Effect of Lactobacillus acidophilus Fermented Broths Enriched with Eruca sativa Seed Extracts on Intestinal Barrier and Inflammation in a Co-Culture System of an Enterohemorrhagic Escherichia coli and Human Intestinal Cells.

Lactic acid bacteria (LAB) "fermentates" confer a beneficial effect on intestinal function. However, the ability of new fermentations to improve LAB broth activity in preventing pathogen-induced intestinal inflammation and barrier dysfunction has not yet been studied. The objective of this study was to determine if broths of LAB fermented with Eruca sativa or Barbarea verna seed extracts prevent gut barrier dysfunction and interleukin-8 (CXCL8) release in vitro in human intestinal Caco-2 cells infected with enterohemorrhagic Escherichia coli (EHEC) O157:H7. LAB broths were assayed for their effects on EHEC growth and on Caco-2 viability; thereafter, their biological properties were analysed in a co-culture system consisting of EHEC and Caco-2 cells. Caco-2 cells infected with EHEC significantly increased CXCL8 release, and decreased Trans-Epithelial Electrical Resistance (TEER), a barrier-integrity marker. Notably, when Caco-2 cells were treated with LAB broth enriched with E. sativa seed extract and thereafter infected, both CXCL8 expression and epithelial dysfunction reduced compared to in untreated cells. These results underline the beneficial effect of broths from LAB fermented with E. sativa seed extracts in gut barrier and inflammation after EHEC infection and reveal that these LAB broths can be used as functional bioactive compounds to regulate intestinal function.

Encapsulations of wild garlic (Allium ursinum L.) extract using spray congealing technology.

The objective of this study was to incorporate wild garlic (A. ursinum) extract into microparticles (MPs) in order to protect its valuable active compounds and improve its oral bioavailability. For this purpose, spray congealing technology was applied and Gelucire 50/13 (Stearoyl polyoxyl-32 glycerides) was selected as MPs carrier. MPs were characterized in terms of yield, encapsulation efficiency and particle size. Differential scanning calorimetry (DSC) and Fourier-transform infrared spectroscopy (FT-IR) analysis of MPs showed the absence of chemical interactions between carrier and extract and suggested that spray congealing process did not modify nor degrade the encapsulated extract. The encapsulation into MPs led to an improvement of the extract dissolution performance as well as an enhancement in solubility of >18 fold compared to the pure extract. Additionally, MPs were stable over three months showing only a minor decrease in the content of active compounds (allicin and S-methyl methanethiosulfonate) and maintaining a good antimicrobial activity. Therefore, obtained results suggested that the encapsulation of A. ursinum extract in MPs by spray congealing is a promising approach to improve the biopharmaceutical properties of the extract, without affecting its antibacterial activity.

Encapsulation of Vitamin A palmitate for animal supplementation: Formulation, manufacturing and stability implications.

Two manufacturing methods and numerous formulative approaches have been evaluated to obtain a stable oral pharmaceutical form of Vitamin A palmitate (VAP), a substance very sensitive to light, temperature, humidity and metal ions. The best results were obtained by formulating VAP, stabilized with butylated hydroxytoluene (BHT), in double layer microcapsules constituted by a core of chitosan, Tween 20, CaCl(2) and EDTA surrounded by a first chitosan-alginate membrane and an outer membrane of calcium-alginate. This formulation design enabled the production of beads with high drug loading (42% w/w) and high encapsulation efficiency (94%). The stability of VAP-loaded microcapsules was assessed according to EMEA guidelines. This formulation design showed the best performance in terms of VAP recovery (t(50%) > 360 days) after 1 year of storage at room conditions. This is a very important result considering the poor shelf-life (45 days) of pure VAP stabilized with BHT stored at the same conditions.

Evaluation of spray congealing as technique for the preparation of highly loaded solid lipid microparticles containing the sunscreen agent, avobenzone.

Solid lipid microparticles (SLMs) loaded with high amounts of the sunscreen agent, butyl methoxydibenzoylmethane (avobenzone) were prepared in order to reduce its photoinstability. The microparticles were produced, using carnauba wax as lipidic material and phosphatidylcholine as the surfactant, by the classical melt dispersion method or the spray congealing technique with pneumatic atomizer. The sunscreen agent loading was 40.1-48.5% (w/w), with no significant differences between the production methods. However, release studies indicated that spray congealing enabled a more efficient modulation of avobenzone release from the SLMs (26% of encapsulated avobenzone released after 2 h as compared to 60% for melt dispersion). The photoprotective efficacy of the SLMs was evaluated after their introduction in a model cream. A statistically significant decrease of the light-induced degradation of avobenzone was obtained by the SLMs prepared by the melt dispersion procedure (the extent of degradation was 38.6 +/- 3.6% for nonencapsulated avobenzone and 32.1 +/- 4.3% for the microparticle-entrapped sunscreen). On the other hand, the SLMs produced by spray congealing achieved a more marked reduction in avobenzone photodecomposition to 15.4 +/- 4.1%. Therefore, the spray congealing technique was superior to the classical melt dispersion method for rapid and solvent free production of SLMs with a high avobenzone loading capacity.

Evaluation of beta-lactose, PVP K12 and PVP K90 as excipients to prepare piroxicam granules using two wet granulation techniques.

The present investigation aimed at evaluating the use of different excipients, beta-lactose and polyvinylpyrrolidone of two molecular weights (PVP K12 and PVP K90), in the production of improved release piroxicam granules, by wet granulation using both water and steam as granulation liquid. The formulations examined were: piroxicam (Px)/beta-lactose; Px/PVP K12 and Px/PVP K90, each one at a 1:9 weight ratio. The most significant difference between beta-lactose and PVP is that, using the first excipient, both steam and water granules were produced while, when PVP were employed, only steam granules were obtained. Image analysis revealed that beta-lactose steam granules had a larger surface area with respect to water granules, whereas lower values of this parameter were observed in PVP-s granules, confirming the Scanning Electron Microscopy micrographs and the fractal analysis results. As regards the enhancement of the dissolution profiles, the best result was obtained using beta-lactose steam granules followed by PVP K12 ones, even if the reactive dimension values indicated that during the dissolution process PVP K12 granules modified the surface more than beta-lactose granules. As regards PVP K90, this excipient was the one less influencing the granule morphology and the dissolution behaviour. Differential Scanning Calorimetry analysis suggested the partial amorphisation of the drug in the granules containing the three excipients. This result was then confirmed by X-ray powder diffraction analysis. Therefore, beta-lactose and PVP K12 could be proposed as useful excipients to enhance the dissolution rate of Px from granules prepared using the steam granulation technique.