Simulated Salivary Fluid Research Articles

Observation and Analysis of In Vitro Digestibility of Different Breads Using a Human Gastric Digestion Simulator.

The digestion behavior of a food bolus comprising bread particles in the presence of gastric peristalsis remains poorly understood. This study systematically investigated the effect of bread type on in vitro gastric digestion behavior using a human gastric digestion simulator (GDS) that is capable of quantitatively simulating gastric peristalsis. A food bolus consisting of 60 g of bread (white bread, bagel, German bread, French bread, or croissant), 15 mL of a simulated salivary fluid, and 240 mL of a simulated gastric fluid was used for gastric digestion in vitro using the GDS for 3 h at 37 °C. Direct observation of the gastric digestion behavior in the GDS vessel demonstrated that the structure and composition of breads considerably influenced the physical digestion processes of bread particles. These processes include their fracture, rubbing, disintegration, swelling owing to the penetration of gastric fluid, and release of fat from their surface. Fluorescence microscopy enabled an improved understanding of the variations in the microstructure and major component distribution of the breads during the gastric digestion in vitro. The results showed how the different breads influenced gastric digestibility in vitro through quantitative gastric peristalsis. The GDS can also be applicable to studying gastric digestibility in vitro of other types of bread.

Impact of saliva incorporation on the rheological properties of in vitro gastric contents formulated from sour cream.

Rheological properties of gastric contents depend on the food ingested, and on the volume and composition of secretions from the host, which may vary. This study investigates the impact of saliva regular incorporation in the stomach after a meal on the rheological properties of gastric contents, considering two levels of salivary flow (low = 0.5 and high = 1.5 mL/min). In vitro chymes were obtained by mixing sour cream, simulated gastric fluid, two different volumes of oral fluid (at-rest human saliva, SSF for Simulated Salivary Fluid or water) and adjusting pH at 3. Chymes samples were characterized at 37°C for their particle size and rheological properties. Overall, particle size distribution was not different between samples: incorporating a larger volume of saliva resulted in more heterogeneity, but the surface area moment D[3,2] and volume moment D[4,3] did not differ significantly with the oral fluid type. Shear viscosity of chyme samples was higher when saliva was incorporated, in comparison with water or SSF. In addition, as shown from data extracted at = 20 s-1 the higher the fluid volume the lower the shear viscosity, which is attributed to a dilution effect. However, this dilution effect was attenuated in the case of saliva, most likely due to its composition in organic compounds (e.g., mucins) contributing to the rheological properties of this biological fluid. In these in vitro conditions, both saliva and the salivation rate had a significant but slight impact on the rheological properties of gastric contents (of the order of 1-5 mPa s at = 20 s-1).

A biorelevant test for tablets glycine sublingual in the «simulated saliva» dissolution medium

Introduction. Biorelevant dissolution media reconstitute the composition of the contents of the gastrointestinal tract. They are used as dissolution media in the evaluation of dissolution profiles of different dosage forms. Simulated biological fluids allow prediction of in vivo test results. The development of the composition of simulated salivary fluid allows the evaluation of drug properties under physiologically relevant conditions.Aim. Evaluation of the release of the drug product "glycine, sublingual tablets, 100 mg", domestically produced in Simulated Saliva 5 pH 6.8.Materials and methods. The preparations used for analysis were: «Glycine, sublingual tablets, 100 mg», domestically produced with valid expiration date. Comparative dissolution kinetics test was carried out on the dissolution test apparatus DT 6 (ERWEKA GmbH, Germany). Chromatographic separation and detection were performed on a Waters W1525 Binary HPLC Pump high-performance liquid chromatograph (Waters Corporation, USA) equipped with column and sample thermostat, degasser, autosampler and Waters 2487 Dual Absorbance Detector (Waters Corporation, USA). Detection was performed at a wavelength of 254 ± 2 nm after derivatization of the glycine molecule with 4-toluenesulfonyl chloride. A Grace Platinum C18-EPS 5 μm 4.6 × 250 mm Grace Platinum C18-EPS 5 μm 4.6 × 250 mm column (Grace, USA) and a Grace Platinum C18-EPS 5 μm 4.6 × 250 mm pre-column (Grace, USA) were used. The following software was used for the study: validated Microsoft Excel spreadsheet for calculating glycine release values.Results and discussion. The technique for quantitative determination of glycine was developed and validated under CDKT in purified water medium and Simulated Saliva 5 pH 6.8. The validated analytical range of the methodology was 10–110 % of the nominal concentration of the dosage form in 300 mL volume of medium. The developed analytical technique was validated in the biopredictive in vitro test of glycine preparations. During the study in Simulated Saliva medium for drug formulations, more discriminative data were obtained, which were expressed as: different dissolution rate, curvature of the slope of the dissolution profile and time to reach the plateau in contrast to the dissolution medium purified water.Conclusion. The quantification technique was developed and validated for biopredictive tests of tablets "Glycine, sublingual tablets, 100 mg". The analytical range of the technique was 10–110 % of the nominal concentration of the dosage form in 300 mL volume of medium. The results of the test in artificial saliva medium were more discriminatory.

Functionalization of sterculia gum for making platform hydrogels via network formation for use in drug delivery

Recently, various advancements have been made in the development of functional polymeric materials for innovative applications. Herein this work, functionalization of sterculia gum (SG) was carried out via grafting of poly(2-(methacryloyloxy) ethyltrimethylammonium chloride) (METAC)-polyvinyl pyrrolidone (PVP) to develop hydrogel dressings as a platform for use in drug delivery (DD). The innovation of the present work is the exploration of inherent antioxidant and antimicrobial properties of the SG along with antimicrobial characteristic of poly(METAC) and PVP, to design the doxycycline encapsulated hydrogel dressings for better wound healing. FESEM, EDS and AFM analyzed the surface morphology of hydrogels. FTIR, 13C NMR and XRD inferred inclusion of poly(METAC)-PVP into polymers. 13C NMR confirmed the incorporation of poly(METAC) and PVP onto gum by the presence of a peak at 54.74 ppm because of methyl carbon attached to quaternary nitrogen of poly(METAC) and at 45.48 ppm due to the ring carbon of PVP along with FTIR peak at 949 cm−1 because of CN bending of quaternary nitrogen of poy (METAC). Thermal characterization of copolymers has been performed using TGA analysis. One gram of copolymeric hydrogel dressing absorbed 6.51 ± 0.03 g simulated salivary fluid (SSF) and 7.65 ± 0.03 g simulated wound fluid (SWF). Release of doxycycline drug occurred in a sustained manner and followed the Non-Fickian diffusion mechanism from hydrogels. The release profile was most effectively described by Hixon-Crowell kinetic model. Hydrogel demonstrated biocompatibility and expressed thrombogenicity 79.7 ± 4.9 % during its polymer-blood interactions. Copolymer revealed mucoadhesive property, requiring a force of 77.00 ± 0.01 mN to detach from bio-membrane. Additionally, it exhibited antioxidant features, showing 43.81 ± 0.286 % free radical scavenging. Hydrogel dressings were mechanically stable and revealed 0.76 ± 0.09 N mm−2 tensile strength and 9.18 ± 0.01 N burst strength. Polymer films were permeable to oxygen and water vapor and were impermeable to microorganisms. Hydrogel dressings exhibited antimicrobial properties against Pseudomonas aeruginosa and Staphylococcus aureus bacteria. Overall, these properties displayed the suitability of hydrogels for wound dressing (WD) applications which may actively enhance wound healing.

Semisolid extrusion 3D printing of Dolutegravir-Chitosan nanoparticles laden polymeric buccal films: personalized solution for pediatric treatment.

In this work, the semi solid extrusion 3D printing process was utilized to incorporate anti-HIV drug Dolutegravir and its nanoparticles into the buccal film (BF) that was fabricated using the developed polymer ink. The composite made of polyvinyl alcohol (PVA) and sodium alginate was processed into a 3D printing polymer ink with optimum viscosity (9587 ± 219 cP) needed for the seamless extrusion through the nozzle of the 3D printer. The formulated BFs were assessed for its physical properties like weight (0.414 ± 0.3 g), thickness (1.54 ± 0.02 mm), swelling index (18.5 ± 0.91%), and mucoadhesiveness strength (0.165 ± 0.09 N) etc, The structural integrity and the surface morphology of the developed BFs were investigated by scanning electron microscopy analysis. The chemical stability and the solid-state nature of the drug in the BFs were assessed by Fourier transform infrared and x-ray diffraction analysis respectively. Further the BFs were assessed for drug dissolutionin-vitroandex-vivo, to study the effect of polymer composition and printing condition on the dissolution profile of the drug in the simulated salivary fluid. The results demonstrated that the developed PVA based polymer ink for 3D printing utilizing pressure is a versatile approach in the context of manufacturing mucoadhesive BFs customized in terms of shape and the amount of drug loaded.

The Behavior of Phenolic Compounds from Apples during Simulated Gastrointestinal Digestion with Focus on Chlorogenic Acid.

The fate of phenolic compounds during digestion is important for their bioactive effects in the digestive tract. The aim was to study the various phenolic compounds occurring in the peel and flesh of apples in in vitro simulated gastrointestinal digestion, focusing on the behavior of chlorogenic acids. Additionally, the behavior of individual chlorogenic acids (chlorogenic, neochlorogenic, and cryptochlorogenic) was studied in models of simulated salivary, gastric, and intestinal fluid electrolyte solutions (SSF, SGF, SIF). At the end of the intestinal phase of the digestion of peel and flesh, the amount of recovered dihydrochalcones and flavonols increased or was similar to the amount in the gastric phase, which showed their stability. Anthocyanins and flavan-3-ols decreased, which suggests their biotransformation. Chlorogenic acid isomerized into neochlorogenic and cryptochlorogenic acid: chlorogenic acid from the peel into 22% and 41% of the isomers in the salivary and intestinal phases, respectively; chlorogenic acid from the flesh into 12% of the isomers in the intestinal phase. Similarly, chlorogenic acid isomerized in model solutions (20% and 26% of the isomers in SSF and SIF, respectively). Neochlorogenic and cryptochlorogenic acid isomerized in SSF and SIF into other two forms. They were all stable in SGF. For bioactive effects in the digestive tract, the biotransformation of chlorogenic acids should be considered.

Solvent-Free Method for Masking the Bitter Taste of Azithromycin Dihydrate Using Supercritical Fluid Technology

ABSTRACT Introduction and purpose The unpleasant extremely bitter taste of the orally administered broad-spectrum antibiotic azithromycin decreases patient compliance, especially in pediatrics. This issue can be overcome by decreasing drug interaction with the tasting buds using insoluble polymers at salivary pH (6.8 -7.4), like the cationic polymer Eudragit EPO. Supercritical fluid technology is a green synthesis method for preparing pharmaceutical preparations that replace organic solvents with safe supercritical CO2. This study aimed to mask the bitter taste of azithromycin using the supercritical fluid method and a pH-sensitive Eudragit EPO polymer. Methods: A foaming process was investigated for preparing a formulation (TEST), which comprises treating the polymer with supercritical carbon dioxide (CO2) fluid to prepare a taste-masked dosage form without employing organic solvents or flavors. Results: The use of the supercritical technique at 40 °C and 10 MPa for two hours allowed the manufacturing of solvent-free polymeric foam with azithromycin dispersions; the average calculated percentage of apparent volume change was 62.5 ± 5.9% with an average pore diameter of 34.879 Å. The formulated sample showed low drug release in simulated salivary fluid while keeping its crystalline nature. Moreover, clinical studies on healthy subjects showed that the formula successfully masked azithromycin's bitter taste. Conclusions: Overall, it has been shown herein that the supercritical fluid technology foaming method is promising in masking the bitter taste of bitter ingredients.

Comparison between solvent evaporation and supercritical CO2 technology in taste-masking of Azithromycin bitter-taste using pH-sensitive Eudragit EPO or Eudragit S100 polymers

Despite the broad spectrum of the antibiotic Azithromycin, its extremely bitter taste after oral dosing decreases patient compliance. This bitter taste can be masked by minimizing Azithromycin interaction with the tasting buds using polymers that are insoluble at salivary pH (6.8–7.4), like the cationic polymers Eudragit EPO and Eudragit S100. The purpose of this study was to employ two different techniques (solvent evaporation (SE) and supercritical fluid technology (SFT)) for encapsulating Azithromycin into Eudragit microparticles to mask its bitter taste. The formulations were characterized using Fourier-transform infrared spectroscopy (FTIR(, powder X-ray diffraction (PXRD), Differential scanning calorimetry (DSC), and scanning electron microscope (SEM). Also, the Azithromycin in vitro release and in vivo assessment of bitter taste masking were conducted. The present work showed promising results in veiling the bitter taste of Azithromycin. Taste panel scores for the in vivo clinical taste study of the formulation prepared using SE was 0.3 after 30 seconds compared to Azithromycin, resulting in a score of 3 owing to its palpable bitter taste. Whereas drug-Eudragit EPO showed no interaction, FTIR results indicated azithromycin interaction with Eudragit S100. The formulation prepared by the SE method and Eudragit EPO showed efficient taste masking, within-matrix encapsulation, lower drug release in simulated salivary fluid (SSF, <2% released over 60 seconds), and loss of Azithromycin’s crystallinity. On the contrary, SFT had higher encapsulation efficiency (91%) but faster in vitro release (6% released over 60 seconds). Thus, SE was better than SFT in Azithromycin taste masking using Eudragit EPO.

Transformation of Nano-Size Titanium Dioxide Particles in the Gastrointestinal Tract and Its Role in the Transfer of Nanoparticles through the Intestinal Barrier.

In this work, the size transformation of the TiO2 nanofraction from pharmaceutical grade E171 powder was studied during its transit through the gastrointestinal tract (GIT). It was shown that pharmaceutical-grade TiO2 powder contained about 0.68% (w/w) of particles smaller than 240 nm in diameter. In the observed GIT transit process the TiO2 nanoparticles were agglomerated up to 150-200 nm in simulated salivary fluid, with gradual agglomerate enlargement up to 300-600 nm and more than 1 micron in simulated gastric fluid. In the intestinal fluid the reverse process occurred, involving a decrease of agglomerates accompanied by the formation of a small fraction with ~50 nm average size. This fraction can be further involved in the histohematic transport process. The acidity degree (pH) and mineral composition of solutions, as well as the transit speed along the gastrointestinal tract, influence the nature of the particle transformation significantly. The rapid passing between the gastrointestinal tract sections creates conditions for a decrease in part of the TiO2 particles, up to 100 nm, and may be associated with the violation of the structural and functional integrity of the intestinal mucus layer.

DEVELOPMENT OF ORODISPERSIBLE TABLETS OF LORATADINE CONTAINING AN AMORPHOUS SOLID DISPERSION OF THE DRUG IN SOLUPLUS® USING DESIGN OF EXPERIMENTS

Objective: The objective of the present work was to develop an orodispersible tablet of loratadine, an orally active, non-sedating anti-histaminic, belonging to BCS Class II. The drug was prepared as a solid dispersion using Soluplus® as carrier and formulated into an optimal tablet using Design of Experiments. Methods: Solid dispersions of loratadine with varying ratios of Soluplus® were prepared by solvent evaporation and subjected to solubility study in simulated salivary fluid. Selected composition was characterized by differential scanning calorimetry and X-ray diffraction and formulated into an orodispersible tablet by direct compression after addition of suitable excipients. DOE based on a full factorial design was used to optimize the product using a trial version of JMP software, so as to obtain a tablet with low friability, rapid disintegration and maximal drug dissolution within 5 min. The optimized tablet was prepared and evaluated for several attributes, including in vivo disintegration and palatability. Results: A solid dispersion prepared with a 1: 4 ratio of loratadine: Soluplus® was found to show a 130-fold increase in drug solubility in the simulated salivary fluid. X-ray diffraction revealed loratadine in amorphous form. The exercise using DOE for optimization of the orodispersible tablet formula served to balance the proportion of crospovidone as super disintegrant and PVP as dry binder and yielded a formulation with good mechanical strength, rapid in vitro disintegration (39 sec) and dissolution of 93.78% of the drug within 5 min. When evaluated in vivo, the tablets were found to disintegrate in about 60 secs and were reported to be palatable. Conclusion: A patient-friendly dosage form containing a highly soluble form of loratadine was prepared and could be of potential benefit in offering quick relief from allergic conditions.

Nano- and Micro-Encapsulation of Long-Chain-Fatty-Acid-Rich Melon Seed Oil and Its Release Attributes under In Vitro Digestion Model.

Melon seed oil (MSO) possesses plenty of long-chain fatty acids (LFCAs, oleic-linoleic acid 90%), remarkable antioxidant activity (DPPH (0.37 ± 0.40 µmol TE/g), ABTS (4.98 ± 0.18 µmol TE/g), FRAP (0.99 ± 0.02 µmol TE/g), and CUPRAC (4.94 ± 0.11 µmol TE/g)), and phenolic content (70.14 ± 0.53 mg GAE/100 g). Encapsulation is a sound technology to provide thermal stability and controlled release attributes to functional compounds such as plant seed oil. Nano-sized and micro-sized capsules harboring MSO were generated by utilizing thin film dispersion, spray drying, and lyophilization strategies. Fourier infrared transform analysis (FTIR), scanning electron microscopy (SEM), and particle size analyses were used for the authentication and morphological characterization of the samples. Spray drying and lyophilization effectuated the formation of microscale capsules (2660 ± 14 nm, 3140 ± 12 nm, respectively), while liposomal encapsulation brought about the development of nano-capsules (282.30 ± 2.35 nm). Nano-liposomal systems displayed significant thermal stability compared to microcapsules. According to in vitro release studies, microcapsules started to release MSO in simulated salivary fluid (SSF) and this continued in gastric (SGF) and intestinal (SIF) environments. There was no oil release for nano-liposomes in SSF, while limited release was observed in SGF and the highest release was observed in SIF. The results showed that nano-liposomal systems featured MSO thermal stability and controlled the release attributes in the gastrointestinal system (GIS) tract.

Matrices of Native and Oxidized Pectin and Ferrous Bisglycinate and Their In Vitro Behavior through Gastrointestinal Conditions

Colloidal matrices of native and oxidized pectin were developed to improve iron bioavailability through the digestive tract. Ferrous bisglycinate (Gly-Fe), obtained by precipitation of glycine chelation to Fe2+, was mixed with native and peroxide-oxidized citrus pectin, and subsequently lyophilized. Controls included matrices with iron and glycine without chelation. The resulting samples were characterized through FTIR, SEM, and TGA/DSC before and after in vitro digestion, which was performed in simulated salivary, gastric, and intestinal fluids. During these digestions, swelling capacity and iron release were assessed. All matrix formulations were porous, and while pectin oxidation did not alter architecture, it changed their properties, increasing thermal stability, likely due to greater number of interaction possibilities through carbonyl groups generated during oxidation. This also resulted in lower swelling capacity, with greater stability observed when using the chelated complex. Higher swelling was found in gastric and intestinal fluids. Pectin oxidation also increased retention of the chelated form, contrary to what was observed with unchelated iron. Thus, there is an important effect of pectin oxidation combined with iron in the form of ferrous biglyscinate on matrix stability and iron release through the digestive tract. These matrices could potentially improve iron bioavailability, diminishing organoleptic changes in fortified iron foods.

Prebiotic properties of isomaltooligosaccharides from cassava as a potential ingredient in high-protein drinks for athletes

Background: Studies show that prebiotics can improve the health of athletes. Isomaltooligosaccharide (IMO) is a food ingredient containing prebiotic properties.Objectives: The purpose of the study is to examine the prebiotic properties of isomaltooligosaccharides based on digestibility of in vitro under-simulated upper-gut conditions and a prebiotic activity score. Additionally, the study explores the potential to use IMO as an ingredient for high protein drinks.Methods: IMO powder from cassava starch was prepared through enzymatic methods. The prebiotic properties of IMO were evaluated based on in vitro digestibility and a prebiotic activity score. Researchers assessed the digestibility of in vitro in simulated upper-gastrointestinal-tract conditions, consisting of mouth digestion, gastric digestion, and small-intestine digestion. The study calculated the probiotic activity score according to the number of growing beneficial and harmful bacteria. Finally, researchers determined the potential to use IMO as an ingredient for developing high-protein drink products.Results:The digestion of IMO by simulated salivary fluid using human salivary α-amylase for 2 min, artificial human gastric juice at pH 2.0 for two hours, intestinal fluid with pancreatic α-amylase (0.75 unit/mL), and pancreatic lipase (1.6 unit/mL) for two hours with a pH of 6.9 and a temperature of 37 oC were 1.54±0.33%, 9.19±0.64%, and 33.27±4.09%, respectively. Comparing the results with commercial isomaltooligosaccharide (cIMO), researchers found that the percentage of digestion differed significantly. Prebiotic activity scores of IMO for L. rhamnosus LGG®, L. paracasei CASEI 431®, L. acidophilus LA 5, B. longum DSM 219, B. animalis subsp. BB12® and B. bifidum BB536 were 0.477±0.07, 2.197±0.58, -0.058±0.16, 1.660±0.63, 0.801±0.59 and 1.179±0.05, respectively. Notably, the results were not significant when compared to cIMO. Researchers measured the nutritional formula in a high-protein drink containing IMO at 40 g (30 g protein) and the total serving at 148 kcal. For macronutrient distribution, the ratio of protein, carbohydrate, and fat in the product is 81:19:0. Micronutrients were added, comprising of 0-50% Thai RDI. Finally, the product also met relevant standards for the microbial quality of food products in powdered form. Conclusion:IMO from cassava was partially resistant to in vitro digestion under simulated upper-gastrointestinal conditions and promoted the growth of probiotic bacteria. Moreover, powdered IMO can be used as an ingredient for high-protein drink products.Keywords: prebiotic, probiotic, high protein drinking, athletes, IMO

Chitosan-coated nanoliposomes for efficient delivery of betanin with enhanced stability and bioavailability

Betanin is a high-value health-promoting food ingredient. However, the bioavailability of betanin is constrained by its low stability. In this study, for the first time, betanin was stabilized and delivered using chitosan-coated nanoliposomes (CC-NLs). The CC-NLs were firstly synthesized and characterized. The results showed that increasing chitosan concentration from 0% to 1.0% increased particle size of CC-NLs from 156.4 nm to 217.2 nm. With the use of CC-NLs prepared with 0.6% chitosan, it was found that increasing pH from 1.5 to 9.0 reduced zeta potential of CC-NLs from 8.62 mv to-9.65 mv while the average size of CC-NLs of 221.40 nm peaked at pH 5.5. In aqueous solution, 29.0% of loaded betanin was released from NLs compared to 15.8% from CC-NLs. The in vitro digestion analysis indicated that uncoated NLs and CC-NLs had similar stabilities and relatively stable in oral and gastric fluids. However, in intestinal fluid, the average size of both NLs and CC-NLs were significantly reduced due to bile salt and trypsin. Furthermore, in vitro antioxidant activity assay results showed that betanin delivered by CC-NLs had the highest ORAC and PSC values. This study demonstrated that betanin could be efficiently delivered by CC-NLs with improved stability and bioavailability. The information generated from this study is very useful for the applications of betanin in functional food, pharmaceutical and cosmetics industry. • Betanin was succussfully loaded on chitosan-coated nanoliposomes (CC-NLs). • Controlled release of betanin from CC-NLs was achieved. • CC-NLs were stable in simulated salivary and gastric fluids and were digested in simulated intestinal fluid. • Betanin delivered by CC-NLs had the highest in vitro and cellular antioxidant activities.

Fabrication of Hydroxypropyl Methylcellulose Orodispersible Film Loaded Mirtazapine Using a Syringe Extrusion 3D Printer

Depression is a mental illness causing a continuous negative feeling and loss of interest and affects physical and mental health. Mirtazapine (MTZ) is an effective medicine for treating depression, but patients lack compliance. However, transforming a pharmaceutical dosage form to an orodispersible film (ODF) could resolve this issue. This study aims to fabricate ODF-loading mirtazapine, using a syringe extrusion 3D printer, and compare its properties with the solvent-casting method. The ODFs were prepared by dissolving the mirtazapine in a hydroxypropyl methylcellulose E15 solution, and then fabricated by a 3D printer or casting. The 3D printing was accurate and precise in fabricating the ODFs. The SEM micrographs showed that the mirtazapine-printed ODF (3D-MTZ) was porous, with crystals of mirtazapine on the film’s surface. The 3D-MTZ exhibited better mechanical properties than the mirtazapine-casted ODF (C-MTZ), due to the 3D-printing process. The disintegration time of the 3D-MTZ in a simulated salivary fluid, pH 6.8 at 37 °C, was 24.38 s, which is faster than the C-MTZ (46.75 s). The in vitro dissolution study, in 0.1 N HCl at 37 °C, found the 3D-MTZ quickly released the drug by more than 80% in 5 min. This study manifested that 3D-printing technology can potentially be applied for the fabrication of ODF-containing mirtazapine.

Bioaccessibility of Plant Sterols in Wholemeal Rye Bread Using the INFOGEST Protocol: Influence of Oral Phase and Enzymes of Lipid Metabolism.

Bioaccessibility of plant sterols (PS) in an enriched wholemeal rye bread was evaluated, for the first time, using the INFOGEST protocol without gastric lipase (GL) and cholesterol esterase (CE), with GL or GL + CE. Moreover, human chewing and an in vitro oral phase (simulated salivary fluid and α-amylase) were evaluated for this purpose. The addition of GL decreased the bioaccessibility of total PS (from 23.8 to 18.5%), whereas the use of GL + CE does not significantly affect PS bioaccessibility. The in vitro oral phase resulted in an ineffective homogenization of the fresh vs partially dried and milled bread, reducing the bioaccessibility of total (from 20.2 to 12.8%) and individual PS. The INFOGEST digestion including the use of GL and CE, as well as an oral phase with human chewing, is proposed for the assessment of PS bioaccessibility in a solid matrix such as wholemeal rye bread since it more closely approximates the in vivo situation.

Survival of human coronavirus 229E at different temperatures on various food-contact surfaces and food and under simulated digestive conditions

The COVID-19 pandemic caused by SARS-CoV-2 has had a major impact on human health and the global economy. Various transmission possibilities of SARS-CoV-2 have been proposed, such as the surface of food in the cold chain and food packaging, as well as the fecal-oral route, although person-to-person contact via droplets and aerosols has been confirmed as the main route of transmission. This study evaluated the survivability of HCoV-229E, a SARS-CoV-2 surrogate, in suspension, on food-contact surfaces and on food at various temperatures, and in simulated digestive fluids by TCID50 assay. In suspension, HCoV-229E survived after 5 days at 20 °C with a 3.69 log reduction, after 28 days at 4 °C with a 3.07 log reduction, and after 12 weeks at –20 °C with a 1.18 log reduction. On food-contact surfaces, HCoV-229E was not detected on day 3 on stainless steel (SS), plastic (LDPE), and silicone rubber (SR) at 20 °C with a 3.28, 3.24 and 3.28 log reduction, respectively, and survived after 28 days on SS and LDPE at 4 °C with a 3.13 and 2.88 log reduction, respectively, and survived after 12 weeks on SS, LDPE, and SR at –20 °C with a 1.92, 1.32 and 1.99 log reduction, respectively. On food, HCoV-229E was not detected on day 3 on lettuce and day 4 on chicken breast and salmon at 20 °C with a 3.61, 3.26 and 3.08 log reduction, respectively, and on day 14 on lettuce and day 21 on chicken breast and salmon at 4 °C with a 3.88, 3.44 and 3.56 log reduction, respectively. The virus remained viable for 12 weeks in all foods at –20 °C with 2–2.47 log reduction. In addition, in simulated digestive fluid experiments, HCoV-229E was relatively resistant in simulated salivary fluid (SSF; pH 7, 5), fed state simulated gastric fluid (FeSSGF; pH 3, 5, 7), and fasted state simulated intestinal fluid (FaSSIF; pH 7). However, the virus was less tolerant in fasted state simulated gastric fluid (FaSSGF; pH 1.6) and fed state simulated intestinal fluid (FeSSIF; pH 5). Therefore, this study suggested that HCoV-229E remained infectious on various food-contact surfaces and foods; in particular, it survived longer at lower temperatures and survived depending on the pH of the simulated digestive fluid.

Pharmacotechnical Evaluation by SeDeM Expert System to Develop Orodispersible Tablets.

Sediment delivery model (SeDeM) system is innovative tool to correlate micromeritic properties of powders with compressibility. It involves computation of indices which facilitate direct compressibility of solids and enable corrective measures through particle engineering. Study had multiple objectives, viz, (i) to enhance solubility of BCS class II, nevirapine using solid dispersions; (ii) SeDeM analyses of excipients and solid dispersions to analyze direct compressibility; and (iii) prepare orodispersible tablets (ODT). Solid dispersions were prepared by solvent evaporation. Superdisintegrants and solid dispersions were analyzed for primary indices of dimension, compressibility, flowability, stability, and disgregability derived from micromeritic properties. Radar diagrams were constructed to provide visual clues to deficient properties for direct compressibility. ODTs were prepared using excipients which passed criteria for direct compressibility and evaluated for tablet properties. Solid dispersions with Eudragit S100 revealed 6 to 10 fold increase in solubility in various dissolution media including biorelevant media in comparison with plain drug. Solubility was found to be pH dependent. SeDeM analyses facilitated identification of superdisintegrants and excipients with unfavorable compressibility. Radar diagrams provided a clear pictorial evidence of lacunae in powder properties. Based on SeDeM results, tablets were formulated by direct compression using crosspovidone, croscarmellose sodium, and mannitol. All batches showed 40% release in first minute in simulated salivary fluid.

The surface mechanics of cooked rice as influenced by gastric fluids measured using a micro texture analyzer.

In this study, a micro texture analyzer (MTA) was employed to explore the texture characteristics of the surface of an individual steamed rice (SR) and fried rice (FR) grain exhibited in four simulated digestion environments in vitro. The elastic modulus, hardness and elastic index of the single cooked rice particle were measured using the MTA. The hardness of SR particles decreased by 66, 81, 89.1, and 95% after simulated digestion in distilled water, HCl, simulated gastric fluid (SGF), and simulated salivary and gastric fluid (SSF + SGF), respectively. This is in line with the most significant volume expansion and structure ruptures when digested in SSF + SGF. Similar mechanical and structural behaviors were shown for FR, but the hardness and elastic modulus decreased less than those of SR under the same digestion conditions. The different surface mechanics are consistent with the reduced expansion and more compact structure with smaller voids in FR during in vitro digestion. This could be attributed to the encapsulation by frying oil on the surface that would retard the diffusion of digestive fluids into the rice kernels. A weak negative correlation was found between the elastic modulus and the moisture content of the cooked rice. The present study has quantitatively assessed the surface mechanics of cooked rice as influenced by gastric fluids using the MTA. This is practically meaningful for gaining an in-depth understanding of the influence of textural modifications on disintegration of solid foods and release of nutrients during digestion.

Inhibitory Effect of Oral Thin Films (OTFs) Containing Xylitol Against Streptococcus mutans

Dental Caries is a chronic disease affecting half of the global population, causing pain and discomfort due to progressive damage to the teeth. Whilst xylitol has been studied for its effect on dental caries prevention, current practices present few limitations for its successful oral delivery, including short residence time in the mouth and poor patient compliance. Recently, oral thin films (OTFs) emerged as an alternative to delivering xylitol in the oral cavity. This research aims to develop novel OTFs containing xylitol with extended-release properties (as determined by the disintegration time) and to investigate its effect on a cariogenic bacterial strain, Streptococcus mutans. The minimum inhibitory concentration (MIC) of xylitol was determined. Employing the microdilution broth method, the antibacterial activity of the oral thin films containing xylitol for oral S. mutans was performed with simulated salivary fluid, incubated at 1, 4, and 10 h. The MIC of xylitol was found at 10%. Meanwhile, there was no significant difference in the inhibition of S. mutans (p > 0.05) between the control, OTFs (10 h), and xylitol-OTF (1 h), with the latter, demonstrated only 16.58% inhibition. Interestingly, when compared to xylitol-OTF (1 h), xylitol-OTF showed significant inhibition (p < 0.05) to S. mutans after four h (+53.24 %) and almost a complete inhibition after ten h (-92.58 %). These results suggest that the OTFs demonstrated a gradual release of xylitol and inhibited oral biofilm formation by decreasing the growth of S. mutans in a time-dependent manner. Most importantly, the study indicated the successful development of a novel xylitol-OTF with potential as an oral health biotherapeutic agent.