systems.

Casein micelle as a natural nano-capsular vehicle for nutraceuticals

Casein micelles (CM) are in effect nano-capsules created by nature to deliver nutrients, such as calcium, phosphate and protein, to the neonate. A novel approach is herein presented, to harness CM, for nano-encapsulation and stabilization of hydrophobic nutraceutical substances for enrichment of non-fat or low-fat food products. Such nano-capsules may be incorporated in dairy products without modifying their sensory properties. This study introduces new possibilities for encapsulation and delivery of sensitive health-promoting substances using natural GRAS (generally regarded as safe) ingredients. As a model hydrophobic nutraceutical compound we studied the fat-soluble vitamin D2, which is essential for calcium metabolism. A protocol for incorporation of vitamin D2 into CM was established. The encapsulation process was evaluated, and so was the protective effect of the micelles against photochemical degradation of the vitamin. We have demonstrated, for the first time, the possibility to load a nutraceutical compound into CM, utilizing the natural self-assembly tendency of bovine caseins. The vitamin was about 5.5 times more concentrated within the micelles than in the serum where it was only present bound to residual soluble caseins. Moreover, the morphology and average diameter of the re-assembled micelles were similar to those of naturally occurring CM. We have also demonstrated that the re-assembled CM can provide partial protection against UV-light-induced degradation to vitamin D2 contained in them. This study suggests that CM may be useful as nano-vehicles for entrapment, protection and delivery of sensitive hydrophobic nutraceuticals within food products.

A transgenic rice seed accumulating an anti-hypertensive peptide reduces the blood pressure of spontaneously hypertensive rats

RPLKPW is a potent anti-hypertensive peptide designed according to the structure of ovokinin(2–7) (RADHPF). In this study, we generated transgenic rice plants that accumulate the RPLKPW peptide as a fusion protein with the rice storage protein glutelin. The engineered peptide is expressed under the control of endosperm-specific glutelin promoters and specifically accumulates in seeds. Oral administration of either the RPLKPW-glutelin fraction or transgenic rice seeds to spontaneously hypertensive rats (SHRs) significantly reduced systolic blood pressures. These results suggest the possible application of transgenic rice seed as a nutraceutical delivery system and specifically for administration of active peptides in hypertension.

Food protein-based materials as nutraceutical delivery systems

Abstract Incorporation of bioactive compounds–such as vitamins, probiotics, bioactive peptides, and antioxidants etc.–into food systems provide a simple way to develop novel functional foods that may have physiological benefits or reduce the risks of diseases. As a vital macronutrient in food, proteins possess unique functional properties including their ability to form gels and emulsions, which allow them to be an ideal material for the encapsulation of bioactive compounds. Based on the knowledge of protein physical–chemistry properties, this review describes the potential role of food proteins as substrate for the development of nutraceutical delivery systems in the form of hydrogel, micro-, or nano- particles. Applications of these food protein matrices to protect and delivery-sensitive nutraceutical compounds are illustrated, and the impacts of particle size on release properties are emphasized.

Dynamics of concentrated colloidal suspensions: diffusion, aggregation and gelation

We show that diffusing wave spectroscopy (DWS) permits the characterization of dynamic properties of concentrated colloidal suspensions on a large range of time– and length–scales ranging from a few angstroms to tens of nanometres. We focus in particular on the study of the aggregation and sol–gel transition in concentrated colloidal suspensions. We present a new technique to overcome the problem of nonergodicity in DWS of solid–like systems. Using this technique we obtain quantitative information about the microscopic dynamics all the way from an aggregating suspension to the final gel, thereby covering the whole sol–gel transition. At the gel point a dramatic change of the particle dynamics from diffusion to a subdiffusive arrested motion is observed. We combine DWS with small–angle neutron scattering and demonstrate that we can obtain an in situ characterization of the changes in the microstructure and the local particle dynamics as the system undergoes a sol–gel transition.