Search Results (286)

This study developed phospholipid-based liposomes loaded with extract from wild thyme (Thymus serpyllum L.) tea processing residues to enhance polyphenol stability and delivery. Liposomes were prepared with phospholipids alone or combined with 10–30 mol% cholesterol or β-sitosterol. The effect of different lipid compositions on encapsulation efficiency (EE), particle size, polydispersity index (PDI), zeta potential, stability, thermal properties, diffusion coefficient, and diffusion resistance of the liposomes was investigated. Liposomes with 10 mol% sterols (either cholesterol or β-sitosterol) exhibited the highest EE of polyphenols, while increasing sterol content to 30 mol% resulted in decreased EE. Particle size and PDI increased with sterol content, while liposomes prepared without sterols showed the smallest vesicle size. Encapsulation of the extract led to smaller liposomal diameters and slight increases in PDI values. Zeta potential measurements revealed that sterol incorporation enhanced the surface charge and stability of liposomes, with β-sitosterol showing the most pronounced effect. Stability testing demonstrated minimal changes in size, PDI, and zeta potential during storage. UV irradiation and lyophilization processes did not cause significant polyphenol leakage, although lyophilization slightly increased particle size and PDI. Differential scanning calorimetry revealed that polyphenols and sterols modified the lipid membrane transitions, indicating interactions between extract components and the liposomal bilayer. FT-IR spectra confirmed successful integration of the extract into the liposomes, while UV exposure did not significantly alter the spectral features. Thiobarbituric acid reactive substances (TBARS) assay demonstrated the extract’s efficacy in mitigating lipid peroxidation under UV-induced oxidative stress. In contrast, liposomes enriched with sterols showed enhanced peroxidation. Polyphenol diffusion studies showed that encapsulation significantly delayed release, particularly in sterol-containing liposomes. Release assays in simulated gastric and intestinal fluids confirmed controlled, pH-dependent polyphenol delivery, with slightly better retention in β-sitosterol-enriched systems. These findings support the use of β-sitosterol- and cholesterol-enriched liposomes as stable carriers for polyphenolic compounds from wild thyme extract, as bioactive antioxidants, for food and nutraceutical applications. Full article

Background/Objectives: Mesoporous silica materials, particularly KIT-6, offer promising features, such as large surface area, tunable pore structures, and biocompatibility, making them ideal candidates for advanced drug delivery systems. The aims of this study were to develop and evaluate an innovative modified-release platform for metformin hydrochloride (MTF), using KIT-6 mesoporous silica as a matrix, to enhance oral antidiabetic therapy. Methods: KIT-6 was synthesized using an ultrasound-assisted sol-gel method and subsequently loaded with MTF via adsorption from alkaline aqueous solutions at two concentrations (1 and 3 mg/mL). The structural and morphological characteristics of the matrices—before and after drug loading—were assessed using SEM-EDX, TEM, and nitrogen adsorption–desorption isotherms (the BET method). In vitro drug release profiles were recorded in simulated gastric and intestinal fluids over 12 h. Kinetic modeling was performed using seven classical models, and a multifractal theoretical framework was used to further interpret the complex release behavior. Results: The loading efficiency increased with increasing drug concentration but nonlinearly, reaching 56.43 mg/g for 1 mg/mL and 131.69 mg/g for 3 mg/mL. BET analysis confirmed significant reductions in the surface area and pore volume upon MTF incorporation. In vitro dissolution showed a biphasic release: a fast initial phase in an acidic medium followed by sustained release at a neutral pH. The Korsmeyer–Peppas and Weibull models best described the release profiles, indicating a predominantly diffusion-controlled mechanism. The multifractal model supported the experimental findings, capturing nonlinear dynamics, memory effects, and soliton-like transport behavior across resolution scales. Conclusions: The study confirms the potential of KIT-6 as a reliable and efficient carrier for the modified oral delivery of metformin. The combination of experimental and multifractal modeling provides a deeper understanding of drug release mechanisms in mesoporous systems and offers a predictive tool for future drug delivery design. This integrated approach can be extended to other active pharmaceutical ingredients with complex release requirements. Full article

To enhance the antibacterial activity of cefquinome (CEF) against Escherichia coli, a Carboxymethylcellulose sodium (CMCNa)/D-Mannosamine hydrochloride (DMH)-based nanogels delivery system capable of protecting CEF from gastric acid degradation while enabling intestinal sustained release and targeted antibacterial enhancement was developed. Systematic research was conducted on the best formulation, physicochemical characteristics, stability, gastrointestinal fluid-responsiveness, and antibacterial activity of the optimal formulation. The results showed that the optimized CEF nanogels demonstrated an enhanced loading capacity (13.0% ± 1.7%) and encapsulation efficiency (52.2% ± 1.0%). CEF nanogels appeared as uniform transparent spheres with a smooth surface under transmission electron microscopy and exhibited a three-dimensional porous network via scanning electron microscopy. More importantly, stability studies revealed that the CEF nanogels hold satisfactory stability. In addition, the formed CEF nanogels could effectively avoid the destruction of CEF by gastric acid in simulated gastric juice. In addition, they had the effect of slow and targeted release in the simulated intestinal tract. Compared to the free CEF, CEF nanogels have stronger antibacterial activity against Escherichia coli. In short, the prepared CEF nanogels had stronger antibacterial activity than CEF through sustained and targeted release. Full article

Morin is a natural flavonoid with potent antioxidant activity, yet its clinical and nutraceutical applications remain limited due to poor aqueous solubility and low bioavailability. This study explores the interaction of morin with bovine serum albumin (BSA) and the development of BSA-based nanoparticles as a delivery platform. Fluorescence spectroscopy confirmed the formation of a stable 1:1 morin–BSA complex, governed by hydrophobic interactions, with a binding constant (Ka) of 1.87 × 10⁵ L·mol⁻¹. Binding conferred enhanced photostability, as BSA attenuated morin degradation under oxidative stress conditions. BSA nanoparticles prepared by desolvation encapsulated morin with high monodispersity and encapsulation efficiencies up to 26%. Co-encapsulation with ellagic acid or tocopherol succinate improved loading capacity but reduced morin release, suggesting intermolecular stabilization. Release studies in simulated intestinal fluid showed controlled diffusion, while compatibility assays in milk-based food matrices confirmed colloidal stability in whole and reduced-fat milk. These findings support BSA–morin nanoparticles as a promising system for the oral delivery and functional food incorporation of polyphenolic antioxidants. Full article

Hyperuricemia arises from urate overproduction and/or underexcretion. Probiotics offer the potential for alleviating hyperuricemia by degrading urate precursors. This study characterized Enterococcus faecium YC07 isolated from the traditional Chinese fermented food Jiangshui, which demonstrated efficient biodegradation of nucleosides (urate precursors), converting 2.0 g/L to nucleobases within 48 h. Whole genome sequencing revealed a 2.53 Mb draft genome (59 contigs, 38.21% GC content) containing 2387 protein-coding genes. Genomic and phenotypic analysis confirmed its probiotic potential, including high tolerance of simulated gastric fluid (98.89% survival) and intestinal fluid (44.51% survival), and strong adhesion capacity (24.16% auto-aggregation, 35.48% hydrophobicity), pathogen inhibition, and antioxidant activity. The identified antibiotic resistance genes and virulence factors were assessed alongside acute oral toxicology, cytotoxicity, antibiotics susceptibility, hemolysis, and enzymatic activity assays, confirming safety. Furthermore, successful pilot-scale fermentation in a 100 L fermenter demonstrated industrial feasibility. These findings established E. faecium YC07 as a safe and effective probiotic candidate for functional foods targeting hyperuricemia management. Full article

Chitosan, a naturally occurring alkaline polysaccharide with excellent biocompatibility, non-toxicity, and renewability, has the ability to undergo cross-linking reactions with polyphenolic compounds. In this study, chitosan-encapsulated green tea extract microsphere resin (CS-GTEMR) was successfully prepared using chitosan and green tea extract via reversed-phase suspension cross-linking polymerization. The structural characterization of CS-GTEMR was conducted using Fourier Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC). Additionally, its physical properties, swelling behavior, polyphenol content, and antioxidant activities were investigated. The results indicate that CS-GTEMR consists of reddish-brown microspheres with a smooth surface and dense pores. The study found that the total content of polyphenolic compounds encapsulated in CS-GTEMR was 50.485 ± 0.840 μg/g. The characteristic absorption peak of phenolic hydroxyl groups appeared in the FTIR spectrum, suggesting that the polyphenolic compounds had been successfully encapsulated within the CS-GTEMR. The equilibrium swelling ratio of CS-GTEMR was determined to be 229.7%, indicating their suitability for use in solutions with a pH range of 1–13. In simulated gastric and intestinal fluids, the release rates of polyphenolic compounds from CS-GTEMR were 24.934% and 3.375%, respectively, indicating that CS-GTEMR can exert a sustained-release effect on polyphenolic compounds. CS-GTEMR demonstrated antioxidant activities such as scavenging DPPH radicals, superoxide anion radicals, hydroxyl radicals, and hydrogen peroxide, as well as exhibiting iron-reducing and molybdenum-reducing powers. With its high mechanical strength, acid resistance, and organic solvent resistance, CS-GTEMR can protect polyphenolic compounds from damage. Therefore, CS-GTEMR can be utilized as a natural antioxidant or preventive agent in food, expanding the application scope of green tea extracts. Full article

Probiotics are often advised to be taken separately from antibiotics due to their sensitivity to antibiotic activity and gastrointestinal (GI) stress. However, Clostridium butyricum spores, as next-generation probiotics, may withstand concurrent use with antibiotics due to their unique structural adaptations. This study systematically evaluated the survival rates and morphological changes of C. butyricum spores exposed to 10 clinically relevant antibiotics in simulated gastric/intestinal fluids, exploring their feasibility for co-administration with antibiotics. Survival rates of C. butyricum spores were tested against 10 antibiotics across four classes (β-lactams, macrolides, aminoglycosides, and tetracyclines) in simulated GI fluids. Time–kill curves analyzed spore survival over 0–4 h, while scanning electron microscopy (SEM) observed spore wall integrity and morphological changes under different conditions. The spore survival rates remained >89% in intestinal fluid and >60% in gastric fluid across all antibiotics. SEM revealed gastric acid and proteolysis increased spore wall fragmentation, reducing resistance, whereas the intestinal environment preserved spore integrity. This study was the first to demonstrate that C. butyricum spores can survive simultaneous exposure to antibiotics in the gastrointestinal tract, challenging traditional probiotic usage guidelines. The findings support their co-administration with antibiotics to simplify dosing regimens and improve medication adherence. Such an approach advances antimicrobial stewardship by optimizing therapeutic strategies for antibiotic–probiotic combinations. Full article

Objectives: This study characterised and evaluated the stability, solubility, and in vitro drug release of OA- and AA-loaded SLNs. Methods: The OA- and AA-SLNs were formulated using the emulsion solvent evaporation method and characterised based on particle size (PS), polydispersity index (PDI), zeta potential (ZP), and transmission electron microscopy (TEM). Solubility studies were conducted in PBS (pH 1.2 and 6.8) and dH₂O using HPLC, while in vitro drug release was assessed in simulated intestinal fluid (SIF) (pH 6.8). Results: The optimised OA-SLNs (1:1 drug-to-lipid ratio) showed PS, PDI, ZP, and EE% values of 312.9 ± 3.617 nm, 0.157 ± 0.014, −17.0 ± 0.513 mV, and 86.54 ± 1.818%, respectively. The optimised AA-SLNs (1:2 drug-to-lipid: ratio) had a PS of 115.5 ± 0.458 nm, PDI of 0.255 ± 0.007, ZP of −11.9 ± 0.321 mV, and EE% of 76.22 ± 0.436%. The SLNs remained stable for 60 days at 4 °C and room temperature (p < 0.05). The solubility study revealed that free OA and AA showed no measurable values in the three solvents. However, OA-SLNs showed the highest solubility in H₂O (16-fold) followed by PBS at pH 6.8 (10-fold) and pH 1.2 (10-fold). AA-SLNs significantly improved the solubility in PBS at pH 6.8 (88-fold), compared to dH₂O (6-fold) and PBS at pH 1.2 (26-fold). In vitro drug release studies showed that OA release from the SLNs was significantly increased within 300 min (p < 0.05) compared to the free drug. Similarly, AA release from the SLNs was significantly increased within 300 min (p < 0.05) compared to free AA. Conclusions: These results demonstrate that SLNs enhance OA and AA solubility and drug release, suggesting a promising strategy for improving oral bioavailability and therapeutic efficacy. Full article

Bioactive compounds of natural origin are central to the development of nutraceutical formulations. To improve their stability and to target their delivery to the intestinal or colonic tract, alginate/k-carrageenan spherical gels have been produced at different volumetric ratios (100/0, 70/30, 50/50, 30/70, and 0/100 v/v), by means of solution dripping and external gelation. Different drying methods were compared, and only through supercritical technologies was it possible to achieve interpenetrated networks that feature nanometric pore size distribution. Hybrid aerogels inherited the most relevant characteristics of alginate and k-carrageenan: they showed remarkable water uptake capacity (e.g., 50.60 g/g), and stability in aqueous media over large timespans. Naringin release tests in simulated intestinal and colonic fluids proved that it is possible to target drug delivery by choosing intermediate alginate/k-carrageenan ratios. Overall, by means of supercritical gel drying, it is possible to generate advanced biopolymeric aerogels, yielding fully natural interpenetrated networks that valorize the most compelling properties of each species involved. Full article

Rose Bengal (RB) holds promise for therapeutic applications in the gastrointestinal (GI) tract but faces significant limitations due to poor bioavailability and stability in the GI environment. This in vitro proof-of-concept study aimed to develop an oral drug delivery system using self-assembled RB–chitosan (RBCS) nanocomposites formed via electrostatic interactions. RBCS nanocomposites exhibited high drug loading efficiency (87%) and a uniform particle size (~443 nm), with physicochemical analyses confirming molecular interactions and structural stability. However, in vitro studies revealed poor and highly variable drug release in simulated gastric fluids (SGFs), underlining the need for further optimization. To address these limitations, RBCS nanocomposites were encapsulated within well-established alginate beads (AlgBs). Among the tested systems, RBCS20-AlgBs were selected as the optimal one, forming a gastroresistant platform. Encapsulation mitigated burst release, enhanced structural integrity, and enabled sustained RB release under intestinal conditions. Swelling studies demonstrated that RBCS20-AlgBs maintained controlled hydration, preventing premature disintegration. Mathematical modeling indicated a matrix relaxation-driven release mechanism, with RBCS20-AlgBs demonstrating improved reproducibility compared to RB-loaded AlgBs (RB-AlgBs). Future studies should focus on evaluating in vivo performance to confirm the system’s efficacy for oral administration. Full article

Background: The antidiabetic drug gliclazide is often taken with antacids due to its gastrointestinal side effects. However, patients rarely report antacid use, making drug–drug interactions a potential cause of therapy failure. Therefore, this study aimed to investigate the in vitro effects of various antacids on gliclazide permeability and to explore the underlying mechanisms. Methods: The permeability of gliclazide alone and in the presence of antacids (sodium bicarbonate, calcium carbonate, aluminum hydroxide, hydrotalcite and calcium carbonate/magnesium carbonate) was investigated using the parallel artificial membrane permeability assay (PAMPA) in four media (buffers pH 1.2, pH 4.5, pH 6.8 and water). The permeability coefficients were calculated, and the effect of pH on gliclazide permeability was also evaluated. Results: At simulated fasting gastric conditions (pH 1.2), groups with calcium carbonate, hydrotalcite and the combination of calcium carbonate/magnesium carbonate showed significantly higher permeability of gliclazide than the control group. At fed-state gastric conditions (pH 4.5), only hydrotalcite did not significantly change the permeability of gliclazide. Sodium bicarbonate, aluminum hydroxide and hydrotalcite significantly reduced the gliclazide permeability in comparison to the control group at pH 6.8 as a representative of fasted-state intestinal fluid. Conclusions: Antacids significantly impact the permeability of gliclazide at different pH values, potentially influencing its bioavailability. Gliclazide permeability is mainly influenced by pH-dependent ionization, though complex or salt formation may also play a role. Since both gliclazide and antacids are taken with food, and gliclazide is primarily absorbed in the small intestine, calcium- and magnesium-based antacids can be considered the most suitable choice. Full article

This study aims to investigate two types of solvents, ethanol and natural deep eutectic solvent (NaDES), using the ultrasound-assisted extraction techniques, in order to analyze their efficiency and ability to extract polyphenolic compounds from red grape pomace. The optimization and validation of the most feasible extraction conditions leading to maximization of the dependent variables (total anthocyanins, polyphenols, flavonoids and antioxidant activity), were carried out using response surface methodology with a central composite design. For ethanol extraction, the validated optimal conditions were at 35 °C for 22.5 min and a concentration of 70% ethanol. The values obtained under these conditions were 105.32 mg cyanindin-3-glucoside (C3G)/g DW, 465.81 mg gallic acid equivalents (GAE)/100 g DW, 15.3 mg catechin equivalents (CE)/100 g DW and 1414.15 mMol Trolox/g DW, respectively. Concerning the extraction using NaDES, consisting of a 1:2:1 molar mixture of choline chloride, lactic acid and water, the optimal conditions that led to a profile consisting in 57.58 mg C3G/g DW, 414.04 mg GAE/100 g DW, 15.8 mg CE/100 g DW and 7.28 mMol Trolox/g DW, respectively, were at 60 °C for 60 min and a solvent volume of 10 mL. Two different chromatographic profiles were obtained, with 12 polyphenolic compounds identified in ethanolic extracts and only 5 in NaDES, respectively. The in vitro digestion study revealed the high bioaccessibility of polyphenols in the gastric environment, with a drastic decrease in simulated intestinal fluid. The results are valuable in terms of identifying the best extraction conditions for polyphenols using alternative, non-toxic, ecofriendly solvents. Full article

Probiotic species have garnered significant attention for their health benefits extending beyond gastrointestinal health. This study investigated the biological and enzymatic functions of selected probiotic species, specifically Lacticaseibacillus rhamnosus (formerly Lactobacillus rhamnosus), Lactiplantibacillus plantarum (formerly Lactobacillus plantarum), Lactobacillus acidophilus, and Lactobacillus delbrueckii, among others, through in vitro experiments. Enzymatic activities, including hemolytic, lipase, esterase, and protease functions, were evaluated. Antioxidant capacity was assessed using DPPH radical scavenging assays, while antimicrobial efficacy was tested against common pathogenic bacteria. Antibiotic-resistance patterns were analyzed to ascertain their safety for human consumption. Furthermore, simulated digestive fluid tolerance experiments were conducted to evaluate survival in the gastrointestinal tract. The findings indicate that these probiotic strains exhibit diverse functionalities beyond intestinal health, with potential roles in digestion, oxidative stress reduction, and immune support. This study provides valuable insights into the functional diversity of probiotics, suggesting their broader applications in health and nutrition. Future research should focus on in vivo validation, mechanism elucidation, and clinical studies to determine optimal dosages and strain-specific benefits. Full article

Colitis in equines has high morbidity and mortality rates, which severely affects the development of the equine-breeding industry. With the issuance of antibiotic bans, there is an urgent need for healthier and more effective alternatives. In recent years, probiotics have been widely used as microbial feed additives in animal husbandry, playing a crucial role in preventing and treating diarrhea and regulating host immune function. In this study, we isolated and screened a strain with rapid and stable acid production using bromocresol purple, litmus milk coloration tests, and acid production performance assessments. Based on morphological characteristics, physiological and biochemical properties, and 16S rDNA identification, the strain was identified as Pediococcus pentosaceus and named M6. The Pediococcus pentosaceus M6 exhibited stable growth and tolerance to high temperatures, acid and bile salt concentrations, and simulated gastrointestinal fluid environments. The M6 strain demonstrated good antibacterial effects against Escherichia coli, Staphylococcus aureus, and Salmonella. The M6 strain did not produce hemolysis zones on Columbia blood agar plates, indicating its high safety, and was found to be insensitive to 12 antibiotics, including cephalexin and neomycin. Additionally, intervention in mice with dextran sulfate sodium (DSS)-induced colitis alleviated weight loss and shortened colon length. To a certain extent, it regulated the expression of inflammatory cytokines and the gut microbiota within the body and reduced inflammatory cell infiltration and intestinal barrier damage. In summary, the isolated Pediococcus pentosaceus M6 strain exhibited excellent probiotic properties and could alleviate DSS-induced colitis in mice, suggesting its potential application value as a probiotic in animal husbandry. Full article

Background: This review examines in vitro techniques for characterizing the pharmacokinetics of medicinal plants, focusing on their role in understanding absorption, distribution, metabolism, and excretion (ADME). The diverse bioactive compounds in medicinal plants highlight the need for robust pharmacokinetic evaluations to ensure their safety and efficacy. Objectives: The objectives were to identify and analyze in vitro techniques applied to medicinal plants’ pharmacokinetics, addressing a gap in the literature. Methods: Studies were included based on predefined eligibility criteria: in vitro pharmacokinetic studies involving medicinal plants, focusing on ADME stages. Ex vivo, in vivo, and in silico studies were excluded, along with reviews. Data were collected from the PubMed, Web of Science, and Scopus databases in June 2024 using Health Sciences Descriptors (DeCS) and their MeSH synonyms. The data extracted included study location, plant species, bioactive compounds, in vitro protocols, and ADME characteristics. Results: The review included 33 studies, with most focusing on metabolism (60%), absorption (25%), or a combination of ADME aspects. Techniques like Caco-2 cells, human liver microsomes, and simulated gastric and intestinal fluids were widely used. Conclusions: The findings highlight methodological heterogeneity, including variability in extract preparation, compound concentrations, and experimental conditions, which limits the comparability and clinical applicability of results. Key limitations include the lack of standardized protocols and physiological relevance in in vitro models, underscoring the need for multidisciplinary approaches and integration with in vivo studies. Full article