Search Results (81)

Background/Objectives: Diabetes mellitus-induced erectile dysfunction (DMED) is characterized by severe endothelial and smooth-muscle dysfunction and reduced responsiveness to conventional therapy. Guanxinning tablet (GXN), a traditional Chinese medicine compound containing Salvia miltiorrhiza (Danshen) and Ligusticum stratum (Chuanxiong), has vascular-protective and anti-oxidative properties, but its effect on DMED remains unclear. This study evaluated whether GXN improves erectile function in a streptozotocin (STZ)-induced type 1 diabetic rat model and explored the possible involvement of PI3K/Akt/FOXO1 signaling. Methods: STZ-induced diabetic rats with ED were treated with GXN. Artery pressure (AP) and intracavernous pressure (ICP) were measured to evaluate erectile dysfunction. Western blots, immunohistochemistry, immunofluorescence, biochemical assays, TUNEL staining, RNA-seq, and in vitro HCMEC assays were performed to evaluate erectile effector cell function, oxidative stress, fibrosis, apoptosis, and PI3K/Akt/FOXO1-associated changes. Results: GXN improved erectile function in DMED rats and was associated with improved endothelial and smooth-muscle-related markers, reduced oxidative stress, attenuated fibrosis, and decreased apoptosis. RNA-seq and protein validation suggested that GXN treatment was associated with activation of PI3K/Akt/FOXO1-related signaling. In HCMECs, LY294002 (a PI3K inhibitor) partially reversed the GXN-associated improvement in cell viability and apoptosis-related markers. Conclusions: GXN ameliorated erectile dysfunction and tissue injury in STZ-induced type 1 diabetic rats, which were associated with PI3K/Akt/FOXO1 signaling. These findings support the potential of GXN as a traditional Chinese medicine compound for treating DMED. Full article

Oral diseases cause a wide range of difficulties for patients. The natural bioactive compound dihydroquercetin (DHQ), which demonstrates regenerative, anti-inflammatory, antioxidative, and antibacterial effects, is of interest for their treatment. The combination of DHQ and l-lysine DHQ is “very easily soluble”. The aim of this study is to compare orally disintegrating tablets based on raw DHQ and on the DHQ-l-lysine composition. Following the guidelines outlined in the ICH Q8 (R2) standard, a fundamental quality target product profile and critical quality attributes were established. The Sediment Delivery Model (SeDeM) method was used to evaluate the substance suitability for direct compression. Quantitative analysis of the DHQ release was carried out by high-performance liquid chromatography, and infrared (IR) spectroscopy was performed using the attenuated total reflection technique without any prior sample preparation. The DHQ-l-lysine composition shows improved dimensions (4.12) and flowability (4.96). The release rate constants (K_release) were 8.14 and 3.61%/min, while the half-release periods (t_50%) were 6.14 and 13.85 min for tablets with DHQ (TF1) and DHQ-l-lysine compositions (TF2), respectively. The difference factor (f₁) and similarity factor (f₂) were 23.43% and 43.37%, respectively. The tablet manufacture had a critical impact on the characteristics of the IR spectra (the r values −0.8785 and 0.5474 for TF1 and TF2). The conducted study demonstrates the promise of using DHQ-l-lysine composition for developing effective dosage forms with improved technological characteristics and controlled release of the active substance. Full article

Background: Hugan tablets (HGP) are a commercially available traditional Chinese medicine preparation used for liver disorders, but the mechanisms underlying their effects on alcoholic liver injury (ALI) remain incompletely understood. This study investigated the hepatoprotective effects and potential mechanisms of HGP in ALI. Methods: An ALI mouse model was established using a Lieber–DeCarli ethanol liquid diet. The effects of HGP were evaluated using biochemical and histopathological assessments, followed by integrated liver and serum metabolomics, liver transcriptomics, and ELISA-based protein validation. Results: HGP alleviated alcohol-induced liver injury, hepatic lipid accumulation, oxidative stress, and inflammatory responses. Integrated multi-omics analyses indicated that HGP treatment was associated with changes in hepatic glutathione metabolism, PPAR signaling, and antioxidant-related processes. ELISA validation showed increased measured concentrations in liver homogenate supernatants of PPARγ, NRF2, GCL, and GPX4 following HGP treatment. These findings support the potential involvement of a PPARγ/NRF2/GPX4-related antioxidant network. Conclusions: HGP alleviated ALI in mice, and its effects may be associated with modulation of hepatic glutathione metabolism and a PPARγ/NRF2/GPX4-related antioxidant network. These findings provide experimental evidence for the potential use of HGP in alcohol-induced liver injury. Full article

Modulation of cholesterol metabolism and reduction in serum cholesterol are key strategies for preventing cardiovascular diseases (CVDs). Functional foods enriched with dietary fiber and phytochemicals have attracted increasing attention for their potential health benefits. In this study, milk tablets containing kale and carrot (KC) were developed and preliminarily evaluated for their cholesterol-lowering potential. KC milk tablets were rich in dietary fiber, contained gallic acid, and exhibited antioxidant properties. They also supported the growth of Lactobacillus casei and Bifidobacterium longum in vitro, accompanied by increased SCFA production. In an open-label, pre–post exploratory study in hypercholesterolemic subjects, daily consumption for 6 weeks was associated with significantly increased HDL-C and reduced LDL-C levels. In addition, circulating ApoB100 and HMGCR levels were reduced, whereas ApoE and TNF-α remained unchanged. Therefore, these preliminary findings suggest that KC milk tablets may accomplish beneficial changes in lipid profiles and support the potential of dietary fiber–phenolic interactions with enhanced SCFA production which might modulate cholesterol metabolism. However, in further studies, randomized controlled trials are required to understand the precise underlying mechanism. Full article

In this work, two-dimensional copper-based metal–organic frameworks (Cu-MOFs) nanozymes, including cuprous oxide-tetrakis (4-carboxyphenyl) porphyrin (Cu₂O-TCPP) and copper-cuprous oxide-tetrakis (4-carboxyphenyl) porphyrin (Cu-Cu₂O-TCPP), were synthesized, which exhibit dual ascorbate oxidase (AO) and peroxidase (POD)-like activities. The reductants, such as ascorbic acid (AA), can be oxidized by the cascade AO and POD catalysis on Cu-MOFs to oxidize p-phthalic acid (PTA) and generate fluorescence. Consequently, a fluorescence sensing platform for AA and other reducing substances was established. This platform offers potential for efficient and selective monitoring of reductive species and related antioxidant levels in food systems. The results showed that the two Cu-MOFs displayed favorable linear relationships (R² ≥ 0.99) for the detection of AA, glutathione (GSH) and L-cysteine (L-Cys). Their limits of detection (LOD) were 5.3 μM for Cu₂O-TCPP and 92.5 μM for Cu-Cu₂O-TCPP. Finally, by detecting real samples of vitamin C tablets and fruits, the accuracy of the two Cu-MOFs nanos enzymes was validated, with Cu₂O-TCPP showing higher accuracy. Full article

Background: Due to its richness in bioactive compounds and health-promoting properties, beetroot is widely used in dietary supplements available in the form of powder, tablets, capsules, as well as in the form of beetroot juice and beetroot kvass. Methods: In this study, the antioxidant potential of selected beetroot supplements in solid form and beetroot drinks available on the Polish market was compared using ABTS⁺ and DPPH radical scavenging assays. Total polyphenol content was also determined using the Folin–Ciocalteu colorimetric method. The study material included two products each in powder, capsule, and tablet form, as well as three beetroot juices and three beetroot sourdoughs. Results: Among solid supplements, powders had the highest polyphenol content (up to 12.9 mg GAE/g) and the highest antioxidant potential, while the lowest values were recorded in tablets (4.20 mg GAE/g). When calculated per recommended dose, these differences were even more pronounced (129 mg GAE/dose for powders vs. 0.67 mg GAE/dose for tablets). In the liquid product group, beetroot juices contained significantly more polyphenols than sourdoughs (up to 2828 vs. 230 mg GAE/100 mL) and showed higher antioxidant activity, especially in the DPPH test. Conclusions: Based on the results obtained, it was found that among solid supplements, powders had the highest polyphenol content and the highest antioxidant potential, especially when calculated per recommended dose. In the group of liquid products, juices showed higher antioxidant activity, especially in the DPPH test, compared to beetroot leaven. Full article

Background: Nutraceuticals are increasingly used in clinical practice for their anti-inflammatory, antiproliferative, and antioxidant properties. This study aimed to evaluate the safety and efficacy of a fixed nutraceutical combination containing chondroitin sulfate, α-lipoic acid, astaxanthin, lycopene, escin, and omega-3 fatty acids (eicosapentaenoic acid and docosahexaenoic acid) in improving pain and quality of life in patients with chronic knee osteoarthritis (OA). Methods: This observational study included patients with chronic knee OA who were referred to the ambulatory pain clinic at Dulbecco University Hospital, Catanzaro, Italy. Participants received one tablet daily for three months. Quality of life was assessed using the 36-Item Short Form Health Survey (SF-36), and adverse drug reactions (ADRs) were evaluated using the Naranjo scale. Results: Fifty patients (20 men and 30 women; mean age, 63.6 ± 11.4 years; range, 26–88 years; mean body mass index, 26.9 ± 3.7 kg/m²) were enrolled. Pain symptoms demonstrated a statistically significant improvement over time (p < 0.01). No ADRs were reported during the study period. Conclusions: The fixed nutraceutical combination improved pain and quality of life in patients with chronic knee OA and demonstrated an excellent safety profile. Full article

Background/Objectives: Rutin, a bioactive flavonol glycoside known for its antioxidant, anti-inflammatory, and anticancer activities, faces limited clinical application due to its poor aqueous solubility and low oral bioavailability. This study aimed to enhance the dissolution of rutin by preparing solid dispersions (SDs) using a fluid-bed coating system and formulating the resulting SDs into tablet dosage forms. Methods: Rutin was dissolved in methanol and sprayed onto various carriers, including lactose monohydrate, mannitol, microcrystalline cellulose, silicon dioxide, and calcium carbonate. Results: Among the carriers tested, lactose monohydrate produced the highest dissolution enhancement, achieving complete drug release within 15 min versus approximately 60% for free rutin. Further investigation into the effect of the rutin-to-lactose ratio on dissolution enhancement identified 1:10 as the most effective. Characterization by powder X-ray diffraction (PXRD) and differential scanning calorimetry (DSC) confirmed a marked reduction in rutin crystallinity, while scanning electron microscopy (SEM) revealed reduced particle size and successful adsorption onto the carrier. Fourier transformed infrared (FT-IR) analysis suggested hydrogen bonding interactions between rutin and lactose monohydrate, which contributed to improved dissolution. The optimal SD was incorporated into tablets containing 50 mg of rutin via wet granulation, and the inclusion of sodium lauryl sulfate further enhanced dissolution. Stability testing demonstrated that the optimized tablets maintained their dissolution profile after 6 months under accelerated conditions (40 °C and 75% RH). Conclusions: These findings indicate that fluid-bed coating is an effective approach for preparing SDs to improve the dissolution of rutin and may be extended to other natural polyphenolic compounds. Full article

Given the limited data in the recent literature regarding spirulina cultivated in Greece, the present study aimed to investigate physicochemical parameters (pH, color), antioxidant activity, and phytochemical content (total phenolic content, quercetin, caffeic acid, C-phycocyanin) of spirulina (Arthrospira platensis) obtained through conventional and organic cultivation methods in different forms (disk-shaped tablets, powder, and flakes) and using different solvents [water and ethanol of grape origin (EEGO)]. Furthermore, the antimicrobial activity of spirulina against selected food pathogens, namely Salmonella Typhimurium, Staphylococcus aureus, Listeria monocytogenes, and Escherichia coli O157:H7, was also investigated. Results showed that the form of spirulina and the solvent used significantly (p < 0.05) affected the physicochemical parameters, antioxidant activity, and phytochemical compounds. Spirulina had a neutral to alkaline pH (6.79 ± 0.02 to 8.24 ± 0.01) and a considerable number of pigments, including C-phycocyanin (0.07 ± 0.01 to 1.65 ± 0.01 mg/mL). The most pronounced effects were recorded in the case of antioxidant activity, where EEGO proved to be the best solvent for the extraction of compounds with antioxidant activity (44.37 ± 2.28% to 48.28 ± 0.39%) against the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical. In contrast, water proved to be the best solvent for the recovery of total phenolics (4.83 ± 0.55 mg/g DM to 17.07 ± 0.66 mg/g DM), primarily in spirulina powder. Regarding the antibacterial activity, spirulina, primarily in powder and tablet form (in both solvents), showed considerable inhibition zones against the studied food pathogens. The present study presents new knowledge concerning spirulina cultivated in Greece in terms of physicochemical parameters, antioxidant activity, phytochemical content, and antibacterial activity. Full article

Background and Objectives: Metabolic syndrome (MetS) is characterized by a cluster of factors, including dyslipidemia, insulin resistance, central obesity, elevated blood pressure, and impaired fasting glucose, which together elevate the risk of type 2 diabetes and cardiovascular disease. Nutraceuticals containing botanical extracts with antioxidant and metabolic activity have emerged as promising adjunctive strategies in the management of MetS. This study evaluated the clinical effectiveness and biological rationale of a standardized food supplement (QUINOLAM), containing extracts of Cydonia oblonga (quince), Olea europaea (olive leaf), and Amaranthus spp., in adults with metabolic syndrome. Materials and Methods: This was a retrospective, single-center observational study including adults with documented MetS who received one tablet daily of the QUINOLAM-based supplement for at least 12 weeks. The primary endpoint was the change in total cholesterol. Secondary endpoints included LDL-C, HDL-C, triglycerides, fasting glucose, HbA1c, HOMA-IR, CRP, and BMI. In parallel, preclinical studies were conducted using HepG2 cells to investigate QUINOLAM’s effects on LDL receptor expression, glucose uptake, antioxidant activity, and cell viability. Results: Thirty patients met the inclusion criteria. A significant reduction in total cholesterol was observed at both 6 and 12 weeks (p < 0.005), accompanied by a significant decline in LDL-C by week 12 (p < 0.05). Among patients with baseline fasting glucose ≥100 mg/dL (n = 19), a significant improvement in glycemia was recorded (p < 0.005). Trends toward improvement were noted in other metabolic indices. In vitro, QUINOLAM enhanced LDL receptor expression (p < 0.05) and glucose uptake (p < 0.01), demonstrated antioxidant activity in the TEAC assay, and showed no cytotoxicity at relevant doses. Conclusions: In a real-world setting, daily supplementation with QUINOLAM was associated with significant improvements in lipid and glycemic control among patients with MetS. Preclinical findings further support its mechanistic plausibility via modulation of LDL handling, glucose metabolism, and oxidative stress. These results warrant confirmation in larger, prospective clinical trials. Full article

Background/Objectives: Neuropathic pain, resulting from damage or pathology affecting the somatosensory nervous system, is a prevalent form of chronic pain that significantly impacts quality of life. Combined therapies are often utilised to manage this condition. Three-dimensional printing (3DP) offers a promising approach for personalising medication doses and dosage forms to meet individual patient needs. Methods: In this study, a formulation suitable for 3D printing was developed using magnesium citrate, uridine monophosphate, vitamins B₃ (niacin), B₆ (pyridoxine), B₁₂ (cobalamin), B₉ (folic acid), and spermidine to create a novel gel-based oral tablet for the targeted treatment of neurological pain. The antioxidant potential of the active pharmaceutical ingredients (APIs) was assessed using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) methods. The physical properties of the tablets were evaluated using a texture analyser, while the in vitro release profiles were determined by high-performance liquid chromatography (HPLC). Results: Results demonstrated that pectin–gelatin tablets hardened over time, with higher citric acid concentrations further enhancing this effect. Formulation AVII exhibited good hardness and low stickiness. Formulation AV, however, showed poor performance across all physical parameters and lacked sufficient structural integrity for practical application. While uridine monophosphate, B₁₂, and B₉ showed no significant differences in the release profiles of the tablets, spermidine, B₆, and B₃ displayed statistically significant variations. Specifically, AVII outperformed AV in terms of spermidine and B₆ release, and AV showed a higher release of B₃ compared to AV. Conclusions: The AVII tablet demonstrates potential for use in combined therapy targeting neurological pain disorders. Full article

Background/Objectives: Rhodiola rosea L. (Crassulaceae), a perennial adaptogenic herb native to Northern Europe, Asia, and North America, is renowned for its therapeutic properties attributed to phenolic compounds including flavonoids, phenylethanoids, phenylpropanoids, and cinnamyl alcohol glycosides. The plant’s antioxidant and anti-inflammatory activities align with its traditional use in boosting physical and cognitive performance, reducing fatigue, and improving stress resilience. However, conventional dosage forms present compliance challenges, particularly for vulnerable populations with swallowing difficulties. This study aimed to develop and optimize orally disintegrating tablets (ODTs) containing standardized Rhodiola rosea root and rhizome (RR) dry extract to ensure rapid disintegration and acceptable taste, thereby improving patient compliance. Methods: Dried Rhodiola rosea root and rhizome (particle size 2–3 mm) were extracted using 70% m/m ethanol using the fractionated maceration methodology. The resulting dry RR extract was standardized to 3.0% m/m rosavin content by blending batches of the extract and analyzed using validated chromatographic methods. The standardized dry extract was formulated into ODTs via direct compression technology. Various excipients were evaluated to achieve rapid disintegration while masking the characteristic bitter taste of RR extract. Results: The optimized ODT formulation (500 mg, 11 mm ø, 20% standardized RR dry extract) disintegrated within 3 min and effectively masking the characteristic bitterness of the RR extract. The formulation maintained content uniformity and did not exhibit loss of active compounds during processing, meeting European Pharmacopoeia requirements for ODTs. Conclusions: The developed ODTs containing standardized Rhodiola rosea extract offer a patient-friendly alternative for oro-mucosal administration, supporting improved compliance in populations with swallowing difficulties while retaining the extract’s phytochemical integrity and sensory acceptability. Full article

Background: Chronic pain represents a major therapeutic challenge due to the limited efficacy and tolerability of conventional pharmacological treatments. Equisetum arvense L., a medicinal plant with potent antioxidant properties, and palmitoylethanolamide (PEA), an endogenous fatty acid amide with well-established anti-inflammatory and analgesic effects, are increasingly recognised as promising nutraceutical agents. Methods: This prospective, single-centre clinical trial aimed to evaluate the efficacy and safety of a novel oral supplement (Assonal^®PEA) combining 600 mg of PEA and 300 mg of Equisetum arvense L. in improving the reduction of pain and quality of life in patients with chronic pain, also obtaining information on the patient’s state of satisfaction after the treatment. Fifty patients suffering from chronic pain (low back pain and radiculopathy) for two months were enrolled and received the supplement over eight weeks in a tapered regimen (two tablets daily for two weeks, followed by one tablet daily). Results: Clinical outcomes were evaluated using validated instruments, including the Numeric Pain Rating Scale (NPRS), Verbal Rating Scale (VRS), Short-Form McGill Pain Questionnaire (SF-MPQ), Global Perceived Effect (GPE), and EuroQol-5D-5L. Results showed a significant decrease in pain intensity (NPRS: −3.8 points; VRS: −2.1 points; p < 0.0001), along with meaningful improvements in patient-perceived benefit, pain descriptors, and quality of life (EQ-5D-5L: +35%; p < 0.0001). Conclusions: These findings endorse the use of this novel PEA–Equisetum arvense formulation as a safe, well-tolerated, and potentially effective supplementary intervention for managing chronic pain. No adverse events were reported, and the overall response rate reached 94%. Full article

Antioxidant nanomaterials, particularly mesoporous silica nanoparticles (MSNs) functionalized with polyphenols, offer innovative solutions for protecting oxidation-sensitive components and enhancing bioavailability in pharmaceuticals or extending the shelf life of nutraceutical and food products. This study investigates the influence of MSNs functionalized with caffeic acid (MSN-CAF) on powder flow properties and their tableting performance. Aminated MSNs were synthesized via co-condensation and conjugated with caffeic acid using EDC/NHS chemistry. Antioxidant capacity was evaluated using DPPH^●, ABTS^●+, ORAC, and FRAP assays. Powder blends with varying MSN-CAF concentrations (10–70%) were characterized for flow properties (angle of repose, Hausner ratio, Carr’s index), tablets were produced via direct compression, and critical quality attributes (weight uniformity, hardness, friability, disintegration, nanoparticle release) were assessed. MSN-CAF exhibited reduced antioxidant capacity compared with free caffeic acid due to pore entrapment but retained significant activity. Formulation F1 (10% MSN-CAF) showed excellent flowability (angle of repose: 12°, Hausner ratio: 1.16, Carr’s index: 14%), enabling robust tablet production with rapid disintegration, low friability, and complete nanoparticle release in 10 min. Additionally, the antioxidant nanomaterial demonstrated biocompatibility with the HepG2 cell line. MSN-CAF is a versatile nanoexcipient for direct compression tablets, offering potential as an active packaging agent and delivery system in the nutraceutical and food industries. Full article

Glycyrrhiza glabra (licorice) has been used as an herbal medicine for a long time due to its anti-inflammatory, antioxidant, and antimicrobial properties. Additionally, multiple reports have demonstrated its ability to promote wound healing. Several randomized controlled or clinical trials (RCTs) have demonstrated its potentially therapeutic effects in oral mucosal diseases, especially in recurrent aphthous stomatitis (RAS). This systematic review aims to summarize the evidence for Glycyrrhiza glabra in treating RAS. A systematic search was performed across five databases: PubMed (Medline), ScienceDirect, Scopus document, Cochrane Central Register of Controlled Trials (CENTRAL), and the Cochrane Library Database of Systematic Reviews. This study was reported following the PRISMA guidelines. RCT study using Glycyrrhiza glabra for treating RAS was included in this study with several reported outcomes like changes in ulcer diameter, pain, and healing periods. Seven RCTs were included, which used Glycyrrhiza glabra in the form of patches, pastes, mucoadhesive tablets, and mouthwashes for treating RAS. Glycyrrhiza glabra treatment in various regimens showed significant improvements in pain, ulcer diameter, and healing time in patients with RAS. This review suggests the potential of Glycyrrhiza glabra as an alternative treatment option for RAS. Full article