Search Results (2,860)

Lipid-based formulations (LBFs) play a crucial role in enhancing the oral bioavailability of poorly water-soluble drugs by leveraging lipid digestion and solubilization processes. However, developing robust in vitro–in vivo correlations (IVIVCs) for LBFs presents unique challenges due to the complex interplay of digestion, permeation, and dynamic solubilization. This article reviews the construction of IVIVC in the context of LBFs, highlighting the limitations of traditional methods and the need for tailored approaches. It examines the in vitro tools commonly employed for LBF characterization, such as USP dissolution tests, lipolysis assays, and combined models, and discusses their relevance to in vivo performance prediction. The review also explores the sources of in vivo data essential for validating IVIVC and describes the most popular in silico tools for predicting in vivo performance, focusing on lipid-based formulations. This work aims to pave the way for more effective and adaptable IVIVC methodologies for lipid-based drug delivery systems. Full article

The development of phenolic-based functional food ingredients is of growing interest due to their beneficial effects on human health. This study investigated the combined influence of microparticle physical state, phenolic compound type (gallic acid, GA; and ellagic acid, EA), and model food matrix on the release profile, bioaccessibility, and antioxidant activity of GA and EA during in vitro gastrointestinal digestion. GA and EA were encapsulated with inulin (In) by spray-drying. By varying formulation and operational conditions, both semicrystalline (GA-InSc, EA-InSc) and amorphous (GA-InA, EA-InA) microparticles were obtained. Microparticles were characterized for crystallinity, encapsulation efficiency, particle size, morphology, and release profile during in vitro simulated gastrointestinal digestion following the INFOGEST method. The physical state of microparticles and type of phenolic compound critically influenced release profile, bioaccessibility, and antioxidant activity during digestion. GA, being more water-soluble, was rapidly released, reaching nearly 100% in the gastric phase, whereas EA exhibited limited gastric release and higher intestinal release, particularly in EA-InSc. Incorporation into different food matrices further modulated these effects; carbohydrate- and blend-based matrices improved phenolic release and antioxidant activity for both compounds. These findings highlight the importance of microparticle formulation, phenolic characteristics, and matrix interactions in designing functional food ingredients with optimized health benefits. Full article

Given the limitations of clinical and potent natural α-glucosidase inhibitors, novel selective inhibitors are urgently needed. To accelerate discovery, we employed machine learning-integrated virtual screening to rapidly evaluate a library of 100 K⁺ compounds, identifying a series of selective α-glucosidase inhibitors. Activity validation demonstrated that these inhibitors exhibit significantly enhanced selectivity and potency compared to the positive control acarbose. Mechanistic studies through inhibition kinetics and fluorescence quenching revealed their improved inhibitory profile. Molecular docking indicates that key interactions—hydrogen bonding or salt bridges with the catalytic residue ASP526—strengthen binding within the active site. These interactions competitively obstruct enzyme-substrate binding, thereby amplifying inhibition. In vitro and in vivo starch digestion assays further corroborated these findings. Full article

The poultry industry requires sustainable strategies to improve gut health and nutrient utilization while reducing antibiotic use. This study assessed the effects of dietary supplementation with a microencapsulated phytosynbiotic from Yanang (Tiliacora triandra) leaf extract fermented with Pediococcus acidilactici V202 (YEP) on broiler ileal digestibility, microbial viability, and cecal fermentation using an in vitro gastrointestinal simulation model. Six YEP inclusion levels (0–2.5%) were tested. Results revealed significant improvements in ileal dry matter and gross energy digestibility and enhanced survival and proliferation of beneficial lactic acid bacteria in the ileum. Increased gas production, lactic acid, and volatile fatty acid concentrations, including acetate, propionate, and butyrate, indicated that cecal fermentation was enhanced in a dose-dependent manner. Moderate YEP levels optimized fermentation speed and butyrate synthesis, while higher levels enhanced total gas and acetate production. YEP also shifted the cecal microbiota toward a healthier profile, enhancing Lactobacillaceae counts and the Lactobacillaceae-to-Enterobacteriaceae ratio. Overall, protective microencapsulation, synergistic phytochemical interactions, and balanced nutrient supply had positive effects at the gut level. Thus, the data highlight YEP as a promising synbiotic feed additive that can enhance nutrient utilization, microbial balance, and gut health in broilers, warranting future in vivo validation. Full article

Background/Objectives: Lipid-based formulations are widely used to enhance the oral bioavailability of poorly water-soluble drugs. However, for weakly basic drugs with higher solubility under acidic conditions, precipitation and recrystallisation after gastric emptying can compromise a formulation’s ability to maintain the drug in a solubilised, absorbable state. To address this, we evaluated an enteric coating strategy to preserve the biopharmaceutical performance of a silica-solidified lipid-based formulation. Methods and Results: The model weakly basic BCS Class IV drug, abiraterone acetate, was loaded into a lipid-based formulation and solidified using mesoporous silica nanoparticles. In an in vitro lipolysis model, introducing the formulation only after the onset of the intestinal phase led to lower precipitation and over 50% greater drug presence in the aqueous phase compared to a two-stage gastric–intestinal digestion. In an in vivo pharmacokinetic study in Sprague Dawley rats, the silica–lipid formulation (6 mg/kg), delivered in gelatine minicapsules enteric-coated with Eudragit L100-55, resulted in a 2.6-fold higher systemic exposure compared to the non-coated formulation (p < 0.0001). Conclusions: These findings support the use of enteric coating for lipid-based formulations and silica nanoparticles containing weakly basic drugs as a strategy to maintain formulation integrity until reaching the small intestine. Full article

Livestock production raises significant environmental concerns, necessitating the development of sustainable feeding strategies based on non-conventional forages, such as locally available vegetation. This study evaluated the effects of a pelleted concentrate containing 10% Acacia farnesiana leaves as a dietary supplement on in vitro ruminal fermentation. Four experimental diets were formulated with increasing levels of the concentrate (0%, 25%, 50%, and 75%). Analyses were performed in triplicate and included chemical composition, in vitro gas and methane production, fermentation kinetics, ammonia nitrogen concentration (N–NH₃), in vitro dry matter digestibility (IVDMD), and metabolizable energy (ME) estimation. The results revealed no significant differences (p > 0.05) in most gas production kinetic parameters, overall fermentation patterns, or metabolizable energy. In contrast, a significant increase (p < 0.05) in secondary metabolite concentrations was detected. While methane production remained unaltered (p > 0.05), a significant linear reduction was observed for IVDMD, the lag phase (L), and N–NH₃ concentration (p = 0.0064, p = 0.0036, and p < 0.0001, respectively). These findings suggest that A. farnesiana can be incorporated into ruminant concentrates without increasing methane emissions. However, in vivo trials and mechanistic studies are required to validate and further elucidate these results. Full article

This multidisciplinary comparative study investigates consumption patterns, health-related properties, and quality attributes of trademarked and local extra virgin olive oil (EVOO) samples. It highlights the importance of localization in promoting agricultural sustainability, strengthening regional economies, and enhancing socio-economic impacts within EVOO production and consumption systems. In terms of quality characteristics, significant differences were observed in color parameters (L*, a*, b*, Chroma, Hue angle) among EVOO samples (p < 0.05). Regarding nutritional and functional properties, total phenolic content (TPC) measured with the Folin–Ciocalteu method ranged from 58.15 to 176.29 mg of gallic acid equivalents/kg of oil, while total antioxidant capacity (TAC) measured by CUPRAC and DPPH assays varied between 3.42 and 6.54 and 8.56–10.71 µmol of Trolox equivalents/g of oil, respectively. TPC and TAC were also evaluated for their stability during in vitro gastro-intestinal digestion, demonstrating that EVOO’s bioactive potential remains stable under gastric and intestinal conditions. Local samples exhibited significantly higher TACs than trademarked products across undigested, gastric, and intestinal phases (p < 0.05). Concurrently, a face-to-face consumer survey assessed purchasing behaviors and preferences, revealing that 71.3% of consumers preferred local EVOO and showed a low tendency to purchase commercial brands (p < 0.05). Cooperatives were identified as the main distribution channel, playing a crucial role in sustaining local production systems. This study offers valuable insights into EVOO’s bioactive content and consumer behavior, providing a foundation for developing both localized and commercial products that support health outcomes. Additionally, the findings contribute to policy development concerning sustainable food systems and geographical indications. Full article

Protein-based emulsion gels and bigels serve as ideal delivery systems owing to their distinctive structural properties, high encapsulation efficiency, and adjustable digestive behavior. However, limited research has examined the differences between emulsion gels and bigels as polyphenol delivery systems. In this study, oil-in-water (O/W)-type emulsion gels formulated with soy protein isolate (SPI) and κ-carrageenan (κ-CG) were fabricated using a cold-set gelation method, and then the bigels were prepared through further oil gelation by the addition of glycerol monostearate (GMS). Both SPI-κ-CG emulsion gels and bigels were mainly stabilized by electrostatic and hydrophobic interactions, exhibiting high gel strength, varying from 940 g to 1304 g, and high water holding capacity (~84%). Both the SPI-κ-CG emulsion gels and bigels demonstrated high curcumin encapsulation efficiency, reaching 98~99%. Stability testing revealed that bigels prepared with 15% and 20% GMS exhibited the highest curcumin retention ratios, with a value of around 78% after storage for 21 days at 25 °C, suggesting that denser network structures more effectively prevent the degradation of the encapsulated compound. During the in vitro simulated gastric digestion, higher GMS content significantly delayed curcumin release by over 7%. Increasing GMS concentration from 0% to 20% elevated lipolysis by over 8% and concurrently improved the release of curcumin by more than 18% during the in vitro simulated intestinal digestion. This study provides comparative insights into polyphenol delivery performance between emulsion gels and bigels, offering valuable guidance for developing functional foods based on gel delivery systems. Full article

It was hypothesized that differences in production system and muscle type may influence the formation of lipid oxidation products (LOP) as well as protein oxidation (protein carbonyl compounds, PCC) during the in vitro gastrointestinal digestion of chicken meat. To test our hypothesis, we investigated the formation of LOP and PCC after heating and in vitro gastrointestinal digestion of conventional and organic chicken breast and thigh meat and Wooden Breast meat. Prior to the in vitro digestion, thigh and breast meat was minced and heated. Digests of organic thigh meat had significantly higher levels of all LOP measured compared to conventional thigh meat (between +37% and +173%). Lower levels of LOP were found in digests of breast meat regardless of the production system and Wooden Breast phenotype. LOP correlated positively with heme-Fe and polyunsaturated fatty acids, negatively with anserine, and not with carnosine and α-tocopherol. PCC levels were significantly higher in thigh meat than in breast meat after heating (+43%) and digestion (+25%), irrespective of the production system. Overall, organic thigh meat exhibited the highest oxidative sensitivity during digestion. The cut-dependent differences in composition and oxidative susceptibility between organic and conventional chicken highlight the need for further research to assess potential health implications. Full article

Okara, a protein-rich byproduct of soymilk production, is highly perishable because of its high moisture content. This study evaluated the preservation and nutritional value of okara fermented by lactic acid bacteria for use in dairy cattle diets. Fermentation effectively reduced pH within 2 weeks and maintained quality for up to 6 weeks. However, aerobic exposure increased the concentration of ammonia, indicating a decline in stability. In vitro assessments revealed no significant differences in in vitro true dry matter digestibility, in vitro neutral detergent fiber digestibility, or gas production between fermented and fresh okara, although fermented okara had a higher concentration of ammonia nitrogen. In situ analysis revealed slightly lower dry matter effective degradability (ED) in fermented okara, but similar rumen-degradable and undegradable protein fractions. When fermented okara was used to replace soybean meal in total mixed rations, 25–50% inclusion-maintained digestibility and fermentation characteristics, with 25% replacement yielding the highest ED at a low ruminal passage rate (0.02 h⁻¹). Taken together, these results suggest that fermented okara can be strategically incorporated into dairy rations as a sustainable protein alternative, supporting both rumen function and bypass protein supply. Full article

In this study, nanoparticles prepared by the heat-induced self-assembly of bovine serum albumin-dextran conjugates (BSA-DX) were utilized as an effective delivery system for the immunoregulatory peptide Gln-Leu-Asn-Trp-Asp (QLNWD) from Meretrix meretrix. The effects of dry-heating duration on the fabrication and characteristics of glycoprotein nanoparticles (GBA NPs) were investigated. Stable GBA NPs (110.84 nm) were obtained after 9 h of dry-heating. Depending on the addition sequence of QLNWD, the QLNWD-loaded nanoparticles were categorized into two types: pre-loading and post-loading. The two strategies were evaluated based on physicochemical characterization, colloidal stability, and RAW264.7 macrophage uptake. Results showed that upon QLNWD incorporation, both pre-loading NPs and post-loading NPs exhibited spherical morphology, with particle sizes decreasing to 105.51 nm and 94.27 nm, respectively. The encapsulation efficiency of pre-loading NPs for QLNWD was higher (87.74%), and the co-localization ability between post-loading NPs and QLNWD was stronger (Pearson’s correlation coefficient = 0.95). In vitro simulated gastrointestinal digestion experiments showed that QLNWD bioaccessibility increased to 47.5% and 42.7% for pre-loaded and post-loaded NPs, respectively. Compared to free QLNWD, NP encapsulation significantly enhanced the uptake of QLNWD by macrophages. Thus, GBA NPs, particularly those prepared by the pre-loading method, are considered promising delivery systems for marine bioactive peptides. Full article

Cocoa pod husk (CPH) has the potential to be utilized for polyphenol extraction to be used in functional food formulations and pharmaceutical formulations due to its health benefits. However, polyphenols are sensitive to environmental factors that reduce their stability and functionality. Therefore, encapsulation is necessary to protect their antioxidant capacity, mask undesirable flavours and smells, and, at the same time, allow the release of polyphenols in the gastrointestinal phases. This study encapsulated polyphenols using complex coacervation (CC) and spray drying (SD) with gum arabic (GA), sodium alginate (SA), chitosan (C), and gelatine (G), and evaluated yield (EY), encapsulation efficiency (EE), loading efficiency (LE), and bioaccessibility through in vitro digestion. The results showed that in the encapsulation using CC, the highest LE of 36.95 ± 7.63% was obtained using SA-G. In SD, significant differences in LE were observed among the tested encapsulant ratios, with the highest LE of 34.77 ± 1.2% achieved using GA (1:3). Bioaccessibility varied significantly depending on the encapsulation technique and encapsulating agent (EA) used. Using GA and spray drying (SD), the highest polyphenol release was achieved at 76.55 ± 5.10%, in contrast to only 6.41 ± 1.61% for the non-encapsulated extract. In conclusion, both techniques for encapsulating polyphenols extracted from CPH are efficient. However, SD allows for greater polyphenol bioaccessibility. Full article

Two HPLC-based analytical methods, one with DAD and the other with an FLD detector, were developed and validated for the simultaneous analysis of B₁, B₂, and B₆ vitamins, both in pharmaceutical gummies and in gastric and intestinal fluids (with water or milk or orange juice). For the detection of B₁ by fluorometry, a pre-column oxidation/derivatization process was accomplished in the presence of B₂ and B₆ vitamins. The methods were performed on an Aqua column (250 mm × 4.6 mm, 5 mm) at 40 °C, with isocratic elution (70% NaH₂PO₄ buffer pH 4.95 and 30% methanol) and a flow rate of 0.9 mL/min. Both were validated according to ICH specifications in terms of linearity (R² > 0.999), accuracy (% Mean Recovery 100 ± 3%) and precision (%RSD < 3.23). For the analysis of the samples, a stability study (in diluents, pH and fluids) was conducted, while for their purification two different extraction procedures, a liquid/solid for the gummies (%Recovery > 99.8%) and a Solid Phase Extraction (SPE) for the Gastrointestinal (G.I.) fluids, (%Recovery 100 ± 5%) were developed. Finally, to investigate whether the co-administration of B-complex with water, orange juice or milk plays a significant role in their release from gummies, a three-phase in vitro digestion protocol was applied. The results did not show significant differences with a slight superiority in the release of B₂ and B₆ with water, while B₁ with orange juice. Full article

This study addressed the challenges posed by wet-grade maize distiller’s dried grains with solubles (DDGS), which are characterized by high moisture and complex fibers that limit their storage and utilization in poultry feed. Three experiments were conducted to enhance their nutritional value through enzymatic and solid-state fermentation treatments. In vitro pre-digestion using multiple enzymes significantly improved dry matter solubility (DMS) and reducing sugar yield for maize DDGS and the ingredient maize germ meal (MGM). Using optimized parameters, wet-based DDGS-MGM was subjected to solid-state fermentation with 500 mg/kg of cellulase and 200 mg/kg of the X1 enzyme (a laboratory-developed multi-enzyme complex), and this treatment enhanced both DMS and reducing sugar yield, and the resulting fermented product was subsequently applied in further experiments. In the broiler trial, forty 22-day-old Arbor Acres broilers with similar body weights were randomly assigned to five treatment groups, including the control group, (50% DDGS + 50% MGM) unfermented group, (62.5% DDGS + 37.5% MGM) unfermented group, (50% DDGS + 50% MGM) fermented group, and (62.5% DDGS + 37.5% MGM) fermented group, with eight replicates per treatment (one broiler per replicate). Replacement of 30% of the basal diet with fermented 50:50 DDGS-MGM material significantly increased apparent metabolizable energy (AME) and nitrogen-corrected AME by 2.74 MJ/kg and 2.73 MJ/kg, respectively, corresponding to improvements of 39.60% and 40.81% compared to the unfermented control (p < 0.05). Economic analysis indicated that using 5% fermented DDGS-MGM in feed reduced cost by 20.45 RMB per metric ton. These findings demonstrate that bioprocessing can improve the utilization and economic value of maize processing by-products, although further validation under practical conditions is needed. Full article

Snack bars are convenient, ready-to-eat foods with various natural ingredients and may serve as functional foods, offering bioactive phytochemicals. In this study, tomato-based snack bars enriched in plant proteins were evaluated for their antioxidant, antidiabetic, anti-obesity, and anti-inflammatory properties by in vitro test, comparing different protein sources (pea and RuBisCO) and drying methods (microwave vacuum and oven). The rubisco bars exhibited the highest levels of polyphenols (10.12 ± 0.27 mg GAE/g) and flavonoids (5.65 ± 0.47 mg CE/g), and demonstrated superior antioxidant capacity in DPPH, ORAC, and FRAP assays, particularly when microwaved. Rubisco bars also exhibited better inhibition activity of dipeptidyl-peptidase IV and pancreatic lipase, suggesting potential antidiabetic and anti-obesity effects. In contrast, pea bars displayed notable anti-inflammatory effects by reducing tumor necrosis factor (TNF)-α-induced cyclooxygenase-2 (COX-2) expression in intestinal cells. Both protein types were digestible, though rubisco bars released more peptides during simulated gastrointestinal digestion. While these in vitro findings provide insights into the functional potential of tomato-based snack bars, further studies, including in vivo investigations, are required to confirm their health-promoting effects and to evaluate physiologically relevant doses. Overall, these findings highlight the potential of tomato-based snack bars as sustainable, nutrient-rich functional foods with potential health-promoting properties. Full article