Search Results (30)

Background: Oral administration remains the most common route for drug absorption. Emerging evidence highlights the important role of gut microbiome in the pharmacokinetics of oral medications. Glycyrrhizic acid (GL), a widely used hepatoprotective drug, is orally administrated and subsequently biotransformed by the gut microbiota into its active metabolite, glycyrrhetinic acid (GA), which exerts a therapeutic effect. However, it remains unclear whether the disturbance of the gut microbiome directly impacts the metabolism of GL. Methods: Antibiotic cocktail and probiotic Lacticaseibacillus rhamnosus R0011 were applied as two interventions targeting the gut microbiome. Pharmacokinetic parameters were evaluated by LC-MS, and 16S rRNA sequencing was applied to analyze the gut microbiome composition. The transcriptome analysis of Caco-2 cells was used to elucidate the regulation mechanism of polar metabolites resulting from gut microbiome perturbation. Results: R0011 supplementation could significantly increase the Area Under Curve (AUC) value of GA, which was positively correlated with the change in gut microbiome composition. In contrast, the plasma levels of GA were nearly undetectable following antibiotic intervention. Furthermore, the relative expressions of transporter multidrug resistance gene 1 (MDR1) in the ileum were site specifically downregulated under the probiotic intervention. The polar gut microbial metabolites may play a crucial role in differentiated regulating MDR1 expression, likely through the modulation of transcription factors FoxO1 and TP53. Conclusions: Our research provides new insights into the regulatory mechanism by which the gut microbiome affects the bioabsorption of orally administrated drugs, potentially offering strategies to optimize drug bioavailability and improve clinical efficacy. Full article

The present study investigates the potential capacity of fungi for the use in mercury (Hg) leaching and immobilization during the dissolution of cinnabar ore, the updated understanding of the mechanisms involved, and the evaluation of Hg absorption by these fungal strains. Two fungal strains are isolated from Hg-polluted soils in French Guiana and identified as Trichoderma koningiopsis and Talaromyces verruculosus. These fungal strains possess a high capacity for Hg resistance. The Hg concentrations causing 50% growth reduction (EC₅₀) are 5.9 and 1.5 ppm for T. koningiopsis and T. verruculosus, respectively. The results of medium-culture-containing cinnabar ore show that these fungal strains remove over 99% of the Hg content in the culture media by the end of the experiment. Fungal biomass decreases with increasing mercury concentration. The production of organic acids by fungi is observed for both fungal strains, leading to an acidic pH in the medium culture. Oxalic and citric acids are preferentially produced to dissolve Fe from minerals, which may impact Hg leaching. The results of this study provide evidence that the two fungi seem to have potential use for the bioremediation of Hg during the dissolution of cinnabar ores through biosorption mechanisms. Full article

In the interests of using green and sustainable chemical innovations to create sustainable products with minimized (or no) chemical hazard potential, the polyester fabric in this work was activated and functionalized with chitosan and its durability was investigated. Chitosan is a natural biopolymer derived from chitin. As it has good biocompatibility, bio-absorption, anti-infectious, antibacterial and hemostatic properties and accelerates wound healing, it is increasingly being researched for the antimicrobial treatment of textiles. Due to the increased demands on the durability of antimicrobial properties during care, its binding to cellulose in cotton and cotton–polyester blends has been researched, but not to polyester alone. Therefore, the functionalization of polyester fabrics with chitosan by thermosol in the form of submicron particles and pad-dry-curing with homogenized gel was investigated in this work. The functionalization with chitosan was carried out on untreated polyester fabric and polyester fabric activated by alkali hydrolysis. In order to reduce the release of chemical substances during the entire life cycle of textile production, no binder was used. The effects were evaluated by electrokinetic analysis (zeta potential), and the mechanical, spectral, moisture management and antimicrobial properties were determined using standard methods. The functionalized polyester fabrics were submitted to 10 washing cycles in a solution of non-ionic surfactant for determination of its durability. It was shown that the functionalization of hydrolyzed polyester fabric with homogenized chitosan gel by pad-dry-curing results in excellent antimicrobial efficacy and moisture management properties while maintaining the mechanical properties of the fabric even after 10 washing cycles. Full article

Background: Supersaturating drug delivery systems (SDDSs) have gained significant attention as a promising strategy to enhance the solubility and bioabsorption of Biopharmaceutics Classification System (BCS) II drugs. To overcome challenges associated with polymer-based amorphous SDDS (aSDDS), coamorphous (CAM) systems have emerged as a viable alternative. Among them, “drug-drug” CAM (ddCAM) systems show considerable potential for combination drug therapy. However, many drugs in their pure amorphous forms are unstable at room temperature (RT), complicating their formation and long-term stability profiles. Consequently, limited knowledge exists regarding the behavior of ddCAMs containing RT-unstable components formed via quench cooling. Methods: In this study, we used naproxen (NAP), a RT-unstable amorphous drug, in combination with felodipine (FEL) or nitrendipine (NTP), two RT-stable amorphous drugs, to create “FEL-NAP” and “NTP-NAP” ddCAM pairs via quench cooling. Our work used a series of methods to perform a detailed analysis on the co-amorphization, dissolution, solubility, and stability profiles of ddCAMs containing RT-unstable drugs, contributing to advancements in co-amorphization techniques for generating SDDS. Results: This study revealed that the co-amorphization and stability profiles of ddCAMs containing RT-unstable components produced via a quench-cooling method were closely related to drug-drug pairing types and ratios. Both quench-cooling and incorporation into coamorphous systems improved the dissolution, solubility, and physical stability of individual APIs. Conclusions: Our findings provide deeper insight into the co-amorphization, dissolution, and stability characteristics of specific drug-drug coamorphous systems FEL-NAP and NTP-NAP, offering valuable guidance for developing new ddCAM coamorphous formulations containing some RT-unstable drugs. Full article

Phytosomes are used as vehicles that carry plant extracts. They exhibit biological activities and possess better bioavailability, bioabsorption, and lower toxicity than drugs. Obesity is an inflammatory state in which oxidative stress is present, which triggers severe effects on the body’s organs. This study aimed to evaluate the impact of the extract and phytosomes of Callistemon citrinus on oxidative stress and inflammation in the liver and heart of Wistar rats fed with a high-fat-fructose diet. Phytosomes containing the extract of leaves of C. citrinus were prepared. The antioxidant, pro-inflammatory enzymes, and biomarkers of oxidative stress were evaluated. Among the groups, only the high-fat-fructose group presented an increase in the COX-2, 5-LOX, and MPO inflammatory enzymes, while the XO enzyme exhibited decreased activity. The groups were fed a hypercaloric diet for 15 weeks while orlistat, C. citrinus extract, and phytosomes were administered at three different concentrations, exhibiting enzyme activities similar to those of the control group. It was also observed that the lowest concentration of phytosomes had a comparable effect to the other concentrations. Callistemon citrinus extract can modulate the activities of enzymes involved in the inflammation process. Furthermore, small doses of phytosomes can serve as anti-inflammatory agents. Full article

This work aims to assess the bioavailability and bioaccumulation of Cr, Cu, Pb, and Zn in the soil–plant system (Erigeron canadensis L.) in the zone of anthropogenic impact in Dnipro city, a significant industrial and economic centre of Ukraine. Sampling was carried out at three locations at distances of 1.0 km, 5.5 km, and 12.02 km from the main emission sources associated with battery production and processing plants in Dnipro. The concentrations of heavy metals such as Cr, Cu, Pb, and Zn were analysed using atomic emission spectrometry from soil and parts of Erigeron canadensis L. The highest concentrations of elements in the soil, both for the mobile form and the total form, were determined to be 48.96 mg kg⁻¹ and 7830.0 mg kg⁻¹, respectively, for Pb in experimental plot 1. The general ranking of accumulation of elements in all experimental plots, both for the plant as a whole and for its parts, was as follows: Zn > Cu > Cr > Pb. Zn for plants was the most available heavy metal among all studied sites and had the highest metal content in the plant (339.58 mg kg⁻¹), plant uptake index (PUI-506.84), bioabsorption coefficient (BAC-314.9), and bioconcentration coefficient (BCF-191.94). According to the results of the study, it is possible to evaluate Erigeron canadensis L. as a hyperaccumulator of Zn, Cu, and Cr and recommend it for phytoextraction of soils contaminated with Zn, Cu, and Cr and phytostabilization of soils contaminated with Pb. Full article

This study investigates the effectiveness of Chlorella vulgaris in treating copper, cadmium, and zinc in aqueous solutions; the aim of this study was to examine the effects of various factors on the adsorption capacity of Chlorella in water. This study explored the intra- and extracellular adsorption and accumulation patterns of copper (Cu(II)), cadmium (Cd(II)), and zinc (Zn(II)), revealing their molecular response mechanisms under the most suitable conditions. The adsorption capacity of Chlorella to Cu(II), Cd(II), and Zn(II) in water was 93.63%, 73.45%, and 85.41%, respectively. The adsorption mechanism for heavy metals is governed by both intracellular and extracellular diffusion, with intracellular absorption serving as a supplement and external uptake predominating. XRD, XPS, FTIR, SEM-EDX, and TEM-EDX analyses showed that there would be the formation of precipitates such as Cu₂S, CuS₂, CdS, and ZnSO₄. The adsorption of Cu(II) involves its simultaneous reduction to Cu(I). Moreover, specific functional groups present on the cellular surface, such as amino, carboxyl, aldehyde, and ether groups, interact with heavy metal ions. In view of its efficient heavy metal adsorption capacity and biosafety, this study recommends Chlorella as a potential biosorbent for the bioremediation and environmental treatment of heavy metal contaminated water in the future. Full article

Nonsteroidal anti-inflammatory drugs (NSAIDs) are class II biopharmaceutics classification system drugs. The poor aqueous solubility of NSAIDs can lead to limited bioavailability after oral administration. Metformin (MET), a small-molecule compound, can be used in crystal engineering to modulate the physicochemical properties of drugs and to improve the bioavailability of orally administered drugs, according to the literature research and preliminary studies. We synthesized two drug–drug molecular salts (ketoprofen–metformin and phenylbutazone–metformin) with NSAIDs and thoroughly characterized them using SCXRD, PXRD, DSC, and IR analysis to improve the poor solubility of NSAIDs. In vitro evaluation studies revealed that the thermal stability and solubility of NSAIDs-MET were substantially enhanced compared with those of NSAIDs alone. Unexpectedly, an additional increase in permeability was observed. Since the structure determines the properties, the structure was analyzed using theoretical calculations to reveal the intermolecular interactions and to explain the reason for the change in properties. The salt formation of NSAIDs with MET could substantially increase the bio-absorption rate of NSAIDs, according to the in vivo pharmacokinetic findings, which provides an experimental basis for developing new antipyretic and analgesic drugs with rapid onset of action. Full article

Ruan Hua Tang (RHT) and Ruan Hua Fang (RHF) are two Chinese herbal mixtures that have been used in clinical cancer treatment for decades. This study validated our hypothesis that RHT and RHF can inhibit lung tumor development in the mouse model of Benzo(a)pyrene-induced lung tumorigenesis. An RHT oral solution was diluted to 9% and 18% in water. RHF was mixed into the diet at 15% and 30% of total food in the final doses. Two weeks after injecting BP into mice, we administered RHT and RHF for eighteen weeks. We found that 9% and 18% RHT reduced tumor multiplicity by 36.05% and 38.81% (both p < 0.05) and the tumor load by 27.13% and 55.94% (p < 0.05); 15% and 30% RHF inhibited tumor multiplicity by 12.75% and 39.84% (p < 0.01) and the tumor load by 18.38% and 61.68% (p < 0.05). Ki67 expressions in the 9% and 18% RHT groups were 19.55% and 11.51%, significantly lower than in the control (33.64%). The Ki67 levels in the 15% and 30% RHF groups were 15.56% and 14.04%, significantly lower than in the control (27.86%). Caspase 3 expressions in the 9% and 18% RHT groups were 5.24% and 7.32%, significantly higher than in the control (2.39%). Caspase 3 levels in the 15% and 30% RHF groups were 6.53% and 4.74%, significantly higher than in the control (2.07%). The bio-absorption was confirmed via a pharmacokinetic test. This study showed that RHT and RHF are safe and can inhibit lung tumor development, with anti-proliferative and pro-apoptotic effects. Full article

Alzheimer’s disease (AD) is a neurodegenerative disorder characterized by the deposition of amyloid β-peptide (Aβ) and subsequent oxidative inflammatory response, leading to brain damage and memory loss. This study explores the potential of Antrodia cinnamomea (AC), a Taiwan-native fungus known for its anti-inflammatory and antioxidant properties. The metabolites of AC, including dehydroeburicoic acid (DEA), 4-acetylantroquinonol B (4-AAQB), dehydrosulphurenic acid (DSA), and polysaccharides, were of particular interest. In the experiment, deep ocean water (DOW) was used to facilitate the solid-state fermentation of Antrodia cinnamomea NTTU 206 (D-AC), aiming to enhance its functional components. The impact of D-AC on the modulation of AD-related risk factors and the augmentation of cognitive abilities was subsequently evaluated in an AD rat model. This model was established via consecutive infusions of Aβ40 into the brain over a 28-day period. The administration of D-AC resulted in remarkable improvements in the rats’ reference memory, spatial probe test, and working memory. Notably, it restored the hippocampal magnesium levels by upregulating the expression of the magnesium transporter MAGT1. Concurrently, D-AC significantly downregulated the expressions of β-secretase 1 (BACE1) and the phosphorylated tau protein (p-tau), which were both implicated in AD progression. Additionally, it mitigated inflammatory responses, as suggested by the decreased levels of tumor necrosis factor α (TNF-α), interleukin-1β (IL-1β), and interleukin-6 (IL-6) in the hippocampus and cerebral cortex. Ultimately, the ability of D-AC to restore the brain magnesium levels, attenuate inflammatory responses, and reduce hippocampal Aβ40 deposition led to significant improvements in the cognitive decline of AD rats. D-AC demonstrated a comparable efficacy with its counterpart, AC fruiting bodies (F-AC group), despite their componential differences. This study underscores the potential of D-AC, enriched through fermentation, as a novel dietary strategy for Alzheimer’s disease prevention. Full article

The health benefits of polyphenols are based on their bioavailability, which is why a significant portion of research focuses on factors that affect their bioavailability. Previous studies suggest that the intake of polyphenols along with macronutrients in food represents one of the key factors influencing the bioavailability of polyphenols and, consequently, their biological activity in the organism. Since polyphenols in the human diet are mainly consumed in food together with macronutrients, this study investigated the in vivo absorption, metabolism, and distribution of polyphenolic compounds from the water extract of blackthorn flower (Prunus spinosa L.) in combination with a protein-enriched diet in the organs (small intestine, liver, kidney) of C57BL/6 mice. The bioaccumulation of polyphenol molecules, biologically available maximum concentrations of individual groups of polyphenol molecules, and their effect on the oxidative/antioxidative status of organs were also examined. The results of this study indicate increased bioabsorption and bioavailability of flavan-3-ols (EC, EGCG) and reduced absorption kinetics of certain polyphenols from the groups of flavonols, flavones, and phenolic acids in the organs of C57BL/6 mice after intragastric administration of the water extract of blackthorn flower (Prunus spinosa L.) in combination with a diet enriched with whey proteins. Furthermore, subchronic intake of polyphenols from the water extract of blackthorn flower (Prunus spinosa L.) in combination with a diet enriched with whey proteins induces the synthesis of total glutathione (tGSH) in the liver and superoxide dismutase (SOD) in the liver and small intestine. The results of this study suggest potential applications in the development of functional foods aimed at achieving the optimal health status of the organism and the possibility of reducing the risk of oxidative stress-related disease. Full article

In this work, the path from the cultivation of Arthrospira platensis at an increased concentration of CO₂ to the production of bio-oil by hydrothermal liquefaction (HTL) of the grown biomass is realized. The cultivation was carried out in a 90 L photobioreactor at an initial CO₂ concentration of 8 vol.% for 15 days. During the cultivation stage, the optical density for microalgae suspension, pH and chemical composition of nutrient medium were monitored. The grown biomass was separated from the nutrient medium with a 100 µm mesh and then subjected to HTL at 330 °C for 1 h. The biomass growth rate was 82 ± 4.1 mg × L⁻¹day⁻¹ and the pH was in the range from 9.08 ± 0.22 to 8.9 ± 0.24. Biochemical and CHNS analyses were applied for the obtained biomass. The contents of carbohydrates, proteins and lipids in the grown biomass were 38.7 ± 0.4 wt.%, 37.4 ± 0.5 wt.% and 3.8 ± 0.4 wt.%, respectively. Bio-oil yield after the HTL procedure was 13.8 wt.%. The bio-oil composition and properties were determined by GH-MS, TLC-PID and ICP-MS techniques. ICP-MS revealed the contents of 51 metals in bio-oil. Full article

Tissue engineering and regenerative medicine have emerged as innovative approaches to enhance clinical outcomes by addressing tissue lesions and degenerations that can significantly impair organ function. Since human tissues have limited regenerative capacity, the field of regenerative medicine aims to restore damaged tissues and their functionalities. Recent decades have witnessed remarkable progress in materials science, tissue engineering, and medicine, leading to the development of regenerative engineering. This interdisciplinary field has revolutionized the production of artificial matrices, enabling the design of anatomically accurate structures with enhanced biocompatibility, bioabsorption, and cell adhesion. Among the techniques utilized for fabricating cellular scaffolds, the electrospinning of fibers stands out as an ideal approach due to its ability to mimic the characteristics of the extracellular matrix (ECM). Electrospun scaffolds exhibit distinct advantages, including a high surface area-to-volume ratio, exceptional porosity, uniformity, compositional diversity, structural flexibility, and the ease of functionalization with bioactive molecules for controlled release. These versatile properties allow for the creation of nanofiber scaffolds that closely resemble the architecture of the ECM. Consequently, they facilitate the transport of nutrients and oxygen to cells as well as the incorporation of growth factors to stimulate cell growth. These advancements open up a wide range of applications in the field of regenerative medicine. Full article

Research has confirmed that the utilisation of Antarctic microorganisms, such as bacteria, yeasts and fungi, in the bioremediation of diesel may provide practical alternative approaches. However, to date there has been very little attention towards Antarctic microalgae as potential hydrocarbon degraders. Therefore, this study focused on the utilisation of an Antarctic microalga in the bioremediation of diesel. The studied microalgal strain was originally obtained from a freshwater ecosystem in Paradise Bay, western Antarctic Peninsula. When analysed in systems with and without aeration, this microalgal strain achieved a higher growth rate under aeration. To maintain the growth of this microalga optimally, a conventional one-factor-at a-time (OFAT) analysis was also conducted. Based on the optimized parameters, algal growth and diesel degradation performance was highest at pH 7.5 with 0.5 mg/L NaCl concentration and 0.5 g/L of NaNO₃ as a nitrogen source. This currently unidentified microalga flourished in the presence of diesel, with maximum algal cell numbers on day 7 of incubation in the presence of 1% v/v diesel. Chlorophyll a, b and carotenoid contents of the culture were greatest on day 9 of incubation. The diesel degradation achieved was 64.5% of the original concentration after 9 days. Gas chromatography analysis showed the complete mineralisation of C₇–C₁₃ hydrocarbon chains. Fourier transform infrared spectroscopy analysis confirmed that strain WCY_AQ5_3 fully degraded the hydrocarbon with bioabsorption of the products. Morphological and molecular analyses suggested that this spherical, single-celled green microalga was a member of the genus Micractinium. The data obtained confirm that this microalga is a suitable candidate for further research into the degradation of diesel in Antarctica. Full article

Cannabidiol (CBD) is a non-psychoactive cannabinoid, and available evidence suggests potential efficacy in the treatment of many disorders. DehydraTECH™2.0 CBD is a patented capsule formulation that improves the bioabsorption of CBD. We sought to compare the effects of CBD and DehydraTECH™2.0 CBD based on polymorphisms in CYP P450 genes and investigate the effects of a single CBD dose on blood pressure. In a randomized and double-blinded order, 12 females and 12 males with reported hypertension were given either placebo capsules or DehydraTECH™2.0 CBD (300 mg of CBD, each). Blood pressure and heart rate were measured during 3 h, and blood and urine samples were collected. In the first 20 min following the dose, there was a greater reduction in diastolic blood pressure (p = 0.025) and mean arterial pressure MAP (p = 0.056) with DehydraTECH™2.0 CBD, which was probably due to its greater CBD bioavailability. In the CYP2C9*2*3 enzyme, subjects with the poor metabolizer (PM) phenotype had higher plasma CBD concentrations. Both CYP2C19*2 (p = 0.037) and CYP2C19*17 (p = 0.022) were negatively associated with urinary CBD levels (beta = −0.489 for CYP2C19*2 and beta = −0.494 for CYP2C19*17). Further research is required to establish the impact of CYP P450 enzymes and the identification of metabolizer phenotype for the optimization of CBD formulations. Full article