Anna Kogan, Inna Popov, Vladimir Uvarov, Shmuel Cohen, Abraham Aserin, and Nissim. Garti. 2008. “Crystallization of Carbamazepine Pseudopolymorphs from Nonionic Microemulsions.” Langmuir, 24, 3, Pp. 722–733. Abstract
Crystn. of carbamazepine (CBZ), an antiepileptic drug, pptd. from confined spaces of nonionic microemulsions was investigated. The study was aimed to correlate the structure of the microemulsion [water-in-oil (W/O), bicontinuous, and oil-in-water (O/W)] with the cryst. structure and morphol. of solid CBZ. The pptd. CBZ was studied by DSC, TGA, powder x-ray diffraction, single-crystal x-ray diffraction, SEM, and optical microscopy. The results suggest that the microstructure of the microemulsions influences the crystn. process and allows crystg. polymorphs that exhibit different crystal structure and habits. W/O nanodroplets orient the crystg. CBZ mols. to form a prism-like anhyd. polymorphic form with monoclinic unit cell and P21/n space group. Bicontinuous structures lead to platelike dihydrate crystals with orthorhombic unit cell and Cmca space group. The O/W nanodroplets cause the formation of needlelike dihydrate crystals with monoclinic unit cell and P21/c space group. The morphol. features of solid CBZ remain predetd. by the basic symmetry and parameters of its unit cell. Pptn. of CBZ pseudopolymorphs from supersatd. microemulsion is discussed in terms of oriented attachment that provides perfect packing of numerous sep. nucleated ordered nuclei of CBZ into microscale platelets and then into macroscopic crystals. Crystn. from microemulsion media enabling one to obtain the drug (CBZ) with predicted structure and morphol. should be of great significance for pharmaceutical applications. [on SciFinder(R)]
Hyoungill Lee, Josh Rivner, Jeffrey L Urbauer, Nissim Garti, and Louise. Wicker. 2008. “De-esterification pattern of Valencia orange pectinmethylesterases and characterization of modified pectins.” Journal of the Science of Food and Agriculture, 88, 12, Pp. 2102–2110. Abstract
Pectinmethylesterase (PME, E.C.1.1.11) isoenzymes from Valencia orange prepns. with different specific activities were used to de-esterify citrus and sugar beet pectins. Enzymic modification offers the opportunity to create pectins of tailored functionality and gelling ability. Based on NMR spectra, catalysis by all PME exts. produced block-wise de-esterification patterns in both citrus and sugar beet pectins. PME activity resulted in increased nos. of contiguous de-esterified groups and decreased nos. of contiguous esterified groups. De-esterification by PMEs increased the elastic property (G') of citrus and sugar beet pectins in the presence of calcium from 10 to 571 and from 0.05 to 201 Pa, resp. The results demonstrate the predilection of citrus PMEs toward block wise de-esterification of pectins and the relationship between calcium binding ability and de-esterification degree and patterning. Within a narrow range of de-esterification (37-48%) and with a narrow distribution of contiguous groups, PME modification did not markedly change gelling ability. At lower or higher de-esterification values, a 2-fold increase or 50-fold decrease, resp. in G' values was obsd. [on SciFinder(R)]
Rivka Efrat, Deborah E Shalev, Roy E Hoffman, Abraham Aserin, and Nissim. Garti. 2008. “Effect of Sodium Diclofenac Loads on Mesophase Components and Structure.” Langmuir, 24, 14, Pp. 7590–7595. Abstract
We studied the effect of a model electrolytic drug on intermol. interactions, conformational changes, and phase transitions in structured discontinuous cubic QL lyotropic liq. crystals. These changes were due to competition with hydration of the lipid headgroups. Structural changes of the phase induced by solubilization loads of sodium diclofenac (Na-DFC) were investigated by directly observing the water, ethanol, and Na-DFC components of the resulting phases using 2H and 23Na NMR. Na-DFC interacted with the surfactant glycerol monoolein (GMO) at the interface while interfering with the mesophase curvature and also competed with hydration of the surfactant headgroups. Increasing quantities of solubilized Na-DFC promoted phase transitions from cubic phase (discontinuous (QL) and bicontinuous (Q)) into lamellar structures and subsequently into a disordered lamellar phase. Quadrupolar coupling of deuterated ethanol by 2H NMR showed that it is located near the headgroups of the lipid and apparently is hydrogen bonded to the GMO headgroups. A phase transition between two lamellar phases (L$\alpha$ to L$\alpha$*) was seen by 23Na NMR of Na-DFC at a concn. where the characteristics of the drug change from kosmotropic to chaotropic. These findings show that loads of solubilized drug may affect the structure of its vehicle and, as a result, its transport across skin-blood barriers. The structural changes of the mesophase may also aid controlled drug delivery. [on SciFinder(R)]
LA Shaw, H Faraji, T Aoki, D Djordjevic, DJ McClements, and EA Decker. 2008. “Emulsion droplet interfacial engineering to deliver bioactive lipids into functional foods.” In Delivery Controlled Release Bioact. Foods Nutraceuticals, Pp. 184–206. Woodhead Publishing Ltd. Abstract
A review. When bulk $ømega$-3 oils are added to foods, the oil will no longer be in a bulk form but will instead exist as an oil-in-water or water-in-oil dispersion. Most omega-3 oil processors add polar antioxidants to protect their bulk oil against oxidn. during storage. However, when the oil is then dispersed into foods, these antioxidants can partition into the aq. phase where they are ineffective and can be potentially prooxidative due to their ability to make transition metals more prooxidative. Use of oil-in-water emulsions to deliver $ømega$-3 fatty acids into functional foods may provide an alternative to bulk oils. [on SciFinder(R)]
CM Sabliov and CE Astete. 2008. “Encapsulation and controlled release of antioxidants and vitamins.” In Delivery Controlled Release Bioact. Foods Nutraceuticals, Pp. 297–330. Woodhead Publishing Ltd. Abstract
A review discusses the importance of antioxidants to human health, advantages of nanoencapsulation of these components over traditional delivery methods. Top-down techniques available to entrap antioxidants and vitamins in biodegradable and biocompatible polymeric nanoparticles are discussed, methods available for polymeric nanoparticle characterization are briefly mentioned, and some insights on the release profile of antioxidants and vitamins from polymeric nanoparticles are presented. [on SciFinder(R)]
K Kailasapathy. 2008. “Encapsulation and controlled release of folic acid.” In Delivery Controlled Release Bioact. Foods Nutraceuticals, Pp. 331–343. Woodhead Publishing Ltd. Abstract
A review discusses the delivery of microencapsulated folates through food such as cheese and its controlled release. [on SciFinder(R)]
A Millqvist-Fureby. 2008. “Encapsulation approaches for proteins.” In Delivery Controlled Release Bioact. Foods Nutraceuticals, Pp. 404–425. Woodhead Publishing Ltd. Abstract
A review discusses solid formulations for proteins, and in particular how spray drying can be used to encapsulate bioactive materials in solid formulations, and the application of polyelectrolyte multilayer microcapsules to protein encapsulation in liq. formulations. [on SciFinder(R)]
S.-J. Lee and DY Ying. 2008. “Encapsulation of fish oils.” In Delivery Controlled Release Bioact. Foods Nutraceuticals, Pp. 370–403. Woodhead Publishing Ltd. Abstract
A review describes the microencapsulation technologies and encapsulant materials used to deliver fish oils and the application of encapsulated fish oils in food products. It also discusses the benefits of fish oil and challenges of adding fish oils to foods. [on SciFinder(R)]
CP Champagne and K Kailasapathy. 2008. “Encapsulation of probiotics.” In Delivery Controlled Release Bioact. Foods Nutraceuticals, Pp. 344–369. Woodhead Publishing Ltd. Abstract
A review discusses the encapsulation technologies for probiotics. However, technologies applied to probiotics are generally limited to gel particles, spray-coating, spray-drying, extrusion and emulsions. [on SciFinder(R)]
Marina Shevachman, Nissim Garti, Arnon Shani, and Amnon C Sintov. 2008. “Enhanced Percutaneous Permeability of Diclofenac Using a New U-Type Dilutable Microemulsion.” Drug Development and Industrial Pharmacy, 34, 4, Pp. 403–412. Abstract
Enhanced systemic absorption in vivo and percutaneous penetration in vitro was demonstrated after transdermal administration of diclofenac sodium formulated in U-type microemulsion. Diclofenac sodium was solubilized in a typical four-component system consisting of an oil, polyoxyethylene-10EO-oleyl alc. (Brij 96V) as the surfactant, and 1-hexanol along water diln. line W46 (40 wt. % surfactant and 60 wt. % oil phase before water titrn.). Viscosity and small angle x-ray scattering measurements have evidenced bicontinuous structures within water fractions of 0.25 and 0.5 along the diln. line. Self-diffusion NMR studies showed that drug mols. accumulated in the interfacial film and, to some extent, dissolved in the oil. Relative to a com. macro-emulsion cream (Voltaren Emulgel), microemulsions contg. paraffin oil or iso-Pr myristate increased the in vivo transdermal penetration rate of diclofenac by two order of magnitude, whereas the rat plasma levels were increased by one order of magnitude. The in vitro data obtained from excised rat skin were comparable to the in vivo results, but suffered from discrepancies from the ideal in vivo-in vitro correlation, which might be explained by optimal in vitro conditions of perfusion and hydration. It has also been found that when jojoba oil is formulated as the oil phase in the microemulsion, the penetration rate of the drug decreases significantly. Based on the three-dimensional structure of jojoba oil, the wax is presumed to prevent the drug from being freely diffused into the skin while migrating from the interfacial film into the continuous oil phase. [on SciFinder(R)]
M Subirade and L Chen. 2008. “Food-protein-derived materials and their use as carriers and delivery systems for active food components.” In Delivery Controlled Release Bioact. Foods Nutraceuticals, Pp. 251–278. Woodhead Publishing Ltd. Abstract
A review illustrates the potential of food protein-based matrixes to serve as carriers for the controlled release of functional food components. It focuses on recent progress in the design, prepn. and evaluation of food-protein-based delivery systems based on hydrogel or micro- and nanoparticles and their potential for the development of innovative functional foods. [on SciFinder(R)]
Dima Libster, Paul Ben Ishai, Abraham Aserin, Gil Shoham, and Nissim. Garti. 2008. “From the Microscopic to the Mesoscopic Properties of Lyotropic Reverse Hexagonal Liquid Crystals.” Langmuir, 24, 5, Pp. 2118–2127. Abstract
The authors aimed to explore a correlation between the microstructural properties of the lyotropic reverse hexagonal phase (HII) of the GMO/tricaprylin/phosphatidylcholine/H2O system and its mesoscopic structure. The mesoscopic organization of discontinuous and anisotropic domains was examd., in the native state, using environmental SEM. The topog. of the HII mesophases was imaged directly in their hydrated state, as a function of aq.-phase concn. and compn., when a proline amino acid was solubilized into the systems as a kosmotropic (water-structure maker) guest mol. The domain structures of several dozen micrometers in size, visualized in the environmental SEM, possess fractal characteristics, indicating a discontinuous and disordered alignment of the corresponding internal H2O rods on the mesoscale. On the microstructural level, SAXS measurements revealed that as H2O content (Cw) increases the characteristic lattice parameter of the mesophases increases as well. Using the H2O concn. as the mass measure of the mixts., a scaling relation between the lattice parameter and the concn. was found to obey a power law whereby the derived fractal dimension was the relevant exponent, confirming the causal link between the microscopic and mesoscopic organizations. The topog. of the HII mesophase is affected by the microstructural parameters and the compn. of the samples. Thermal anal. expts. involving these systems further confirmed that the behavior of H2O underpins both microscopical and mesoscopic features of the systems. Both the swelling of the lattice parameter and the mesoscopic domains is correlated to the bulk H2O concn. in the H2O rods. [on SciFinder(R)]
N Garti. 2008. “The future of controlled release and delivery technologies.” In Delivery Controlled Release Bioact. Foods Nutraceuticals, Pp. 450–464. Woodhead Publishing Ltd. Abstract
A review. In some countries health authorities are advising minimizing the use of insol. solid nanoparticles that have been shown to cause some significant damage to the healthy growth of various cells and to decrease the viability of others. However, companies and those dealing with future foods prefer to conc. on delivery methods and technologies and to refrain from using the term nanosized particles. All the technologies will involve utilization of new encapsulation and entrapment of bioactives and other food additives by advanced encapsulation micro- and nanovehicles. [on SciFinder(R)]
Roy E Hoffman, Hilla Arzuan, Chava Pemberton, Abraham Aserin, and Nissim. Garti. 2008. “High-resolution NMR "chromatography" using a liquids spectrometer.” Journal of Magnetic Resonance, 194, 2, Pp. 295–299. Abstract
NMR spectroscopy is an excellent tool for the structural anal. of pure compds. However, for mixts. it performs poorly because of overlapping signals. Diffusion can be used to sep. compds. of widely differing mol. wt. but the amt. of sepn. is usually insufficient. Addn. of a solid medium, analogous to the stationary phase in chromatog., can preferentially slow the diffusion of some components of a mixt. permitting sepn. in the diffusion dimension. However, this would usually require a solid-state NMR spectrometer otherwise the signals would be too broad. Susceptibility matching the solvent to the solid medium yields a spectrum with narrow signals allowing the measurement of a DOSY spectrum with enhanced sepn. in the diffusion dimension. [on SciFinder(R)]
Rachel Lutz, Hagit Pikarek, Abraham Aserin, and Nissim. Garti. 2008. “Hydrocolloids in relation to their emulsification activity - WPI/hydrocolloid complexes.” Foods & Food Ingredients Journal of Japan, 213, 3, Pp. 216–228. Abstract
The present manuscript is in two parts. In the first part we characterize a new sol. complex (hybrid) formed in aq. soln. from WPI and the hydrocolloids (xanthan, pectin, and LBG), while in the second we demonstrate the advantage of the complexes as amphiphilic biopolymers utilized for steric and depletion stabilization of emulsions and multiple emulsions. It was found that the major factor affecting the formation of a sol. complex (hybrid) of the WPI and the hydrocoltoids is the intermol. charge interactions and not the Mw of the two biopolymers. The best concn. and ratio of WPI and the hydrocolloids (pectin and xanthan) to form the sol. complex are 4 wt% WPI and 0.5-1.0 wt% of the hydrocolloids. The interactions are between some mol. pos. charged patches on the protein and neg. charged fractions of the hydrocolloids. The WPI/hydrocolloid complex can provide good steric stabilization to the external interface of an emulsion and double emulsion. The droplets stabilized with the complex are smaller than those stabilized with WPI alone. Good creaming stability was also obtained. [on SciFinder(R)]
S Rozner, L Verkhovski, Y Nissimov, A Aserin, R Vilensky, D Danino, CC Zouboulis, Y Milner, and N Garti. 2008. “Inhibition of cholesterol transport into skin cells in cultures by phytosterol-loaded microemulsion.” Chemistry and Physics of Lipids, 153, 2, Pp. 109–118. Abstract
Cholesterol and plant phytosterols are lipophilic compds. solubilized by intestinal micelles in a competitive manner. In this work, we used radioactive cholesterol- and phytosterol-loaded oil-in-water microemulsions to follow their incorporation and mutual competition in HaCaT keratinocytes, SZ95 sebocytes, and skin pieces in cultures. Dynamic light scattering showed homogeneous nanostructures of 10.5 ± 1.5 nm diam. and cryo-transmission electron microscopy confirmed the presence of uniform spherical droplets of 7.0 ± 1.0 nm diam. Up to 320 nmol/mL of cholesterol can be solubilized and transported into cells with minimal toxic effect by 0.5 wt.% nanodroplets in a cell medium. Phytosterols inhibit incorporation of cholesterol into cells, in vitro, at molar ratios (phytosterols/cholesterol) of 4 and above. The loaded nanodroplets accumulate in intracellular vesicles (presumably endosomes). No metabolic conversion of cholesterol or phytosterols was found in these cells, in vitro, after 24 h, at 37°. [on SciFinder(R)]
O Ramon and D Danino. 2008. “Lipid self-assembled particles for the delivery of nutraceuticals.” In Delivery Controlled Release Bioact. Foods Nutraceuticals, Pp. 207–233. Woodhead Publishing Ltd. Abstract
A review discusses the principles of lipid self-assembling systems, their integration in the mainframe of the packing concept of Israelachvili and coworkers, thermodn. constraints, and physico-chem. properties. [on SciFinder(R)]
J Barauskas and T Nylander. 2008. “Lyotropic liquid crystals as delivery vehicles for good ingredients.” In Delivery Controlled Release Bioact. Foods Nutraceuticals, Pp. 107–131. Woodhead Publishing Ltd. Abstract
A review focuses on how the non-lamellar liq. cryst. phase can be turned into well-defined LCNP that can be used to entrap compds. with low aq. soly. as well as hydrophilic compds. It also discusses the stability of the compds. in terms of hydrolysis as well as what happens when these particles interact with an interface. [on SciFinder(R)]
N Garti and I Yuli-Amar. 2008. “Micro- and nano-emulsions for delivery of functional food ingredients.” In Delivery Controlled Release Bioact. Foods Nutraceuticals, Pp. 149–183. Woodhead Publishing Ltd. Abstract
A review discusses the impact of the nanotechnol. on food preservation, food quality, and on nutrition and health aspects. [on SciFinder(R)]