Ruojie Zhang

Influence of lipid type on gastrointestinal fate of oil-in-water emulsions: In vitro digestion study

The potential gastrointestinal fate of oil-in-water emulsions containing lipid phases from different sources was examined: vegetable oils (corn, olive, sunflower, and canola oil); marine oils (fish and krill oil); flavor oils (orange and lemon oil); and, medium chain triglycerides (MCT). The lowest rates and extents of lipid digestion were observed for emulsified flavor oil, followed by emulsified krill oil. There was no appreciable difference between the final amounts of free fatty acids released for emulsified digestible oils. Differences in the digestibility of emulsions prepared using different oils were attributed to differences in their compositions, e.g., fatty acid chain length and unsaturation. The particle size distribution, particle charge, microstructure, and macroscopic appearance of the emulsions during passage through the simulated GIT depended on oil type. The results of this study may facilitate the design of functional foods that control the digestion and absorption of triglycerides, as well as the bioaccessibility of hydrophobic bioactives.

Enhancing Nutraceutical Performance Using Excipient Foods: Designing Food Structures and Compositions to Increase Bioavailability

The oral bioavailability of many bioactives (pharmaceuticals, dietary supplements, nutrients, and nutraceuticals) is limited because of physicochemical and physiological events that occur within the gastrointestinal tract (GIT) after their ingestion. These events include: (i) restricted liberation from drugs, supplements, or foods; (ii) extensive metabolism or chemical transformation during passage through the GIT; (iii) low solubility in intestinal fluids; (iv) low permeation through the intestinal cell monolayer; and (v) efflux from epithelium cells. Bioactive bioavailability can often be improved by designing the composition and structure of food matrices to control their liberation, transformation, solubilization, transport, absorption, and efflux in the GIT. This article reviews the potential impact of food composition and structure on the oral bioavailability of bioactives, and then shows how this knowledge can be used to design excipient foods that can improve the bioavailability profile of bioactives. The bioactive may be incorporated within an excipient food or co-ingested with an excipient food. The suitability of oil-in-water emulsions as excipient foods is highlighted. The utilization of excipient foods may provide a new strategy for improving the efficacy of nutraceuticals, supplements, and pharmaceuticals.

Encapsulation of lactase (β-galactosidase) into κ-carrageenan-based hydrogel beads: Impact of environmental conditions on enzyme activity.

Encapsulation of enzymes in hydrogel beads may improve their utilization and activity in foods. In this study, the potential of carrageenan hydrogel beads for encapsulating β-galactosidase was investigated. Hydrogel beads were fabricated by injecting an aqueous solution, containing β-galactosidase (26 U) and carrageenan (1 wt%), into a hardening solution (5% potassium chloride). Around 63% of the β-galactosidase was initially encapsulated in the hydrogel beads. Encapsulated β-galactosidase had a higher activity than that of the free enzyme over a range of pH and thermal conditions, which was attributed to the stabilization of the enzyme structure by K(+) ions within the carrageenan beads. Release of the enzyme from the beads was observed during storage in aqueous solutions, which was attributed to the relatively large pore size of the hydrogel matrix. Our results suggest that carrageenan hydrogel beads may be useful encapsulation systems, but further work is needed to inhibit enzyme leakage.

Food-grade nanoparticles for encapsulation, protection and delivery of curcumin: comparison of lipid, protein, and phospholipid nanoparticles under simulated gastrointestinal conditions

The potential of three nanoparticle-based delivery systems to improve curcumin bioavailability was investigated: lipid nPs (nanoemulsions); protein nPs (zein nanosuspensions); and, phospholipid nPs (nanoliposomes). All three nanoparticle types were fabricated from food-grade constituents, had small mean diameters (d phospholipid nPs) and to increase their solubilization within intestinal fluids (lipid nPs > phospholipid nPs > protein nPs). This latter effect was attributed to the enhanced solubilization capacity of the mixed micelle phase formed after digestion of the lipid nanoparticles. Overall, the lipid nanoparticles (nanoemulsions) appeared to be the most effective at increasing the amount of curcumin available for absorption (at an equal initial curcumin level). This study shows that different types of nanoparticles have different advantages and disadvantages for encapsulating, protecting, and releasing curcumin. This research will facilitate the rational selection of food-grade colloidal delivery systems designed to enhance the oral bioavailability of hydrophobic nutraceuticals.

Enhancing Nutraceutical Bioavailability from Raw and Cooked Vegetables Using Excipient Emulsions: Influence of Lipid Type on Carotenoid Bioaccessibility from Carrots

The influence of the nature of the lipid phase in excipient emulsions on the bioaccessibility and transformation of carotenoid from carrots was investigated using a gastrointestinal tract (GIT) model. Excipient emulsions were fabricated using whey protein as an emulsifier and medium-chain triglycerides (MCT), fish oil, or corn oil as the oil phase. Changes in particle size, charge, and microstructure were measured as the carrot-emulsion mixtures were passed through simulated mouth, stomach, and small intestine regions. Carotenoid bioaccessibility depended on the type of lipids used to form the excipient emulsions (corn oil > fish oil ≫ MCT), which was attributed to differences in the solubilization capacity of mixed micelles formed from different lipid digestion products. The transformation of carotenoids was greater for fish oil and corn oil than for MCT, which may have been due to greater oxidation or isomerization. The bioaccessibility of the carotenoids was higher from boiled than raw carrots, which was attributed to greater disruption of the plant tissue facilitating carotenoid release. In conclusion, excipient emulsions are highly effective at increasing carotenoid bioaccessibility from carrots, but lipid type must be optimized to ensure high efficacy.

Boosting the bioavailability of hydrophobic nutrients, vitamins, and nutraceuticals in natural products using excipient emulsions

Many highly hydrophobic bioactives, such as non-polar nutrients, nutraceuticals, and vitamins, have a relatively low or variable oral bioavailability. The poor bioavailability profile of these bioactives may be due to limited bioaccessibility, poor absorption, and/or chemical transformation within the gastrointestinal tract (GIT). The bioavailability of hydrophobic bioactives can be improved using specially designed oil-in-water emulsions consisting of lipid droplets dispersed within an aqueous phase. The bioactives may be isolated from their natural environment and then incorporated into the lipid phase of emulsion-based delivery systems. Alternatively, the bioactives may be left in their natural environment (e.g., fruits or vegetables), and then ingested with emulsion-based excipient systems. An excipient emulsion may have no inherent health benefits itself, but it boosts the biological activity of bioactive ingredients co-ingested with it by altering their bioaccessibility, absorption, and/or chemical transformation. This review discusses the design and fabrication of excipient emulsions, and gives some examples of recent research that demonstrates their potential efficacy for improving the bioavailability of hydrophobic bioactives. The concept of excipient emulsions could be used to formulate emulsion-based food products (such as excipient sauces, dressings, dips, creams, or yogurts) specifically designed to increase the bioavailability of bioactive agents in natural foods, such as fruits and vegetables.

Encapsulation of Pancreatic Lipase in Hydrogel Beads with Self-Regulating Internal pH Microenvironments: Retention of Lipase Activity after Exposure to Gastric Conditions

Oral delivery of lipase is important for individuals with exocrine pancreatic insufficiency; however, lipase loses activity when exposed to the highly acidic gastric environment. In this study, pancreatic lipase was encapsulated in hydrogel beads fabricated from alginate (gel former), calcium chloride (cross-linker), and magnesium hydroxide (buffer). Fluorescence confocal microscopy imaging was used to map the pH microclimate within the hydrogel beads under simulated gastrointestinal tract (GIT) conditions. The pH within buffer-free beads rapidly decreased when they moved from mouth (pH 6.3) to stomach (pH <4), leading to a loss of lipase activity in the small intestine. Conversely, the pH inside buffer-loaded beads remained close to neutral in the mouth (pH 7.33) and stomach (pH 7.39), leading to retention of lipase activity in the small intestine, as shown by pH-stat analysis of lipid digestion. The presence of the encapsulated buffer also reduced bead shrinkage under gastric conditions.

Controlling the potential gastrointestinal fate of β-carotene emulsions using interfacial engineering: Impact of coating lipid droplets with polyphenol-protein-carbohydrate conjugate

The impact of interfacial coatings comprised of polyphenol-protein-carbohydrate conjugates on the properties of nutraceutical-fortified lipid droplets during digestion was investigated. Surface-active chlorogenic acid-lactoferrin-polydextrose (CA-LF-PD) conjugate was synthesized as emulsifier to stabilize lipid droplets in β-carotene-enriched oil-in-water emulsions. Changes in droplet size, charge, and microstructure were monitored as β-carotene emulsions were passed through a simulated gastrointestinal tract model (mouth, stomach, small intestine). LF-coated droplets were unstable to flocculation at pH 8.0-9.0, due to the reduction in electrostatic repulsion, but CA-LF-PD conjugate-coated droplets were stable. Emulsions stabilized by ternary conjugate had better stability to droplet aggregation under simulated GIT conditions than other systems, which increased β-carotene bioaccessibility. The importance of including an oral phase in the simulated GIT model was also demonstrated. The ternary conjugate-stabilized emulsions developed in this study have potential applications as protectors and carriers of hydrophobic drugs, supplements and nutraceuticals.

Tailoring lipid digestion profiles using combined delivery systems: mixtures of nanoemulsions and filled hydrogel beads

There is considerable interest within the food and pharmaceutical industries in controlling the rate of lipid digestion within the gastrointestinal tract (GIT) to create functional foods with particular physiological effects. In this study, the lipid digestion profile was modulated using mixed colloidal delivery systems containing a mixture of free and encapsulated lipid droplets. Free lipid droplets were fabricated using a microfluidizer to generate an oil-in-water nanoemulsion. Encapsulated lipid droplets were fabricated by injecting a nanoemulsion/alginate solution into a calcium bath to generate filled hydrogel beads. Simulated GIT studies indicated that the rate and extent of lipid digestion was strongly dependent on the ratio of free to encapsulated lipid droplets. Free droplets were digested much more rapidly than encapsulated droplets because it was easier for lipase molecules to come into contact with the droplet surfaces. Varying the ratio of free and encapsulated lipid droplets in the emulsions could therefore be used to control the lipid digestion profile. These mixed colloidal delivery systems may have applications in functional food products designed to modulate triglyceride blood levels, hormone release, and energy intake.

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.