Search Results (2,015)

Colchicine is a potent alkaloid with well-established anti-inflammatory properties. It shows significant promise in treating classic immune-mediated inflammatory diseases, as well as associated cardiovascular diseases, including atherosclerosis. However, its clinical use is limited by a narrow therapeutic window, dose-limiting systemic toxicity, variable bioavailability, and clinically significant drug–drug interactions, partly mediated by modulation of P-glycoprotein and cytochrome P450 3A4 metabolism. This review explores advanced delivery strategies designed to overcome these limitations. We critically evaluate lipid-based systems, such as solid lipid nanoparticles, liposomes, transferosomes, ethosomes, and cubosomes; polymer-based nanoparticles; microneedles; and implants, including drug-eluting stents. These systems ensure targeted delivery, improve pharmacokinetics, and reduce toxicity. Additionally, we discuss chemical derivatization approaches, such as prodrugs, codrugs, and strategic ring modifications (A-, B-, and C-rings), aimed at optimizing both the efficacy and safety profile of colchicine. Combinatorial nanoformulations that enable the co-delivery of colchicine with synergistic agents, such as glucocorticoids and statins, as well as theranostic platforms that integrate therapeutic and diagnostic functions, are also considered. These innovative delivery systems and derivatives have the potential to transform colchicine therapy by broadening its clinical applications while minimizing adverse effects. Future challenges include scalable manufacturing, long-term safety validation, and the translation of research into clinical practice. Full article

This study explores the development of a topical film-forming spray infused with phytobiotic herbs to extend egg shelf life and maintain its quality. Unlike traditional surface treatments, film-forming sprays provide uniform drug distribution, better bioavailability, effective CO₂ retention by sealing pores, and antibacterial effects. The spray includes a polymer to encapsulate phytoconstituents and form the film. The resulting film is highly water-resistant, glossy, transparent, and dries within two minutes. SEM analysis showed a fine, uniform morphology, while zeta analysis revealed a negative potential of −0.342 mV and conductivity of 0.390 mS/cm, indicating stable dispersion. The spray’s effectiveness was tested on 640 chicken eggs stored at varying temperatures. Eggs treated and kept at 2–8 °C showed the best results, with smaller air cells, higher specific gravity, and superior quality indicators such as pH, albumen weight, albumen height and index, Haugh unit, yolk weight, and yolk index. Additionally, the spray significantly reduced microbial load, including total plate count and E. coli. Eggs stored at 28 °C remained safe for 24–30 days, while those at 2–8 °C lasted over 42 days. This innovative film-forming spray offers a promising approach for preserving internal and external egg quality during storage. Full article

The incorporation of Cannabis sativa L. seeds into barley wort was investigated to enhance the functional profile of beer. Hemp seeds (cv. Henola) were malted via controlled steeping, germination, and kilning, then added to barley malt at 10% and 30% (w/w) in both malted and unmalted forms. Standard congress mashing produced worts whose physicochemical parameters (pH, extract, colour, turbidity, filtration and saccharification times) were assessed, alongside profiles of fermentable sugars, polyphenols, B-group vitamins, and cannabinoids. Addition of hemp seeds reduced extract yield without impairing saccharification or filtration and slightly elevated mash pH and turbidity. Maltose and glucose levels declined significantly at higher hemp dosages, whereas sucrose remained stable. Wort enriched with 30% unmalted seeds exhibited the highest levels of trans-ferulic (20.61 µg/g), gallic (5.66 µg/g), trans-p-coumaric (3.68 µg/g), quercetin (6.07 µg/g), and trans-cinnamic (4.07 µg/g) acids. Malted hemp addition enhanced thiamine (up to 0.302 mg/mL) and riboflavin (up to 178.8 µg/mL) concentrations. Cannabinoids (THCA-A, THCV, CBDV, CBG, CBN) were successfully extracted at µg/mL levels, with the total cannabinoid content peaking at 14.59 µg/mL in the 30% malted treatment. These findings demonstrate that hemp seeds, particularly in malted form, can enrich barley wort with bioactive polyphenols, vitamins, and non-psychoactive cannabinoids under standard mashing conditions, without compromising key brewing performance metrics. Further work on fermentation, sensory evaluation, stability, and bioavailability is warranted to realise hemp-enriched functional beers. Full article

Appropriate carriers or templates are crucial for maintaining the stability, biological activity, and bioavailability of selenium nanoparticles (SeNPs). Selecting suitable templates remains challenging for fully utilizing SeNPs functionalities and developing applicable products. Exosome-like nanoparticles (ELNs) have gained importance in drug delivery systems, yet research on selenium products prepared using exosomes remains limited. To address this gap, we utilized Cyperus bean ELNs to deliver SeNPs, investigated three preparation methods for SeNPs-ELNs, identified the optimal approach, and performed characterization studies. Notably, all three methods successfully loaded SeNPs. Ultrasonic cell fragmentation is the optimal approach, achieving significant increases in selenium loading (5.59 ± 0.167 ng/μg), enlargement of particle size (431.17 ± 10.78 nm), and reduced absolute zeta potential (−4.1 ± 0.43 mV). Moreover, both exosome formulations demonstrated enhanced stability against aggregation during storage at 4 °C, while their stability varied with pH conditions. In vitro digestibility tests showed greater stability of SeNP-ELNs in digestive fluids compared to ELNs alone. Additionally, neither ELNs nor SeNP-ELNs exhibited cytotoxicity toward LO₂ cells, and the relative erythrocyte hemolysis remained below 5% at protein concentrations of 2.5, 7.5, 15, 30, and 60 μg/mL. Overall, ultrasonic cell fragmentation effectively loaded plant-derived exosomes with nano-selenium at high capacity, presenting new opportunities for their use as functional components in food and pharmaceutical applications. Full article

Polysaccharides and phenols are commonly co-localized in various plant-derived foods, including highland barley (Hordeum vulgare L. var. nudum Hook. f.). The interactions between these compounds can influence multiple characteristics of food products, including their physicochemical properties and functional performance, such as bioavailability, stability, and digestibility, which may support promising application of the phenol and polysaccharide complex in health food industry. In this study, two complexes with potential existence in highland barley, such as β-glucan-ferulic acid (GF) and β-glucan-quercetin (GQ), were prepared using the equilibrium dialysis method in vitro. FTIR and SEM results showed that ferulic acid and quercetin formed complexes with β-glucan separately, with covalent and non-covalent bonds and a dense morphological structure. The pH value, reaction temperature, and concentration of phosphate buffer solution (PBS) were confirmed to have an impact on the formation and yield of the complex. Through the test of the response surface, it was found that the optimum conditions for GF and (GQ) preparations were a pH of 6.5 (6), a PBS buffer concentration of 0.08 mol/L (0.3 mol/L), and a temperature of 8 °C (20 °C). Through in vitro assays, GF and GQ were found to possess good antioxidant activity, with a greater scavenging effect of DPPH, ABTS, and hydroxyl radical than the individual phenolic acids and glucans, as well as their physical mixtures. Taking GF as an example, the DPPH radical scavenging capacity ranked as GF (71.74%) > ferulic acid (49.50%) > PGF (44.43%) > β-glucan (43.84%). Similar trends were observed for ABTS radical scavenging (GF: 54.56%; ferulic acid: 44.37%; PGF: 44.95%; β-glucan: 36.42%) and hydroxyl radical elimination (GF: 39.16%; ferulic acid: 33.06%; PGF: 35.51%; β-glucan: 35.47%). In conclusion, the convenient preparation method and excellent antioxidant effect of the phenol–polysaccharide complexes from highland barley provide new opportunities for industrial-scale production, development, and design of healthy food based on these complexes. Full article

Heavy metal-contaminated soil poses a severe threat to environmental quality and human health, calling for eco-friendly and efficient remediation strategies. This study explored the use of biochar-immobilized copper-resistant Pseudomonas aeruginosa to remediate copper-contaminated soil and promote growth of Chinese milk vetch (Astragalus sinicus L.). Indoor pot experiments compared four groups: copper-contaminated soil (control), soil with biochar, soil with free bacteria, and soil with biochar-immobilized bacteria (IM). Results showed IM had the most significant effects on soil properties: it raised pH to 7.04, reduced bioavailable copper by 34.37%, and increased catalase (3.48%) and urease (78.95%) activities. IM also altered soil bacterial communities, decreasing their richness and evenness (alpha diversity) while shifting community composition. For Chinese milk vetch, IM reduced leaf malondialdehyde (a marker of oxidative stress) by 15%, increased total dry weight by 90%, and lowered copper accumulation in roots (18.62%) and shoots (60.33%). As a nitrogen-fixing plant, the vetch’s nitrogen fixation in roots and shoots rose by 82.70% and 57.08%, respectively, under IM. These findings demonstrate that biochar-immobilized Pseudomonas aeruginosa is a promising in situ amendment for remediating copper-contaminated soil and boosting plant growth. Full article

Selenium (Se) is an important trace element in our body; however, food composition data remain limited due to analytical challenges and interferences. Seafood, abundant in Thailand, is recognized as a rich source of Se. This study aimed to expand knowledge on Se content in seafood prepared using traditional Thai cooking methods. Twenty seafood species were selected and prepared by boiling, frying, and grilling. Inductively Coupled Plasma–Triple Quadrupole–Mass Spectrometry (ICP-MS/MS) was used to analyze total Se contents in selected seafood species. Results revealed significant variation in Se content across species and cooking methods. The Indo-Pacific horseshoe crab showed the highest Se concentration, with fried samples reaching 193.9 μg/100 g. Se concentrations were in the range of 8.6–155.5 μg/100 g (fresh), 14.3–106.6 μg/100 g (boiled), 17.3–193.9 μg/100 g (fried), and 7.3–160.1 μg/100 g (grilled). Results found significant effects of species and cooking method on Se content (p < 0.05). Fried seafood exhibited the highest estimated marginal mean Se concentration (a 78.8 μg/100 g edible portion), significantly higher than other methods. True retention (%TR) of Se ranged from 40.4% to 100%, depending on species and method. Bigfin reef squid, wedge shell, and silver pomfret showed the highest %TR (100%), while splendid squid exhibited the lowest (52.5%). Significant interaction effects on %TR were also observed (p < 0.05). Fried seafood had the highest mean %TR (88.8%), followed by grilled (82.1%) and boiled (79.7%). These findings highlight the effects of both species and cooking method on Se retention, emphasizing the nutritional value of selected seafood in preserving bioavailable Se after cooking. Full article

Background/Objectives: Holy basil (Ocimum tenuiflorum L.) essential oil exhibits antioxidant, antimicrobial, and anesthetic activities, mainly due to eugenol, methyl eugenol, and β-caryophyllene. However, its clinical application is limited by poor water solubility, instability, and low bioavailability. This study developed and compared two delivery systems, self-nanoemulsifying drug delivery systems (SNEDDS) and microemulsions (ME), to enhance their stability and fish anesthetic efficacy. Methods: The optimized SNEDDS (25% basil oil, 8.33% coconut oil, 54.76% Tween 80, 11.91% PEG 400) and ME (12% basil oil, 32% Tween 80, 4% sorbitol, 12% ethanol, 40% water) were characterized for droplet size, PDI, zeta potential, pH, and viscosity. Stability was evaluated by monitoring droplet size and PDI over time and by determining the retention of eugenol, methyl eugenol, and β-caryophyllene after storage at 45 °C. Fish anesthetic efficacy was tested in koi carp (Cyprinus carpio var. koi). Results: SNEDDS maintained a small droplet size (~22.78 ± 1.99 nm) and low PDI (0.188 ± 0.088 at day 60), while ME showed significant size enlargement (up to 177.10 ± 47.50 nm) and high PDI (>0.5). After 90 days at 45 °C, SNEDDS retained 94.45% eugenol, 94.08% methyl eugenol, and 88.55% β-caryophyllene, while ME preserved 104.76%, 103.53%, and 94.47%, respectively. In vivo testing showed that SNEDDS achieved faster anesthesia (114.70 ± 24.80 s at 120 ppm) and shorter recovery (379.60 ± 15.61 s) than ME (134.90 ± 4.70 s; 473.80 ± 16.94 s). Ethanol failed to induce anesthesia at 40 ppm and performed poorly compared to SNEDDS and ME at other concentrations (p < 0.0001). Conclusions: SNEDDS demonstrated superior physical stability and fish anesthetic performance compared to ME. These findings support SNEDDS as a promising formulation for delivering holy basil essential oil in biomedical and aquaculture applications. Full article

The encapsulation of bioactive compounds using proteins as wall materials has emerged as an effective strategy to enhance their stability, bioavailability, and controlled release. Proteins offer unique functional properties, including amphiphilic behavior, gel-forming ability, and interactions with bioactives, making them ideal candidates for encapsulation. Animal-derived proteins, such as whey and casein, exhibit superior performance in stabilizing lipophilic compounds, whereas plant proteins, including soy and pea protein, demonstrate greater affinity for hydrophilic bioactives. Advances in protein modification and the formation of protein–polysaccharide complexes have further improved encapsulation efficiency, particularly for heat- and pH-sensitive compounds. This review explores the physicochemical characteristics of proteins used in encapsulation, the interactions between proteins and bioactives, and the main encapsulation techniques, including spray drying, complex coacervation, nanoemulsions, and electrospinning. Furthermore, the potential applications of encapsulated bioactives in functional foods, pharmaceuticals, and nutraceuticals are discussed, highlighting the role of emerging technologies in optimizing delivery systems. Understanding the synergy between proteins, bioactives, and encapsulation methods is essential for developing more stable, bioavailable, and sustainable functional products. Full article

Objectives: In this research study, we introduce a novel approach to develop an innovative nanocarrier system comprising gold nanoparticles (GNPs) loaded with doxorubicin (D) in combination with natural molecules, such as trans-resveratrol (R), piperine (P), and icariin (Ic), against human cervical cancer. The final objective is to improve the anticancer efficacy of doxorubicin on HeLa and CaSki cell lines. Methods: Resveratrol was also used for the synthesis of GNP_R1 nanoparticles. Multi-functional GNPs loaded with D, R, P, and Ic (e.g., GNP_R1@D/R/P/Ic) were successfully prepared and fully characterized by SPR, TEM, HR-TEM, XRD, AFM, DLS, and zeta potential. They were investigated for in vitro stability in various biological media. The cytotoxicity activity was tested on HeLa and CaSki cell lines, using the MTT assay, for their applications as anticancer agents. Results: Our results demonstrate that the novel multi-functional GNPs (such as GNP_R1@D/R and GNP_R1@D/R/P/Ic) can effectively target the cervical cancer cells, improving the bioavailability of therapeutic agents and enhancing their cytotoxicity against cervical cancer cells. In vitro assessments demonstrated that the multi-functional GNPs exhibited improved stability and potential anticancer efficacy on human cervical cancer cells. Conclusions: The described strategy connects the benefits of biomolecules with functional nanoparticles toward the development of various GNP_R1@D/R/P/Ic nanocarriers for their applications as anticancer agents against human cervical cancer. This study provides compelling evidence that the innovative nanoparticles can enhance the therapeutic efficacy of doxorubicin against cervical cancer and offer a more advantageous alternative compared to doxorubicin monotherapy. Full article

Poor solubility and bioavailability have limited the application of fucoxanthin in drug and functional food processing. In order to encapsulate fucoxanthin in delivery systems, in this study, cellulose was isolated from industrial brown algae residues and high-pressure homogenized into cellulose nanofibrils (CNFs). Then, fucoxanthin was encapsulated into the Pickering emulsion stabilized by the CNFs. The effect of high-pressure homogenization on the characteristics of cellulose and the stability of fucoxanthin emulsion was evaluated. The results indicated that CNFs prepared at 105 MPa had a diameter of 87 nm and exhibited high zeta potential and thermal stability. Encapsulation efficiency peaked at 70.8% with 1.0 mg/mL fucoxanthin, and after three freeze–thaw cycles the encapsulation efficiency was higher than 60%. The DPPH scavenging activity after 12 days’ storage at 4 °C was still 42%. Furthermore, the Pickering emulsion with 1.0 mg/mL fucoxanthin showed high stability and antioxidant activity under different pH values, salinity, temperature, and UV light exposure duration. The CNFs effectively protected fucoxanthin from degradation, offering a novel delivery system for marine bioactive compounds. To the best of our knowledge, this is the first study on the fucoxanthin delivery system of Pickering emulsion stabilized by the CNFs. Such emulsion might benefit the encapsulation and release of bioactive components in marine drugs. Full article

Background: Crystalline glucosamine sulfate (cGS) claims to be a stabilized form of glucosamine sulfate with a defined crystalline structure intended to enhance chemical stability. It is proposed to offer pharmacokinetic advantages over regular glucosamine sulfate (rGS) which is stabilized with potassium or sodium chloride. However, comparative human bioavailability data are limited. Since both forms dissociate in gastric fluid into constituent ions, the impact of cGS formulation on absorption remains uncertain. This pilot study aimed to compare the bioavailability of cGS and rGS using a randomized, double-blind, crossover design. Methods: Ten healthy adults received a single 1500 mg oral dose of either cGS or rGS with a 7-day washout between interventions. Capillary blood samples were collected over 24 h. Glucosamine and its metabolite concentrations were quantified by Liquid Chromatography-High Resolution Mass Spectrometry (LC-HRMS), and pharmacokinetic parameters—including maximum concentration (C_max), time to reach C_max (T_max), and area under the curve (AUC)—were calculated. Results: Mean AUC_0–24, C_max, T_max, and T_½ values for glucosamine and glucosamine-6-sulfate (GlcN-6-S) were comparable between cGS and rGS. Although the AUC_0–24 for glucosamine was modestly higher with rGS (18,300 ng·h/mL) than with cGS (12,900 ng·h/mL), the difference was not statistically significant (p = 0.136). GlcN-6-S exposure was also similar between formulations (rGS: 50,700 ng·h/mL; cGS: 50,600 ng·h/mL), with a geometric mean ratio of 1.39, a delayed T_max (6–8 h) and longer half-life, consistent with its role as a downstream metabolite. N-acetylglucosamine levels remained stable, indicating potential homeostatic regulation. Conclusions: This pilot study found no significant pharmacokinetic advantage of cGS over rGS. These preliminary findings challenge claims of cGS’ pharmacokinetic superiority, although the small sample size limits definitive conclusions. Larger, adequately powered studies are needed to confirm these results. Full article

Medicinal plants and animal-derived proteins represent valuable natural sources of bioactive components with pharmaceutical potential. Whilst some medicinal plants and animal-derived proteins also offer rich sources of anticoagulant bioactive peptides, their development faces multiple challenges: anticoagulant evaluation relies on single-parameter assays with limited reliability, native proteins demonstrate suboptimal activity without enzymatic treatment, and few researchers investigate bioavailable peptides. Our study establishes an innovative framework using the leech as a case study to overcome these barriers. A novel anticoagulant evaluation model was first established with the Critic-G1 weighting method. And we optimized the enzymatically hydrolyzed extracts with high activity using Box–Behnken response surface methodology. Subsequently, the everted gut sac model was implemented to simulate intestinal absorption and screen for absorbable peptide fractions. Furthermore, peptidomics was employed to identify the bioactive peptides. Lastly, we identified the bioactivity using anticoagulation assays. Results indicated that the optimal hydrolysis conditions were achieved with trypsin at 50.48 °C, an enzyme-to-substrate ratio of 6.78%, 7.51 h, and pH of 8.06. The peptide DLRWM was identified through integrated peptidomics and molecular docking approaches, with subsequent activity validation demonstrating its potent anticoagulant effects. This study has successfully identified a novel anticoagulant peptide (DLRWM) with confirmed intestinal absorption properties and provides a template for unlocking the pharmaceutical potential of medicinal animal proteins. Full article

Curcumin is widely recognized for its various pharmacological properties, including antioxidant, anti-inflammatory, and anti-tumor activities. Nevertheless, the development of curcumin as a therapeutic agent is impeded by its limited oral bioavailability, which stems from its chemical instability, poor aqueous solubility, and rapid degradation. This study aimed to develop granule formulations incorporating poly(N-isopropylacrylamide)-grafted hyaluronic acid or HA-g-pNIPAM to enhance dissolution and protect curcumin from degradation. Three formulations were developed: F10 (HA-g-pNIPAM physically mixed with curcumin), F10 Encap (curcumin encapsulated within HA-g-pNIPAM), and F11 (curcumin granules without HA-g-pNIPAM). The stability results showed that F10 Encap effectively maintained curcumin content throughout the study period, retaining approximately 94% of its initial concentration by day 30, compared to 70% from F11 (p < 0.05) at 30 °C and 75% relative humidity. All dried curcumin granules exhibited excellent flowability, as determined by the angle of repose measurements. All three formulations exhibited a consistent particle size distribution across replicates, with a peak in the 150–180 μm size range. The sustained release observed for F10 Encap and F10 after the initial burst suggested that the HA-g-pNIPAM provided a controlled release mechanism, ensuring continuous curcumin dissolution over 240 min in gastric and intestinal conditions. These findings suggested that HA-g-pNIPAM improved dissolution and stability of curcumin. Full article

Background/Objectives: Alectinib, a second-generation tyrosine kinase inhibitor indicated for the treatment of non-small-cell lung cancer (NSCLC), exhibits suboptimal oral bioavailability, primarily attributable to its inherently low aqueous solubility and limited dissolution kinetics. This study aimed to enhance Alectinib’s solubility and therapeutic efficacy by formulating a G4-NH2-PAMAM dendrimer complex. Methods: The complex was prepared using the organic solvent evaporation method and characterized by DSC, FTIR, dynamic light scattering (DLS), and zeta potential measurements. A validated high-performance liquid chromatography (HPLC) method quantified the Alectinib. In vitro drug release studies compared free Alectinib with the G4-NH2-PAMAM dendrimer complex. Cytotoxicity against NSCLC cell line A549 was assessed using MTT assays, clonogenic assay, and scratch-wound assay. Xenograft effect was investigated in the H460 lung cell line. Pharmacokinetic parameters were evaluated in rats using LC–MS/MS. Results: Alectinib exhibited an encapsulation efficiency of 59 ± 5%. In vitro release studies demonstrated sustained drug release at pH 6.8 and faster degradation at pH 2.5. Anticancer activity in vitro showed comparable efficacy to free Alectinib, with 98% migration inhibition. In vivo tumor suppression studies revealed near-complete tumor regression (~100%) after 17 days of treatment, compared to 75% with free Alectinib. Pharmacokinetic analysis indicated enhanced absorption (shorter Tmax), prolonged systemic circulation (longer half-life), and higher bioavailability (increased AUC) for the dendrimer-complexed drug. Conclusions: These findings suggest that the G4-NH2-PAMAM dendrimer system significantly improves Alectinib’s pharmacokinetics and therapeutic potential, making it a promising approach for NSCLC treatment. Full article