Water-in-oil organogel based emulsions as a tool for increasing bioaccessibility and cell permeability of poorly water-soluble nutraceuticals.

The use of organogels in food and pharmaceutical sciences has several technical problems related with restricted diffusion of the drugs and lack of a proper gelator molecule. These features are important into the new product design. An alternative to improve technological properties in organogels is the use of emulsions. However, there is a lack of knowledge about the behavior on bioaccessibility and permeability of bioactives loaded into organogel-based emulsions. The objective of the present experimental work was to study the physical properties of organogel-based emulsions made with vegetable oil loaded with three different bioactives (betulin, curcumin and quercetin) and the influence on their bioaccessibility. Organogels were made of canola or coconut oils and myverol as gelator (10% w/w). Water-in-oil emulsions (at 5, 10 and 12.5 wt% of water content) were prepared by mixing the melted proper organogel and water (80 °C) under high shear conditions (20,000 rpm). Micrographs, rheological tests (amplitude, frequency, temperature sweeps and creep-compliance measurements), DSC and particle size analysis were performed to samples. In vitro digestion (oral, gastric and intestinal phase), lipolysis assays, bioaccessibility and permeability tests by cell culture of Caco-2 were made. Organogels of coconut oil have shown poor emulsification properties.

Oak kombucha protects against oxidative stress and inflammatory processes.

Black tea infusion is the common substrate for preparing kombucha; however other sources such as oak leaves infusions can be used for the same purpose. Almost any white oak species have been used for medicinal applications by some ethnic groups in Mexico and could be also suitable for preparing kombucha analogues from oak (KAO). The objective of this research was to investigate the antioxidant activity and anti-inflammatory effects of KAO by examining its modulation ability on macrophage-derived TNF-alpha and IL-6. Herbal infusions from oak and black tea were fermented by kombucha consortium during seven days at 28 °C. Chemical composition was determined by LC-ESI-MS/MS. The antioxidant activity of samples against oxidative damage caused by H2O2 in monocytes activated (macrophages) was explored. Additionally, it was determined the anti-inflammatory activity using lipopolysaccharide (LPS) - stimulated macrophages; in particular, the nitric oxide (NO), TNF-alpha, and IL-6 production was assessed. Levels of pro-inflammatory cytokines IL-6 and TNF-alpha were significantly reduced by the sample treatment. Likewise, NO production was lower in treatment with kombucha and KAO compared with LPS-stimulated macrophages. Fermented beverages of oak effectively down-regulated the production of NO, while pro-inflammatory cytokines (TNF-alpha and IL-6) in macrophages were stimulated with LPS. Additionally, phytochemical compounds present in KAO decrease oxidative stress.

Morphological and release characterization of nanoparticles formulated with poly (dl-lactide-co-glycolide) (PLGA) and lupeol: In vitro permeability and modulator effect on NF-κB in Caco-2 cell system stimulated with TNF-α.

Lupeol exhibits anti-inflammatory effects; unfortunately it shows low water solubility. An alternative to overcome this is the development of nanomaterials. Several methods for nanomaterial production are available. One of them is emulsification/solvent-evaporation. The objective of the present work was to evaluate physical properties, transport and in vitro modulator effects on NF-κB of poly (lactide-co-glycolide) (PLGA) nanoparticles loaded with lupeol. Nanonutraceuticals were prepared with 16% (w/v) of lupeol. Size distribution and morphology were measured by particle size analyzer and TEM. In vitro release of lupeol was studied by three different models: Higuchi, Siepmann & Peppas, and Power law. Transport of nanonutraceutical was studied in a Caco-2 cell model and by GC-MS. Modulator effect on NK-κB was studied by western blot analysis. Nanonutraceuticals were 10% larger than the nanoparticles without lupeol (372 vs 337 nm) and presented a broader size distribution (0.28 vs 0.22). TEM results displayed spherical structures with a broader size distribution. Entrapment efficiency of lupeol was 64.54% and it in vitro release data fitted well to the Power law and Higuchi equation (R > 0.84-0.84). Strong regulation of NF-κB of nanonutraceutical was observed. It was not observed any transport across the Caco-2 cell model at the different experimental conditions.

Gastroprotective potential of Buddleja scordioides Kunth Scrophulariaceae infusions; effects into the modulation of antioxidant enzymes and inflammation markers in an in vivo model.

ETHNOPHARMACOLOGICAL RELEVANCE: A common plant used to treat several gastric disorders is Buddleja scordioides Kunth, commonly known as salvilla. AIM OF THE STUDY: To detect inflammatory markers, in order to evaluate the gastroprotective potential of salvilla infusions, as this could have beneficial impact on the population exposed to gastric ulcers and colitis. MATERIALS AND METHODS: The present work attempted infusions were prepared with B. scordioides (1% w/w) lyophilized and stored. Total phenolic content and GC-MS analysis were performed. Wistar rats were divided into five groups (n=8), a negative vehicle control, an indomethacin group, and three experimental groups, named preventive, curative, and suppressive. All rats were sacrificed under deep ether anesthesia (6h) after the last oral administration of indomethacin/infusion. The rat stomachs were promptly excised, weighed, and chilled in ice-cold and 0.9% NaCl. Histological analysis, nitrites quantification and immunodetection assays were done. RESULTS: B. scordioides infusions markedly reduced the visible hemorrhagic lesions induced by indomethacin in rat stomachs, also showed down-regulation of COX2, IL-8 and TNFα and up-regulation of COX-1 with a moderate down-regulation of NFkB and lower amount of nitrites. However, this behavior was dependent on the treatment, showing most down-regulation of COX-2, TNFα and IL-8 in the curative treatment; more down-regulation of NF-kB in the preventive treatment; and more up-regulation of COX-1 for the suppressor and preventive treatments. CONCLUSION: The anti-inflammatory potential of B. scordioides infusions could be related with the presence of polyphenols as quercetin in the infusion and how this one is consumed.

Physical properties of extruded products from three Mexican common beans (Phaseolus vulgaris L.) cultivars.

The physical properties of extruded products from three Mexican common bean cultivars were investigated. Common bean cultivars Flor de Mayo, Pinto Villa and Bayo Victoria from the same harvesting season (2006) were used in this work. Beans were milled and the flour was hydrated to 24, 26 and 28 g of water/100 g of dry weight. Two temperatures, 130 degrees C and 165 degrees C at the end of the extruder barrel without die, were experimented. Common bean flour extrudates were evaluated for water absorption index (WAI), water absorption capacity (WAC), oil absorption capacity (OAC), and emulsifying capacity (EC). Flor de Mayo extrudates showed the highest WAC and WAI values. Thus starch from Flor de Mayo beans showed minor restricted water availability. In all cases, the OAC of extruded products was lower than the crude bean flour. The EC for Bayo Victoria flour increased as a consequence of the extrusion process. The EC for Flor de Mayo was higher at lower temperature and lower moisture content than Pinto Villa and Bayo Victoria beans. EC behavior of Pinto Villa was similar to Bayo cultivar. These results indicate that it is possible to produce new extruded products with good physical properties from these common bean cultivars.

Phenolic diarylheptenones from Alnus rubra bark.

The novel diarylheptenone 1-(3',4'-dihydroxyphenyl)-7-(4''-hydroxyphenyl)-4-hepten-3-one and 1,7-bis( P-hydroxyphenyl)-4-hepten-3-one were isolated from Alnus rubra bark and their structures elucidated by spectrometric techniques.