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PubMed2001

Emulsion properties of casein and whey protein hydrolysates and the relation with other hydrolysate characteristics.

Casein and whey protein were hydrolyzed using 11 different commercially available enzyme preparations. Emulsion-forming ability and emulsion stability of the digests were measured as well as biochemical properties with the objective to study the relations between hydrolysate characteristics and emulsion properties. All whey protein hydrolysates formed emulsions with bimodal droplet size distributions, signifying poor emulsion-forming ability. Emulsion-forming ability of some casein hydrolysates was comparable to that of intact casein. Emulsion instability was caused by creaming and coalescence. Creaming occurred mainly in whey hydrolysate emulsions and in casein hydrolysate emulsions containing large emulsion droplets. Coalescence was dominant in casein emulsions with a broad particle size distribution. Emulsion instability due to coalescence was related to apparent molecular weight distribution of hydrolysates; a relative high amount of peptides larger than 2 kDa positively influences emulsion stability.

Caseins↗
PubMed2004

Characterization of fluorocarbon-in-water emulsions with added triglyceride.

Fluorocarbon-in-water emulsions are being explored clinically as synthetic oxygen carriers in general surgery. Stabilizing fluorocarbon emulsions against coarsening is critical in maintaining the biocompatibility of the formulation following intravenous administration. It has been purported that the addition of a small percentage of long-chain triglyceride results in stabilization of fluorocarbon emulsions via formation of a three-phase emulsion. In a three-phase emulsion, the triglyceride forms a layer around the dispersed fluorocarbon, thereby improving the adhesion of the phospholipid surfactant to the dispersed phase. In the present study, we examined the effect of triglyceride addition on the physicochemical characteristics of the resulting complex dispersion. In particular, we examined the particle composition and stability of the dispersed particles using a method which first fractionates (classifies) the different particles prior to sizing (i.e., sedimentation field-flow fractionation). It was determined that the addition of a long-chain triglyceride (soybean oil) results in oil demixing and two distinct populations of emulsion droplets. The presence of the two types of emulsion droplets is not observed via light scattering techniques, since the triglyceride droplets dominate the scattering due to a large difference in the refractive index between the particles and the medium as compared to fluorocarbon droplets. The growth of the fractionated fluorocarbon emulsion droplets was followed over time, and it was found that there was no difference in growth rates with and without added triglyceride. In contrast, addition of medium-chain-triglyceride (MCT) oils results in a single population of emulsion droplets (i.e., a three-phase emulsion). These emulsions are not stable to droplet coalescence, however, as significant penetration of MCT into the phospholipid lipid interfacial layer results in a negative increment in the monolayer spontaneous curvature, thereby favoring water-in-oil emulsions and resulting in destabilization of the emulsion to the effects of terminal heat sterilization or mechanical stress.

Chemical Phenomena↗
PubMed1998

Influence of interfacial rheological properties of mixed emulsifier films on the stability of water-in-oil-in-water emulsions.

The purpose of this study was to investigate the influence of mixtures of the emulsifiers Span 80, 83 and 85 and Tween 80 on multiple emulsion stability. An oscillatory ring-surface rheometer was used to measure interfacial elasticity at the oil-aqueous interface. Multiple emulsions were prepared via a two-step emulsification process and stability was evaluated by investigation of drug transport from freshly prepared and eight-day-old emulsions by use of a dialysis method. Photomicrography and droplet-size analysis of multiple emulsions were also conducted. Spans 80 and 83 were appreciably elastic (683.10+/-29.13 mNm(-1) and 1128.09+/-14.81 mNm(-1), respectively at 5% w/v) when present at the mineral oil-aqueous interface whereas Span 85 and Tween 80 were not (11.10+/-3.88 mNm(-1) (5% w/v) and 0 (0.1-5% w/v) respectively). The interfacial elasticities of Spans 80 and 83 decreased in the presence of Tween 80 in the aqueous phase; this was attributed to co-adsorption of Tween 80 at the interface or aqueous-phase solubilization of the Spans within mixed micelles, or both. Drug-transport studies indicated that drug release on storage was lower from water-in-oil-in-water (w/o/w) emulsions prepared with 5% w/v Span 80 or 83 and 0.1% w/v Tween 80 than from emulsions prepared with 5% w/v Spans 80 or 83 and 1% w/v Tween 80. Photomicrography and droplet-size analysis indicated the same trend-emulsions containing a higher percentage of Tween 80 were less stable. The relatively stable w/o/w emulsions (e.g. 5% w/v Spans 80 or 83 and 0.1% w/v Tween 80) contained a large number of multiple droplets for up to eight weeks of storage whereas the relatively unstable w/o/w emulsions (e.g., 5% w/v Span 85 and 0.1% w/v Tween 80 and 5% w/v Spans and 1% w/v Tween 80) contained mostly simple droplets after only one week of storage. The mean volume/weight droplet size decreased on storage with breakdown of these w/o/w emulsions to simple oil-in-water emulsions. There was a positive correlation between the interfacial elasticity and emulsion stability data. Mixed emulsifiers giving higher film strength, as quantified by interfacial elasticity measurements, resulted in more stable w/o/w emulsions.

Anti-Inflammatory Agents, Non-Steroidal↗
PubMedDate not supplied

Digestion and absorption of tube-feeding emulsions with different droplet sizes and compositions in the rat.

Assimilation of lipid nutrients depends on the efficiency of emulsified fat hydrolysis by digestive lipases. As shown in vitro, the activity of preduodenal and pancreatic lipases is governed by the physicochemical properties of emulsions. Thus the aim of this study was to evaluate in the rat how emulsions are digested and assimilated depending on their droplet size or solute composition. Fasted rats were intragastrically tube fed emulsions with different median droplet sizes (0.6 microns, fine; 22 microns, coarse) or solute composition (0.8 microns, complex fine) containing 14C-triolein and 3H-cholesterol. Two and 5 hours after feeding, fat-droplet size was measured in gastric and duodenal contents, and lipids were radioactively quantified in different compartments. In the stomach, the droplet size of the fine emulsions significantly increased to values (13 microns to 24 microns) comparable with those of the coarse emulsion (35 microns to 36 microns). In the duodenum, the droplet sizes of the three emulsions were in the range of 14 microns to 33 microns. After 2 hours, gastric triglyceride hydrolysis was significantly higher with the fine than with the coarse emulsion and was lower with the complex fine emulsion. Gastric emptying of fat was significantly different, with the following decreasing order: coarse, fine, and complex fine emulsion. In the small intestine, the fine and coarse emulsions were processed comparably, whereas the assimilation of the fine complex emulsion was significantly delayed. Calculations indicate that ingested fatty acids were distributed in the peripheral tissues at different rates with the same decreasing order. The fate of a lipophilic nutrient, cholesterol, was also markedly altered by the type of emulsion. These data support the concept that tube-fed emulsions with different droplet sizes and solute composition are digested differently and thus are metabolized differently.

Absorption↗
PubMed1996

Pharmacokinetics of highly lipophilic antitumor agent palmitoyl rhizoxin incorporated in lipid emulsions in rats.

The effects of i.v. formulations on the pharmacokinetics were examined for two antitumor agents with different lipophilicities: rhizoxin and palmitoyl-rhizoxin (RS-1541). Blood disposition and tissue distributions in rats were evaluated using three formulations: polyethylene glycol 400 (PEG)/dimethylacetamide (DMA) solution, colloidal solution, and lipid emulsions composed of dioctanoyl decanoyl glycerol (ODO) and polyoxyethylene-(60)-hydrogenated castor oil (HCO-60). The effects of emulsion particle size on the pharmacokinetics were also investigated. Rhizoxin rapidly disappeared from the plasma and showed high distribution in the tissues, and in vitro rapidly degraded in the plasma independent of the formulations used. In in vitro plasma, rhizoxin was easily released from the emulsion particles. In contrast to rhizoxin, the pharmacokinetics of RS-1541 with greater lipophilicity changed considerably depending on the formulations. The emulsions showed high and sustained plasma concentrations for RS-1541. RS-1541 was stably incorporated in the emulsion droplets and protected from the degradation when it was applied as an emulsion. Tissue distributions of RS-1541 in rats after an injection as lipid emulsion were strongly affected by the emulsion particle size. Small size emulsions (100-110 nm) showed the highest plasma concentrations of RS-1541, though they were unable to suppress distributions of the drug in peripheral tissues. Emulsions larger than 200 nm (approx.) in size, on the contrary, effectively inhibited the drug from entering the bone marrow, small intestine and other non-reticuloendothelial system (non-RES) organs, where many cytotoxic compounds showed undesired toxicities. These results indicate that the lipid emulsions composed of ODO and HCO-60 could be a promising and effective DDS carrier for RS-1541, which is highly lipophilic and stabilized in the emulsions. This was not the case for rhizoxin, however, which was less lipophilic than palmitoyl analogue RS-1541. The work described herein has demonstrated that by properly selecting the particle size, these lipid emulsions can control the behavior of a drug in the body.

Animals↗
PubMed1990

Intravascular behavior of a perfluorochemical emulsion.

The purpose of this study was to clarify the reason why two similar perfluorochemical (PFC) emulsions, namely a mixed PFC (perfluorodecalin: FDC and perfluorotripropylamine: FTPA) and an FDC emulsion, resulted in a very different survival time for the exchange-transfused rats. Supposing that some difference in the intravascular behavior of both emulsions would account for such a difference in efficacy, experiments on behavior of PFC emulsions were carried out focusing on the particle size. It was reconfirmed that larger PFC particles were eliminated from the blood stream much more rapidly than smaller particles with three FMIQ (perfluoro-N-methyldecahydroisoquinoline) emulsions. After the FDC + FTPA emulsion or the FDC emulsion were injected into rabbits, PFC particles in the blood tended to decrease in size. When each of the collected blood samples was incubated at 37 degrees C for 24 h, the FDC emulsion enlarged in size markedly, but the FDC + FTPA emulsion showed no change. The retention of PFC particles appeared to depend on the emulsion stability rather than simply on the emulsifying agent alone. These data showed that some differences were observed in intravascular persistence of the FDC + FTPA emulsion and the FDC emulsion, and suggested that the efficacy of PFC emulsions would reflect their behavior in the circulation.

Animals↗
PubMed1998

Influence of protein emulsifier interfacial properties on oil-in-water emulsion stability.

The purpose of this study was to determine whether the interfacial properties of emulsifier films could be related to emulsion stability and therefore be used as stability predictors using Bovine serum albumin (BSA) as a model oil-in water (o/w) emulsifier. Soybean o/w emulsions were prepared by ultrasonication, emulsion droplet interfacial charge was determined by microelectrophoresis, droplet size distribution was measured using an Accusizer, and centrifugal stress was studied using an ultracentrifuge. Real time, thermal kinetic, and centrifugal stress accelerated stability tests were performed. Stability data obtained from centrifugal stress tests followed the same trends as real time stability data and these data were in general agreement with stability predictions made based on interfacial properties. The thermal kinetic accelerated tests were not predictive of stability, because emulsion breakdown was rapid and did not allow differentiation between the emulsions. Emulsion stability increased with an increase in emulsifier concentration (emulsions prepared at 2% w/v BSA had not cracked at 60 days, whereas those prepared at 0.1% w/v had cracked-by 30 days), increase in ionic strength (emulsions prepared at an ionic strength of 1 mM had cracked by 60 days, whereas those prepared at an ionic strength of 10 mM had cracked by 90 days), and decrease in temperature (emulsions prepared at 37 and 60 degrees C had cracked by 5 days, whereas those prepared at 5 and 25 degrees C had not cracked at 60 days). There was no significant change in stability for emulsions prepared at pH 5.3 and pH 7.4. The addition of dextran sulfate improved emulsion stability, whereas the addition of acacia decreased stability. Emulsions prepared with BSA alone cracked by 90 days, those prepared with BSA and acacia cracked by 30 days, and those prepared with BSA and dextran sulfate had not cracked at 90 days. Interfacial properties were useful in predicting emulsion stability.

Drug Stability↗
PubMedDate not supplied

Principles of emulsion stabilization with special reference to polymeric surfactants.

This overview summarizes the basic principles of emulsion stabilization with particular reference to polymeric surfactants. The main breakdown processes in emulsions are briefly described. A section is devoted to the structure of polymeric surfactants and their conformation at the interface. Particular attention is given to two polymeric surfactants that are suitable for oil-in-water (O/W) and water-in-oil (W/O) emulsions. For O/W emulsions, a hydrophobically modified inulin (HMI), obtained by grafting several alkyl groups on the backbone of the inulin (polyfructose) chain, is the most suitable. For W/O emulsions, an A-B-A block copolymer of polydroxystearic acid (PHS), the A chains, and polyethylene oxide (PEO), the B chain, is the most suitable. The conformation of both polymeric surfactants at the O/W and W/O interfaces is described. A section is devoted to the interaction between emulsion droplets containing adsorbed polymer surfactant molecules. This interaction is referred to as steric stabilization, and it is a combination of two main effects, namely, unfavorable mixing of the A chains, referred to as the mixing interaction, Gmix, and loss of configurational entropy on significant overlap of the stabilizing chains, referred to as elastic interaction, Gel. The criteria for effective steric stabilization are summarized. O/W emulsions based on HMI are described, and their stability in water and in aqueous electrolyte solutions is investigated using optical microscopy. Very stable emulsions can be produced both at room temperature and at 50 degrees C. The reason for this high stability is described in terms of the multipoint anchoring of the polymeric surfactant (by several alkyl groups), the strong hydration of the inulin (polyfructose) chains, and the high concentration of inulin in the adsorbed layer. W/O emulsions using PHS-PEO-PHS block copolymer can be prepared at a high volume fraction of water, varphi, and these emulsions remain fluid up to high varphi values (> 0.6). These emulsions also remain stable for several months at room temperature and at 50 degrees C. The last two sections are concerned with the problems of creaming or sedimentation and phase inversion. Creaming or sedimentation can be prevented by the use of "thickeners" in the continuous phase. These molecules produce non-Newtonian systems that will have a high residual or zero shear viscosity. The latter, which may exceed 1000 Pas, can also be prevented by control of the bulk (or elastic) modulus of the system. Phase inversion in O/W emulsions can also be prevented using HMI, since this polymeric surfactant is not soluble in the oil phase. As long as coalescence and Ostwald ripening are prevented, the emulsions can remain stable for very long times both at room temperature and at 50 degrees C.

Cosmetics↗
PubMed2002

Sulfite supported lipid peroxidation in propofol emulsions.

BACKGROUND: Sodium metabisulfite is added to a commercial propofol emulsion as an antimicrobial agent. The sulfite ion (SO3(-2)) is capable of undergoing a number of reactions, including autooxidation and the promotion of lipid peroxidation. This study evaluated sulfite reactivity in propofol emulsions by determining thiobarbituric acid reacting substances (TBARS), sulfite depletion, and emulsion pH in emulsions containing sulfite or EDTA. METHODS: Commercial EDTA and sulfite propofol emulsions were compared, and 10% soybean oil emulsion containing various additives were evaluated for TBARS, sulfite, and pH. TBARS were analyzed with a modified thiobarbituric acid method. Sulfite was analyzed by the reaction of sulfite with 5,5'-dithiobis(2-nitrobenzoic acid). pH was measured by glass electrode methodology. RESULTS: Thiobarbituric acid reacting substances were detectable in commercial sulfite propofol emulsions in concentrations ranging from 0.02 to 0.22 microg/ml based on malondialdehyde. No TBARS were detected in EDTA propofol emulsions. Incubation (37 degrees C, up to 6 h) of sulfite propofol emulsions in air resulted in further increases in TBARS (35-160%). No increases occurred in incubated EDTA propofol emulsions. Metabisulfite (0.25 mg/ml) alone added to 10% soybean oil resulted in large increases in TBARS that were inhibited in part by propofol (10 mg/ml) and completely by ascorbic acid (0.05 mg/ml). Soybean oil emulsion pH declined rapidly on the addition of metabisulfite (0.25 mg/ml). The addition of propofol (10 mg/ml) partially inhibited the decline in pH and ascorbic acid (0.05 mg/ml) completely inhibited it. CONCLUSION: These results show that sulfite supports the peroxidation of lipids in soybean oil emulsions and propofol functions to partially inhibit these processes.

Ascorbic Acid↗
PubMed2006

A rheological method to evaluate the physical stability of highly viscous pharmaceutical oil-in-water emulsions.

PURPOSE: The aim of this study was to develop a rheological method to evaluate the stability of highly viscous pharmaceutical emulsions. Thereby, the time devoted to the storage tests could be reduced and manufacturers could save time in optimizing their formulations and manufacturing techniques for topical pharmaceutical forms. The influence of the type of oil and the type of emulsifier on the microstructure of the emulsions was also studied. MATERIALS AND METHODS: The samples were stored at 25 and at 50 degrees C for 6 months and analysed every month using rheological as well as microscopic techniques. The size and the organization of the droplets within the emulsion were determined by freeze-fracture electron microscopy and optical contrast phase microscopy. RESULTS: A decrease in the rheological parameters was observed for the OC emulsions ("Tween/Span" emulsions made with olive oil) and the "Montanov" emulsions. The rheological measurements showed that the structure of the OC emulsions and that of the emulsions made with the Montanov 82 emulsifier become more brittle when submitted to a shear force. The micrographs obtained by freeze-fracture electron microscopy showed that for OC only the oil droplets arrange in a network structure. Storage tests at 50 degrees C confirmed the rheological assumptions on the stability of emulsions. CONCLUSION: The study of the effect of shearing on the emulsions allowed quick discrimination between the emulsions according to their stabilities. The rheological tool gave information on the structure of the emulsions and on the aging process.

Administration, Topical↗
PubMed2003

Studies of the formation process of water-in-oil emulsions.

This paper summarizes studies to determine the formation process of water-in-oil emulsions and the stability of such emulsions formed in the laboratory and in a large test tank. These studies have confirmed that water-in-oil mixtures can be grouped into four states: stable emulsions, unstable water-in-oil mixtures, mesostable emulsions, and entrained water. These states are differentiated by rheological properties as well as by differences in visual appearance. The viscosity of a stable emulsion at a shear rate of one reciprocal second is about three orders of magnitude greater than that of the starting oil. An unstable emulsion usually has a viscosity no more than about 20 times greater than that of the starting oil. A stable emulsion has a significant elasticity, whereas an unstable emulsion does not. A mesostable emulsion has properties between stable and unstable, but breaks down within a few days of standing. The usual situation is that emulsions are either obviously stable, mesostable, or unstable. Entrained water, water suspended in oil by viscous forces alone, is also evident. Very few emulsions have questionable stability. Analytical techniques were developed to test these observations. The type of emulsion produced is determined primarily by the properties of the starting oil. The most important of these properties are the asphaltene and resin content and the viscosity of the oil. The composition and property ranges of the starting oil that would be required to form each of the water-in-oil states are discussed in this paper.

Chemical Phenomena↗
PubMed2003

Effects of plasma apolipoproteins on lipoprotein lipase-mediated lipolysis of small and large lipid emulsions.

Large (ca. 120 nm) and small (ca. 35 nm) emulsions consisting of triolein (TO) and phosphatidylcholine (PC) were prepared as the primary protein-free models of chylomicrons and their remnants, respectively. Lipoprotein lipase (LPL)-mediated lipolysis of emulsion TO was retarded in chylomicron-free human plasma compared with the hydrolysis activated by isolated apolipoprotein C-II (apoC-II). In 30% plasma, free fatty acid (FFA) release rate was higher for large emulsions than for small ones, while both emulsions were hydrolyzed at similar rates in the presence of isolated apoC-II. Isolated apolipoprotein C-III (apoC-III) or apolipoprotein E (apoE) worked as LPL-inhibitor of the lipolysis activated by apoC-II. It was also observed that apolipoprotein A-I (apoA-I) showed distinct inhibitory effects on the lipolysis of large and small emulsions: more effective inhibition for small emulsions. Kinetic analyses showed that K(m)(app) and V(max)(app) for the lipolysis of emulsions were lower in the presence of 30% plasma than isolated apoC-II. ApoA-I also markedly decreased K(m)(app) and V(max)(app) for LPL-catalyzed hydrolysis of both emulsions. In chylomicron-free serum, the density of bound apoA-I at small emulsion surfaces was about three fold greater than large emulsion surfaces, but the binding densities of apoC-II, apoC-III and apoE were less for small emulsion surfaces than for large ones, suggesting that apoA-I preferentially binds to small particles and displaces other exchangeable apolipoproteins from particle surfaces. These results indicate that, in addition to the well known inhibitory effects of apoC-III and apoE, apoA-I in plasma regulates the lipolysis of triglyceride (TG)-rich emulsions and lipoproteins in a size-dependent manner.

Animals↗
PubMed2004

Influence of iota-carrageenan on droplet flocculation of beta-lactoglobulin-stabilized oil-in-water emulsions during thermal processing.

The influence of thermal processing on droplet flocculation in oil-in-water emulsions stabilized by either beta-lactoglobulin (primary emulsions) or beta-lactoglobulin-iota-carrageenan (secondary emulsions) at pH 6 has been investigated. In the absence of salt, the zeta-potential of the primary emulsion was less negative (-40 mV) than that of the secondary emulsion (-55 mV) due to adsorption of anionic iota-carrageenan to the anionic beta-Lg-coated droplet surfaces. The zeta-potential and mean diameter (d(43) approximately 0.3 microm) of droplets in primary and secondary emulsions did not change after storage at temperatures ranging from 30 to 90 degrees C. In the presence of 150 mM NaCl, the zeta-potential of the primary emulsion was much less negative (-27 mV) than that of the secondary emulsion (-50 mV), suggesting that the latter was less influenced by electrostatic screening effects. The zeta-potential of the primary emulsions did not change after storage at elevated temperatures (30-90 degrees C). The zeta-potential of the secondary emulsions became less negative, and the aqueous phase iota-carrageenan concentration increased at storage temperatures exceeding 50 degrees C, indicating iota-carrageenan desorbed from the beta-Lg-coated droplets. In the primary emulsions, appreciable droplet flocculation (d(43) approximately 8 microm) occurred at temperatures below the thermal denaturation temperature (T(m)) of the adsorbed proteins due to surface denaturation, while more extensive flocculation (d(43) > 20 microm) occurred above T(m) due to thermal denaturation. In the secondary emulsions, the extent of droplet flocculation below T(m) was reduced substantially (d(43) approximately 0.8 microm), which was attributed to the ability of adsorbed carrageenan to increase droplet-droplet repulsion. However, extensive droplet flocculation was observed above T(m) because carrageenan desorbed from the droplet surfaces. Differential scanning calorimetry showed that iota-carrageenan and beta-Lg interacted strongly in aqueous solutions containing 0 mM NaCl, but not in those containing 150 mM NaCl, presumably because salt weakened the electrostatic attraction between the molecules.

Calorimetry, Differential Scanning↗
PubMed2006

Effect of thermal treatment, ionic strength, and pH on the short-term and long-term coalescence stability of beta-lactoglobulin emulsions.

We present experimental results about the effects of thermal treatment, ionic strength, and pH on the protein adsorption and coalescence stability of freshly prepared (2 h after emulsification) and 6-day-stored emulsions, stabilized by the globular protein beta-lactoglobulin (BLG). In all emulsions studied, the volume fraction of the dispersed soybean oil is 30% and the mean drop diameter is d(32) approximately 40 microm. The protein concentration, C(BLG), is varied between 0.02 and 0.1 wt %, the electrolyte concentration, C(EL), between 1.5 mM and 1 M, and pH between 4.0 and 7.0. The emulsion heating is performed at 85 degrees C, which is above the denaturing temperature of BLG. The results show that, at C(BLG) > or = 0.04 wt %, C(EL) > or = 150 mM, and pH > or = 6.2, the heating leads to higher protein adsorption and to irreversible attachment of the adsorbed molecules, which results in enhanced steric repulsion between the protein adsorption multilayers and to higher emulsion stability. At low electrolyte concentration, C(EL) < or = 10 mM, the emulsion stability is determined by electrostatic interactions and is not affected significantly by the emulsion heating. The latter result is explained by electrostatic repulsion between the adsorbed protein molecules, which keeps them separated from each other and thus precludes the formation of disulfide covalent bonds in the protein adsorption layer. The coalescence stability of heated and nonheated emulsions is practically the same and does not depend on C(EL), when pH is around the isoelectric point (IEP) of the protein molecules. This is explained with the adsorption of uncharged BLG molecules, in compact conformation, which stores the reactive sulfhydryl groups hidden inside the molecule interior, thus preventing the formation of covalent intermolecular bonds upon heating. We studied also the effect of storage time on the stability of heated and nonheated emulsions. The stability of nonheated emulsions (C(BLG) = 0.1 wt %, C(EL) > or = 150 mM, and pH = 6.2) significantly decreases after 1 day of storage (aging effect). In contrast, no aging effect is observed after emulsion heating. FTIR spectra of heated and nonheated, fresh and aged emulsions suggest that the aging effect is caused by slow conformational changes of the protein molecules in the adsorption layer, accompanied with partial loss of the ordered secondary structure of the protein and with the formation of lateral noncovalent bonds (H-bonds and hydrophobic interactions) between the adsorbed molecules. After thermal treatment of the BLG emulsions, the molecules preserve their original secondary structure upon storage, which eliminates the aging effect.

Animals↗
PubMedDate not supplied

Biodistribution characteristics of mannosylated and fucosylated O/W emulsions in mice.

Cell-specific drug delivery is one of the most promising strategies for improving therapeutic efficiency and minimizing systemic toxicity. Carrier systems devoted to receptor-mediated targeting need to be developed. In the case of liver-non-parenchymal cell-specific targeting systems, glycosylated emulsions have been developed as carriers for lipophilic drugs and/or peptides. This present study demonstrates the in vivo disposition behaviour and pharmacokinetic characteristics of mannosylated (Man-) and fucosylated (Fuc-) emulsions incorporated with cholesten-5-yloxy-N-(4-((1-imino-2-D-thiomannosylethyl)amino)alkyl)formamide (Man-C4-Chol) and its fucosylated derivatives (Fuc-C4-Chol), respectively. Man- (or Fuc-) emulsions are composed of soybean oil, EggPC and Man-C4-Chol (or Fuc-C4-Chol) in a weight ratio of 70:25:5. After intravenous administration to mice, these two types of [(3)H]cholesteryl hexadecyl ether (CHE)-labelled glycosylated emulsions were rapidly eliminated from the blood circulation and preferentially recovered in the liver. In contrast, bare (Bare-) emulsions composed of soybean oil:EggPC:cholesterol (Chol) in a weight ratio of 70:25:5 were more retained in the blood circulation. The hepatic uptake clearances of Man- and Fuc-emulsions were 3.3- and 4.0-times greater than that of Bare-emulsions. Interestingly, the hepatic uptake clearance of Fuc-emulsions was significantly higher that that of Man-emulsions. The uptake ratios by non-parenchymal cells (NPC) and parenchymal cells (PC) (NPC/PC ratio) for Bare-, Man- and Fuc-emulsions were found to be 0.4, 2.0 and 2.9, respectively. The hepatic uptakes of [(3)H]CHE-labelled Man- and Fuc-emulsions were reduced by pre-dosing with glycosylated proteins and liposomes. These results clearly support the conclusion that Man- and Fuc-emulsions are promising carrier systems for liver NPC-specific targeting via receptor-mediated mechanism.

Animals↗
PubMed2006

Triglycerides in fish oil affect the blood clearance of lipid emulsions containing long- and medium-chain triglycerides in mice.

Lipid emulsions containing long-chain triglycerides (LCT) and medium chain triglycerides (MCT) are widely used in parenteral nutrition. Recently, fish oil (FO) triglyceride (TG)-derived emulsions are considered therapeutic because of their many beneficial biological modulatory actions. We investigated in mice whether adding 10% FO to an intravenous lipid emulsion with MCT and LCT (MCT:LCT:FO -50:40:10% by wt) would affect particle blood clearance and tissue targeting in comparison to LCT (100% by wt) and MCT:LCT (50:50% by wt) emulsions. The 3 emulsions were labeled with [3H] cholesteryl oleoyl ether and administered by bolus injection (400 microg TG/mouse) to C57BL/6J mice. Contributions of LDL receptor (LDL-R) and LDL-R-related protein to emulsion catabolism were assessed using LDL-R-deficient mice and preinjection of lactoferrin, and the effects of lipoprotein lipase (LPL) were determined by preinjection of heparin and Triton WR 1339. Although fractional catabolic rates did not differ among the 3 emulsions, blood removal at each time point after injection was greater for MCT:LCT:FO particles due to their higher initial margination volume. Compared with MCT:LCT and LCT emulsions, patterns of tissue uptake of the MCT:LCT:FO emulsions were different, e.g. MCT:LCT:FO emulsion particle uptake was lower in heart, adipose tissue, and muscle, and higher in lung, and the removal of MCT:LCT:FO emulsion particles was less dependent on LPL, LDL-R, and lactoferrin-sensitive pathways. These data suggest that the addition of a low percentage of FO to MCT:LCT emulsions substantially changes their particle clearance and tissue uptake mechanisms.

Animals↗
PubMedDate not supplied

Parenteral structured triglyceride emulsion improves nitrogen balance and is cleared faster from the blood in moderately catabolic patients.

BACKGROUND: Most postoperative patients lose net protein mass, which reflects loss of muscle tissue and organ function. Perioperative parenteral nutrition may reduce the loss of protein, but in general, with conventional lipid emulsions a waste of protein still remains. METHODS: We compared the effects on nitrogen balance of an emulsion containing structured triglycerides, a new type of synthesized triglycerides, with an emulsion of a physical mixture of medium- and long-chain triglycerides as part of parenteral feeding in moderately catabolic patients. The first 5 days after placement of an aortic prosthesis patients received total parenteral nutrition (TPN) providing 0.2 g of nitrogen per kg body weight per day; energy requirement was calculated using Harris and Benedict's equation, adding 300 kcal per day for activity. Twelve patients were treated with the structured triglyceride emulsion and 13 patients with the emulsion of the physical mixture of medium- and long-chain triglycerides. The design was a randomized, double-blind parallel study. RESULTS: In the patients who completed the study, the mean cumulative nitrogen balance over the first 5 postoperative days was -8+/-2 g in 10 patients on the structured triglyceride emulsion and -21+/-4 g in 9 patients on the emulsion of the physical mixture of medium- and long-chain triglycerides; the mean difference was 13 g of nitrogen (95% confidence interval 4 to 22, p = .015) in favor of the structured triglyceride emulsion. On the first postoperative day serum triglyceride and plasma medium-chain free fatty acid levels increased less during infusion of the structured triglyceride emulsion than with the physical mixture emulsion. CONCLUSIONS: The parenteral structured triglyceride emulsion improves the nitrogen balance and is cleared faster from the blood, compared with the emulsion of the physical mixture of medium- and long-chain triglycerides, in moderately catabolic patients.

Aged↗
PubMed2003

Rheology and stability of water-in-oil-in-water multiple emulsions containing Span 83 and Tween 80.

Multiple emulsions are often stabilized using a combination of hydrophilic and hydrophobic surfactants. The ratio of these surfactants is important in achieving stable multiple emulsions. The objective of this study was to evaluate the long-term stability of water-in-oil-in-water (W/O/W) multiple emulsions with respect to the concentrations of Span 83 and Tween 80. In addition, the effect of surfactant and electrolyte concentration on emulsion bulk rheological properties was investigated. Light microscopy, creaming volume, and rheological properties were used to assess emulsion stability. It was observed that the optimal surfactant concentrations for W/O/W emulsion long-term stability were 20% wt/vol Span 83 in the oil phase and 0.1% wt/vol Tween 80 in the continuous phase. Higher concentrations of Tween 80 had a destructive effect on W/O/W emulsion stability, which correlated with the observation that interfacial film strength at the oil/water interface decreased as the Tween 80 concentration increased. High Span 83 concentrations increased the storage modulus G' (solidlike) values and hence enhanced multiple emulsion stability. However, when 30% wt/vol Span 83 was incorporated, the viscosity of the primary W/O emulsion increased considerably and the emulsion droplets lost their shape. Salt added to the inner aqueous phase exerted an osmotic pressure that caused diffusion of water into the inner aqueous phase and increased W/O/W emulsion viscosity through an increase in the volume fraction of the primary W/O emulsion. This type of viscosity increase imposed a destabilizing effect because of the likelihood of rupture of the inner and multiple droplets.

Drug Stability↗