Enhancement of Carotenoid Bioaccessibility from Tomatoes Using Excipient Emulsions: Influence of Particle Size

The effect of excipient emulsions with different lipid droplet sizes on carotenoid bioaccessibility from tomatoes was investigated using a simulated gastrointestinal tract (GIT). Excipient emulsions with different surface-weighted mean droplet diameters were fabricated: d ₃₂  = 0.15 μm (small), 0.40 μm (medium), and 22.3 μm (large). Changes in particle size, microstructure, ζ-potential, and carotenoid bioaccessibility were measured when tomato-emulsion mixtures that had received different thermal and mixing treatments were passed through the GIT model. Carotenoid bioaccessibility decreased with increasing initial droplet size (small ≥ medium > large), which was attributed to two effects. First, smaller droplets extracted carotenoids from tomato tissue more efficiently. Second, smaller droplets were digested faster leading to more rapid mixed micelle formation, thereby increasing carotenoid solubilization in intestinal fluids. Carotenoid bioaccessibility was higher from boiled than raw tomatoes because thermal disruption of the plant tissue facilitated carotenoid release. Carotenoid bioaccessibility was higher when tomatoes were boiled with emulsions than when they were boiled alone and then added to emulsions. In conclusion, excipient emulsions are highly effective at increasing carotenoid bioaccessibility from tomatoes, but lipid droplet size must be optimized to ensure high efficacy.

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Increasing the Bioaccessibility of Antioxidants in Tomato Pomace Using Excipient Emulsions

Plant-based foods contain numerous bioactive constituents (“nutraceuticals”) that have beneficial effects on human health. However, their oral bioavailability is often relatively low, which limits their potential efficacy. The bioavailability of nutraceuticals can be increased through the utilization of excipient foods whose compositions and structures are specifically designed to increase the amount of nutraceuticals absorbed in an active form. In this study, olive oil excipient emulsions were designed to increase the bioaccessibility of lycopene and other natural antioxidants in tomato pomace. These emulsions consisted of 8 wt% olive oil and 1 wt% Tween 20 or Tween 80 and were prepared using a microfluidizer operated under different processing conditions (12,000 or 20,000 psi; 3 or 5 passes). Changes in particle size, charge, and bioaccessibility were assessed when tomato pomace-emulsion mixtures were exposed to simulated gastrointestinal digestion. The mean particle diameter of the particles in the excipient emulsions increased after digestion (416 to 446 nm) compared to the values before digestion (200 to 220 nm). The presence of excipient emulsions significantly increased the bioaccessibility of lycopene in tomato pomace compared to oil-free control samples. For instance, lycopene bioaccessibility was > 82% when the tomato pomace was mixed with excipient emulsions but only 29% when it was mixed with oil-free buffer solutions. The presence of excipient emulsions also increased the total phenolic content of the tomato pomace. For instance, the phenolic content was considerably higher in the presence of excipient emulsions (1489 to 2055 mg GAE /100 g FW) than in their absence (939 mg GAE /100 g FW). However, the excipient emulsions did not increase naringenin bioaccessibility, which was attributed to the fact that it was not strongly hydrophobic. The efficacy of the excipient emulsions was only modestly dependent on emulsifier type and homogenization conditions. In conclusion, excipient emulsions can be designed to enhance the bioaccessibility of strongly hydrophobic nutraceuticals in tomato-based products, which may boost their healthiness.

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Impact of Lipid Content on the Ability of Excipient Emulsions to Increase Carotenoid Bioaccessibility from Natural Sources (Raw and Cooked Carrots)

The influence of lipid concentration on the ability of excipient emulsions to increase carotenoid bioaccessibility from raw and cooked carrots was investigated using a simulated gastrointestinal tract (GIT). Excipient emulsions were fabricated using whey protein as a natural emulsifier and a long chain triglyceride (corn oil) as a digestible lipid. Changes in particle size, charge, and microstructure were determined as the carrot-emulsion mixtures were passed through simulated mouth, stomach, and small intestine. Carotenoid bioaccessibility increased with increasing digestible lipid concentration in the excipient emulsions (from 0 to 8 %). Carotenoid bioaccessibility was higher from boiled carrots than for raw carrots, which was attributed to disruption of plant cell structure facilitating carotenoid release. In conclusion, excipient emulsions are highly effective at increasing carotenoid bioaccessibility from carrots, which can be attributed to the ability of the small lipid droplets to rapidly solubilize the carotenoids.     

Food Matrix Effects on Nutraceutical Bioavailability: Impact of Protein on Curcumin Bioaccessibility and Transformation in Nanoemulsion Delivery Systems and Excipient Nanoemulsions

Powdered curcumin was either dissolved in the lipid phase of a nanoemulsion delivery system or it was directly mixed with an excipient nanoemulsion. The influence of thermal treatment (30 or 90 °C) and protein addition (caseinate) on the bioaccessibility and transformation of curcumin was then investigated using a simulated gastrointestinal tract (GIT) model: mouth; stomach; small intestine. Curcumin solubility was high in nanoemulsion delivery systems exposed to both thermal treatments because it was already present in the lipid phase. Conversely, curcumin solubility of a powder mixed with an excipient nanoemulsion was appreciably lower when exposed to 30 °C than 90 °C. This effect was attributed to the greater transfer of curcumin to the lipid phase of the excipient nanoemulsions at elevated temperatures. For the heated samples, the bioaccessibility and transformation of curcumin was not greatly affected by original curcumin location or protein addition. However, curcumin bioaccessibility was appreciably higher in the presence of nanoemulsion lipid droplets than in their absence, which was attributed to an increase in the solubilization capacity of the mixed micelle phase. This study provides some useful information for improving the design of functional foods to improve the oral bioavailability profile of lipophilic nutraceuticals.     

Phase Transition Stability of Cocoa Butter Emulsions

The impact of tempering-crystallization on microstructure and stability of water-in-cocoa butter (w/o) emulsions was analyzed using differential scanning calorimetry (DSC). The type and volume fraction of the disperse phase, and cooling rate during DSC analysis were systematically varied. Freshly prepared emulsions were additionally characterized by microscopy and laser diffraction. Fresh cocoa butter emulsions were composed of small and well dispersed droplets of an average size of 2.24 μm and 1.96 μm for water and 50 % sucrose solution as disperse phase, respectively. The thermograms revealed that the dissolved sugar lowered freezing and melting temperature and, dependent on volume fraction, the dispersion in the oil phase led to a change in solidification behavior. The temperature at the solidification peaks gives qualitative information about droplet size whereas width and number of exothermic events are related to particle size distribution (mono/polydispersity and mono/multimodality) and microstructure. Emulsions with water as dispersed phase show a clear shift of the freezing peaks of the disperse phase which points on modified emulsion microstructure because of droplet coalescence, which is more pronounced at higher volume fraction and lower cooling rate. Emulsions with sucrose solution as dispersed phase showed the greatest stability, wherein the volume fraction and the cooling rate does not matter. The results allow conclusions about the mechanisms of crystallization processes in cocoa butter emulsions resulting as network crystallization.     

The Influence of Environmental Conditions,Lipid Composition,and Phase Behavior on the Origin of Cell Membranes

At some point in life’s development, membranes formed, providing barriers between the environment and the interior of the ‘cell.’ This paper evaluates the research to date on the prebiotic origin of cell membranes and highlights possible areas of continuing study. A careful review of the literature uncovered unexpected factors that influence membrane evolution. The major stages in primitive membrane formation and the transition to contemporary cell membranes appear to require an exacting relationship between environmental conditions and amphiphile composition and phase behavior. Also, environmental and compositional requirements for individual stages are in some instances incompatible with one another, potentially stultifying the pathway to contemporary membranes. Previous studies in membrane evolution have noted the effects composition and environment have on membrane formation but the crucial dependence and interdependence on these two factors has not been emphasized. This review makes clear the need to focus future investigations away from proof-of-principle studies towards developing a better understanding of the roles that environmental factors and lipid composition and polymorphic phase behavior played in the origin and evolution of cell membranes.     

脂肪乳剂理化性质和稳定性的影响因素浅析

静脉注射脂肪乳剂是由两种互不相溶的液体(油相和水相)混合而成,是水不溶性药物的良好栽体,可以提高易水解药物的稳定性并且减少各种毒副作用.脂肪乳荆属于热力学不稳定体系,其会表现出各种不稳定的现象如聚集,絮凝,聚结等,最终可能出现相分离.本文就处方、工艺及包装等影响脂肪乳剂理化性质及稳定性的主要因素进行综述.     

Development of Transparent Curcumin Loaded Microemulsions by Phase Inversion Temperature (PIT) Method: Effect of Lipid Type and Physical State on Curcumin Stability

In this study, curcumin loaded transparent microemulsions obtained using the phase inversion temperature (PIT) method were developed. Different lipids (sunflower, peanut, castor, and extra virgin olive oil, tristearin, and tripalmitin) were tested as curcumin carrier in microemulsions. The obtained systems were analyzed for transparency, particle size, lipid crystal polymorphism, and curcumin stability at 20 °C up to 120 days. It was found that the maximum lipid content allowing transparent microemulsions (mean particle diameter of around 25 nm) to be obtained was greatly affected by the lipid characteristics. By using oils rich in long chain fatty acids, such as sunflower, peanut, and extra virgin olive oil, transparent microemulsions can be obtained with oil fractions up to 7.5 % (w/w). On the contrary, when fat containing crystals (e.g. tripalmitin or tristearin) was used, the maximum lipid loading capacity was reduced to 5 % (w/w). Castor oil, rich in polar groups, did not permit the formation of transparent microemulsions at any tested concentration (from 1 to 9 % w/w). The oil type also affected curcumin stability: curcumin degradation rate was lower in tristearin containing microemulsions than in those containing extra virgin olive oil. This result was attributed to the protective effect of solid lipid particles into lipid droplets.     

Influence of Nanoemulsion Addition on the Stability of Conventional Emulsions

Interest in using nanoemulsions as delivery systems for lipophilic food ingredients is growing due to their high optical clarity, good physical stability, and ability to increase bioavailability. Nanoemulsion-based delivery systems may need to be incorporated into food matrices that also contain conventional emulsions. The aim of this work was to evaluate the effect of adding nanoemulsions (d?<?200 nm) to conventional emulsions (d?>?200 nm) on the creaming stability and microstructure of the mixed systems. Droplet flocculation and rapid creaming was observed when the nanoemulsion concentration exceeded a particular level: the critical flocculation concentration (CFC) was 3.75 % and 0.25 % (v/v) for conventional emulsions with average droplet diameters of 350 and 250 nm, respectively. Confocal microscopy indicated that there was appreciable droplet flocculation, and the fraction of individual droplets with diameters?<?100 nm decreased after 14 days storage, which was probably due to Ostwald ripening and/or coalescence. The results of the present study might have important implications for the incorporation of nanoemulsion-based delivery systems into food products containing larger fat droplets, such as dressings, sauces, or beverages.     

Lipoproteins in Drosophila melanogaster-Assembly, Function, and Influence on Tissue Lipid Composition

Interorgan lipid transport occurs via lipoproteins, and altered lipoprotein levels correlate with metabolic disease. However, precisely how lipoproteins affect tissue lipid composition has not been comprehensively analyzed. Here, we identify the major lipoproteins of Drosophila melanogaster and use genetics and mass spectrometry to study their assembly, interorgan trafficking, and influence on tissue lipids. The apoB-family lipoprotein Lipophorin (Lpp) is the major hemolymph lipid carrier. It is produced as a phospholipid-rich particle by the fat body, and its secretion requires Microsomal Triglyceride Transfer Protein (MTP). Lpp acquires sterols and most diacylglycerol (DAG) at the gut via Lipid Transfer Particle (LTP), another fat body-derived apoB-family lipoprotein. The gut, like the fat body, is a lipogenic organ, incorporating both de novo-synthesized and dietary fatty acids into DAG for export. We identify distinct requirements for LTP and Lpp-dependent lipid mobilization in contributing to the neutral and polar lipid composition of the brain and wing imaginal disc. These studies define major routes of interorgan lipid transport in Drosophila and uncover surprising tissue-specific differences in lipoprotein lipid utilization.     

Arsonoliposomes: Effect of Lipid Composition on Their Stability and Morphology

The influence of the lipid composition of arsonoliposomes on their membrane integrity was investigated to evaluate whether it is possible to combine their action with drugs that can be encapsulated in their aqueous interior. This was investigated by measuring the retention of vesicle-encapsulated calcein (100 mM) during incubation, in the absence and presence of serum proteins. Liposomes containing various concentrations of arsonolipid (with the palmitoyl side chain) as well as egg-lecithin (phosphatidylcholine, PC) and cholesterol (lipid/chol 2:1 mol:mol) were prepared. In some experiments, PC was replaced by the synthetic phospholipid DSPC. All PC/arsonoliposomes tested are stable after 24 h of incubation in buffer at 37°C. After incubation in the presence of serum proteins, arsonoliposomes that contain low amounts of arsonolipid (up to 5 mol% of the lipid content without cholesterol) are stable, whereas increased release of calcein is observed when vesicle arsonolipid concentration is raised (from 5 to 15 mol%). Further increase of arsonolipid content results in immediate decrease of calcein latency while the remaining calcein is rapidly released during incubation. DSPC/arsonoliposomes are comparably more stable, and membrane integrity is independent of the vesicle arsonolipid content, in the range investigated (15–40 mol% of the lipid content without cholesterol). Thereby, we conclude that more stable arsonoliposomes that incorporate high arsonolipid concentrations may be produced when PC is replaced by DSPC. The latter arsonoliposomes provide a system that may be used for combining arsonolipid activity with the activity of other drugs.     

Influence of Matrix Composition on the Bioaccessibility of Copper,Zinc, and Nickel in Urban Residential Dust and Soil

This study examines factors affecting oral bioaccessibility of metals in household dust, in particular metal speciation, organic carbon content, and particle size, with the goal of addressing risk assessment information requirements. Investigation of copper (Cu) and zinc (Zn) speciation in two size fractions of dust (< 36 μ m and 80–150 μ m) using synchrotron X-ray absorption spectroscopy (XAS) indicates that the two metals are bound to different components of the dust: Cu is predominately associated with the organic phase of the dust, while Zn is predominately associated with the mineral fraction. Total and bioaccessible Cu, nickel (Ni), and Zn were determined (on dry weight basis) in the < 150 μ m size fraction of a set of archived indoor dust samples (n = 63) and corresponding garden soil samples (n = 66) from the City of Ottawa, Canada. The median bioaccessible Cu content is 66 μ g g^?1 in dust compared to 5 μ g g^?1 in soil; the median bioaccessible Ni content is 16 μ g g^?1 in dust compared to 2 μ g g^?1 in soil; and the median bioaccessible Zn content is 410 μ g g^?1 in dust compared to 18 μ g g^?1 in soil. For the same data set, the median total Cu content is 152 μ g g^?1 in dust compared to 17 μ g g^?1 in soil; the median total Ni content is 41 μ g g^?1 in dust compared to 13 μ g g^?1 in soil; and the median total Zn content is 626 μ g g^?1 in dust compared to 84 μ g g^?1 in soil. Organic carbon is elevated in indoor dust (median 28%) compared to soil (median 5%), and is a key factor controlling metal partitioning and therefore bioaccessibility. The results show that house dust and soil have distinct geochemical signatures and should not be treated as identical media in exposure and risk assessments. Separate measurements of the indoor and outdoor environment are essential to improve the accuracy of residential risk assessments.     

Changes of Lipid Composition with Growth Phase of Cryptococcus neoformans

Qualitative and quantitative profiles of phospholipids, neutral lipids, and fatty acid composition in Cr. neoformans during the growth phase were investigated in relation to pyrophosphatidic acid. A marked increase of the total lipid content, which depended on the accumulation of triglyceride in yeast cells with the growth, was observed. The total phospholipid contents in yeast cells remained almostly constant during the exponential phase and slightly decreased in the stationary phase. The major phospholipids of this yeast were phosphatidylcholine, phosphatidylethanolamine, phosphatidylinositol, phosphatidylserine, and cardiolipin, the next groups being pyrophosphatidic acid, phosphatidic acid, lysophos-phatidylcholine, and unidentified components. The amounts of phosphatidylcholine, phosphatidylinositol, and cardiolipin were fairly constant throughout the growth phase, but the amount of phosphatidylethanolamine increased and that of phosphatidylserine decreased with progressive growth. The pyrophosphatidic acid contents were 0.9~0.7% for total phospholipid during the growth phase. The major fatty acids of pyrophosphatidic acid were C_16:0, C_18:1, and C_18:2 acids. The changing patterns of fatty acid composition in pyrophosphatidic acid through the growth phase closely resembled that of phosphatidic acid, which contained larger amounts of C_18:1 acid (35~45%) than C_16:0 acid (30~25%) and C_18:2 acid (30~25%). Phosphatidylserine and phosphatidylinositol contained considerable amounts of saturated fatty acid (C_16:0 acid, more than 55%). On the other hand, phosphatidylcholine, phosphatidylethanolamine, and cardiolipin contained extremely large amounts of unsaturated fatty acid (C_18:1 and C_18:2 acid, 85ç90%).     

Influence of Membrane Lipid Composition on a Transmembrane Bacterial Chemoreceptor

Most bacterial chemoreceptors are transmembrane proteins. Although less than 10% of a transmembrane chemoreceptor is embedded in lipid, separation from the natural membrane environment by detergent solubilization eliminates most receptor activities, presumably because receptor structure is perturbed. Reincorporation into a lipid bilayer can restore these activities and thus functionally native structure. However, the extent to which specific lipid features are important for effective restoration is unknown. Thus we investigated effects of membrane lipid composition on chemoreceptor Tar from Escherichia coli using Nanodiscs, small (∼10-nm) plugs of lipid bilayer rendered water-soluble by an annulus of “membrane scaffold protein.” Disc-enclosed bilayers can be made with different lipids or lipid combinations. Nanodiscs carrying an inserted receptor dimer have high protein-to-lipid ratios approximating native membranes and in this way mimic the natural chemoreceptor environment. To identify features important for functionally native receptor structure, we made Nanodiscs using natural and synthetic lipids, assaying extents and rates of adaptational modification. The proportion of functionally native Tar was highest in bilayers closest in composition to E. coli cytoplasmic membrane. Some other lipid compositions resulted in a significant proportion of functionally native receptor, but simply surrounding the chemoreceptor transmembrane segment with a lipid bilayer was not sufficient. Membranes effective in supporting functionally native Tar contained as the majority lipid phosphatidylethanolamine or a related zwitterionic lipid plus a rather specific proportion of anionic lipids, as well as unsaturated fatty acids. Thus the chemoreceptor is strongly influenced by its lipid environment and is tuned to its natural one.     

Stability and Liquid-Liquid Phase Separation in Mixed Saturated Lipid Bilayers

The phase stability of a fluid lipid bilayer composed of a mixture of DC₁₈PC, (DSPC), and a shorter DC_ns PC, with n_s from 8 to 17, has been studied using a self-consistent field theory that explicitly includes molecular details and configurational properties of the lipid molecules. Phase separation between two liquid phases was found when there was a sufficient mismatch between the hydrophobic thicknesses of the two bilayers composed entirely of one component or the other. This occurs when n_s ≤ 12 and there is a sufficient concentration of the shorter lipid. The mixture separates into a thin bilayer depleted of DSPC and a thick bilayer enriched in DSPC. Even when there is no phase separation, as in the cases when there is either insufficient concentration of a sufficiently short lipid or any concentration of a lipid with n_s > 12, we observe that the effect of the shorter lipid is to increase the susceptibility of the system to fluctuations in the concentration. This is of interest, given that a common motif for the anchoring of proteins to the plasma membrane is via a myristoyl chain, that is, one with 14 carbons.     

Effects of Culture Method and Growth Phase on Free Lipid Composition of Yersinia pseudotuberculosis

The influence of culture method (free-floating cells in liquid nutrient broth or bacteria attached to agar surface on solid agarized medium of the same formulation) and bacterial age on the composition of free lipids in Yersinia pseudotuber-culosis (O:Ib serovar, strain KS 3058) grown in the cold (5°C) has been investigated. The specific growth rate of the bacteria on solid medium was about threefold less than that in liquid medium. The qualitative composition of phospholipids and fatty acids only slightly depended on the bacterial culture method. At the same time, the colonially growing cultures contained somewhat more total lipids, they synthesized more phospholipids, in the linear growth phase they contained more lysophosphatides, and they had higher fatty acid unsaturation index and higher pathogenic potential than their planktonic counterparts grown in otherwise identical conditions. The bacterial growth phase influenced the amount of 3-hydroxytetrade-canoic acid and, indirectly, that of lipopolysaccharide. The dynamics of changes in the amount of this acid with bacterial age was opposite in the surface and broth cultures.     

Influence of Lipid Composition on Pediocin PA-1 Binding to Phospholipid Vesicles

Pediocin PA-1 bound to anionic lipid vesicles with saturated or unsaturated fatty acid chains in a lipid concentration-dependent fashion. Little change in binding parameters was observed for zwitterionic lipid vesicles. Decreasing the anionic lipid content of the vesicles gave a higher relative dissociation constant for the peptide-lipid interactions and further supports the electrostatic interaction model of binding.     

Effects of Lecithin Addition in Oil or Water Phase on the Stability of Emulsions Made with Whey Proteins

The effects of lecithin addition in oil or water phase on the stability of oil-in-water emulsions made with 0.1 wt% whey protein and 10 wt% n-tetradecane at neutral and acidic pH were studied by monitoring the gravitational creaming and phase separation. The effects of lecithin addition on the interfacial behavior of β-lactoglobulin were also studied to compare with the results of emulsion stability. At neutral pH, crude phosphatidylcholine (PC) from egg yolk or soybean increased the stability of the emulsion made with protein and lowered the interfacial tension of protein films more effectively than pure egg PC. A more remarkable effect on both the emulsion stability and the interfacial tension was found when crude PC was added in the oil phase rather than in the water phase. The purity of lecithins and the way to add them are suggested to be very important to make a stable emulsion with protein. On acidic pH (4.5 or 3.0), the increased creaming or phase separation in a whey protein-stabilized emulsion, but the lowered interfacial tension of β-lactoglobulin films, were found upon the addition of pure or crude PC in oil or water phase. These results suggest that in acidic pH, densely packed films may be formed on a planar oil–water interface, but not on adsorbed layers around oil droplets in an emulsion.     

SN-38-Cyclodextrin Complexation and Its Influence on the Solubility,Stability, and In Vitro Anticancer Activity Against Ovarian Cancer

SN-38, an active metabolite of irinotecan, is up to 1,000-fold more potent than irinotecan. But the clinical use of SN-38 is limited by its extreme hydrophobicity and instability at physiological pH. To enhance solubility and stability, SN-38 was complexed with different cyclodextrins (CDs), namely, sodium sulfobutylether β-cyclodextrin (SBEβCD), hydroxypropyl β-cyclodextrin, randomly methylated β-cyclodextrin, and methyl β-cyclodextrin, and their influence on SN-38 solubility, stability, and in vitro cytotoxicity was studied against ovarian cancer cell lines (A2780 and 2008). Phase solubility studies were conducted to understand the pattern of SN-38 solubilization. SN-38-βCD complexes were characterized by differential scanning calorimetry (DSC), X-ray powder diffraction analysis (XRPD), and Fourier transform infrared (FTIR). Stability of SN-38-SBEβCD complex in pH 7.4 phosphate-buffered saline was evaluated and compared against free SN-38. Phase solubility studies revealed that SN-38 solubility increased linearly as a function of CD concentration and the linearity was characteristic of an A_P-type system. Aqueous solubility of SN-38 was enhanced by about 30–1,400 times by CD complexation. DSC, XRPD, and FTIR studies confirmed the formation of inclusion complexes, and stability studies revealed that cyclodextrin complexation significantly increased the hydrolytic stability of SN-38 at physiological pH 7.4. Cytotoxicity of SN-38-SBEβCD complex was significantly higher than SN-38 and irinotecan in both A2780 and 2008 cell lines. Results suggest that SBEβCD encapsulated SN-38 deep into the cavity forming stable inclusion complex and as a result increased the solubility, stability, and cytotoxicity of SN-38. It may be concluded that preparation of inclusion complexes with SBEβCD is a suitable approach to overcome the solubility and stability problems of SN-38 for future clinical applications.