Diclofenac Research Articles

Diclofenac sodium adsorption in aqueous media by activated carbon obtained from einkorn (Triticum monococcum L.) husk

AbstractThe uncontrolled release of waste diclofenac with low biodegradability is considered to be a potential threat for the environment and creatures. To find effective solution for this issue, this study reports the adsorption performance of diclofenac sodium salt (DCF) by using activated carbon (EHAC) obtained from einkorn (Triticum monococcum L.) husk in aqueous solution under various circumstances. It was found that DCF adsorption on EHAC was highly solution pH dependent, and DCF adsorption by EHAC decreased with increasing adsorption temperature. Equilibrium data showed that fitted isotherm model with the experiment results of DCF adsorption on EHAC followed the order of Langmuir > Temkin > Freundlich > Dubinin-Radushkevich. Adsorption capacity of EHAC for DCF adsorption in aqueous solution was calculated to be 147.06 mg/g at 25 °C. The adsorption kinetic of DCF adsorption on EHAC was determined to obey the pseudo-second-order kinetic model. By utilizing FTIR and pH data obtained from DCF adsorption on EHAC, DCF adsorption mechanisms with some interactions such as π-π stacking, electrostatic interactions, and hydrogen bonding were suggested at diverse pH values. Additionally, intraparticle diffusion model was applied to kinetic results to further recognize the kinetic mechanism of DCF adsorption on EHAC. Furthermore, thermodynamic parameters for DCF adsorption on EHAC were calculated and evaluated, in which DCF adsorption process by EHAC was determined to be exothermic, spontaneous, and feasible.

ECM-mimetic, NSAIDs loaded thermo-responsive, immunomodulatory hydrogel for rheumatoid arthritis treatment

BackgroundRheumatoid arthritis (RA) is a chronic inflammatory autoimmune disease, and it leads to irreversible inflammation in intra-articular joints. Current treatment approaches for RA include non-steroidal anti-inflammatory drugs (NSAIDs), disease-modifying anti-rheumatic drugs (DMARDs), corticosteroids, and biological agents. To overcome the drug-associated toxicity of conventional therapy and transdermal tissue barrier, an injectable NSAID-loaded hydrogel system was developed and explored its efficacy.ResultsThe surface morphology and porosity of the hydrogels indicate that they mimic the natural ECM, which is greatly beneficial for tissue healing. Further, NSAIDs, i.e., diclofenac sodium, were loaded into the hydrogel, and the in vitro drug release pattern was found to be burst release for 24 h and subsequently sustainable release of 50% drug up to 10 days. The DPPH assay revealed that the hydrogels have good radical scavenging activity. The biocompatibility study carried out by MTT assay proved good biocompatibility and anti-inflammatory activity of the hydrogels was carried out by gene expression study in RAW 264.7 cells, which indicate the downregulation of several key inflammatory genes such as COX-2, TNF-α & 18s.ConclusionIn summary, the proposed ECM-mimetic, thermo-sensitive in situ hydrogels may be utilized for intra-articular inflammation modulation and can be beneficial by reducing the frequency of medication and providing optimum lubrication at intra-articular joints.Graphical

Analgesic and Psychotropic Effects of a New Bradykinin Antagonist.

A bradykinin B1 receptors antagonist PAV-0056, an 1,4-benzodiazepin-2-one derivative, intragastrically administrated to mice at doses of 0.1 and 1 mg/kg causes analgesia in the "formalin test" not inferior to that of diclofenac sodium (10 mg/kg) and tramadol (20 mg/kg). PAV-0056 at doses of 0.1 and 10 mg/kg has no anxiolytic and central muscle relaxant effects in mice and does not damage the gastric mucosa in rats. Based on the results of the conditioned place preference test, PAV-0056 also does not induce addiction in mice.

Tramadol/Diclofenac Fixed-Dose Combination for Acute Pain Management: Bioavailability Assessment of a Generic Product.

The multimodal analgesia strategy for acute pain involves using 2 or more analgesic medications with distinct mechanisms of action. This study assessed the bioavailability and tolerability of 2 tramadol hydrochloride (50mg)/diclofenac sodium (50mg) fixed-dose combination formulations under fed conditions to attend the Brazilian regulatory requirements for generic product registration. An open-label, randomized, single-dose, 2-period, 2-way crossover trial was conducted, including healthy subjects of both sexes. Subjects received a single dose of either the test or reference formulation of tramadol/diclofenac fixed-dose combination tablets with a 7-day washout period. Blood samples were collected up to 36hours after dosing for tramadol and 12hours for diclofenac and quantified using a validated liquid chromatography-tandem mass spectrometry method. Of 56 subjects enrolled, 53 completed the study. The 90% confidence intervals for maximum plasma concentration and area under the concentration-time curve from time 0 to the last quantifiable concentration were within acceptable bioequivalence limits of 80%-125%. Considering the results presented in this study, the test formulation is bioequivalent to the reference formulation and could be interchangeable in medical practice.

Fabrication of MXene/chitosan/polyurea nanocomposite decorated on a graphenized substrate for electro-enhanced solid-phase microextraction of diclofenac followed by its determination using differential pulse voltammetry.

A novel solid-phase microextraction fiber based on MXene-chitosan-polyurea (MXene/CS/EPPU) nanocomposite decorated on a graphenized pencil lead fiber (MXene/CS/EPPU/GPLF) was prepared and utilized for electro-enhanced solid-phase microextraction (EE-SPME) of diclofenac (DCF) in biological samples. After extraction and desorption of DCF, it was determined by differential pulse voltammetry (DPV). For this purpose, the working electrode was prepared by deposition of the mentioned MXene/CS/EPPU nanocomposite onto the graphenized pencil lead. The synthesized SPME fiber was characterized using scanning electron microscopy and X-ray diffraction techniques. The effect of various parameters influencing the extraction and the desorption process were investigated, including applied voltage in the extraction and desorption steps, extraction and desorption times, and pH. The developed method exhibited a rather wide linearity in the range 2-1200 ng mL-1 (R2 = 0.985) for the determination of DCF in plasma samples. The limit of detection and the limit of quantification for plasma samples were estimated to be 0.58 and 1.9 ng mL-1 based on the 3Sb/m and 10Sb/m definitions, respectively. The method's accuracy and applicability have been evaluated by the analysis of plasma samples, leading to the relative recoveries in the range 87.0% and 98.0% with the relative standard deviations lower than 3.1%.

Augmented photocatalytic degradation of diclofenac by a novel TiO2-Chitosan-Bocalanine-Ni hybrid material under illumination of various light sources

TiO2-CBA-Ni composite (hydrothermally synthesized TiO2 nanoparticles loaded chitosan-bocalanine nickel complex) was successfully produced using solid and solution approaches, and the finished product was characterized using a variety of instrumentation techniques including UV–Visible, FT-IR, XRD, and SEM. Further, the efficient photocatalytic activity and recombination rates of the prepared TiO2-CBA-Ni composite were evaluated through photoluminescence (PL) spectra compared with pure TiO2. The photocatalytic degradation of diclofenac sodium (DCF) molecules was accomplished utilizing a TiO2-CBA-Ni composite with a pH range of 4.0 to 10.0 and varied light sources. Lower pH levels (pH = 4.0) reveal improved DCF degradation efficiency as compared to higher values (pH = 7.0 and 10.0) under any light source. More importantly, the TiO2-CBA-Ni composite degraded at a greater rate of 94.3 % in an identical reaction time (250 min) than other sources when exposed to visible light and at a lower pH (4.0). This effort has generated interest about the biopolymer grafted ligand metal complex functionalization over the photocatalyst and the effectiveness of the amalgamation, paving the way for a new path to eradicate the toxicity of pharmaceutical items from the ecosystem.

Adsorption of Diclofenac Sodium and Tetracycline From Aqueous Solution Using PVA Films Prepared with Modal/Cotton Fiber Wastes

AbstractIn this study, fiber‐polymer composite films were prepared by adding 0.5 g, 1.0 g, and 1.5 g of modal/cotton (50 : 50) waste to 10 % PVA film, and the properties of the films were revealed by SEM, FTIR analyzes and swelling percentage. It is observed that the strength of the bonds in the FTIR analysis decreases when modal/cotton fibers are added to the PVA film. While a 406 % swelling is achieved in the PVA film, the swelling percentages of the films decrease when modal/cotton fibers are added to the PVA film, and a greater swelling is observed at pH 9 compared to pH 5. The adsorption efficiency of tetracycline and diclofenac sodium on the films was researched at different pH levels and film doses. Tetracycline removal reached its highest value at pH 9, while diclofenac sodium removal reached its highest value at pH 5. Langmuir and Freundlich isotherm models were determined for tetracycline and diclofenac sodium adsorption. Tetracycline removal is better described by the Freundlich isotherm model, whereas diclofenac sodium removal fits the Langmuir isotherm model better. As a result, films prepared with modal/cotton waste not only provide tetracycline and diclofenac sodium removal but also contribute to waste recycling by utilizing waste fiber materials.

A Self-Delivery Nanodrug Simultaneously Inhibits COX-2/PGE2 Mediated Inflammation and Downregulates PD-L1 to Boost Photoimmunotherapy.

Phototherapy promotes anti-tumor immunity by inducing immunogenic cell death (ICD), However, the accompanying inflammatory responses also trigger immunosuppression, attenuating the efficacy of photo-immunotherapy. Herein, they co-assembled a cell-membrane targeting chimeric peptide C16-Cypate-RRKK-PEG8-COOH (CCP) and anti-inflammatory diclofenac (DA) to develop a nanodrug (CCP@DA) that both enhances the immune effect of phototherapy and weakens the inflammation-mediated immunosuppression. CCP@DA achieves cell membrane-targeting photodynamic and photothermal synergistic therapies to damage programmed death ligand 1 (PD-L1) and induce a strong ICD to activate anti-tumor response. Simultaneously, the released DA inhibits the cycoperoxidase-2 (COX-2)/prostaglandin E2 (PGE2) pathway in tumor cells to inhibit pro-tumor inflammation and further down-regulate PD-L1 expression to relieve the immunosuppressive microenvironment. CCP@DA significantly inhibitedtumor growth and inflammation both in vitro and in vivo, while maintaining a potent anti-tumor immune response. Additionally, it exhibits excellent anti-metastatic capabilities and prolongs mouse survival time with a single dose and low levels of near-infrared (NIR) light exposure. This work provides a valuable strategy to control the therapy-induced inflammation for high-efficiency photoimmunotherapy.

Unveiling the potential of machine learning in cost-effective degradation of pharmaceutically active compounds: A stirred photo-reactor study

In this study, neural networks and support vector regression (SVR) were employed to predict the degradation over three pharmaceutically active compounds (PhACs): Ibuprofen (IBP), diclofenac (DCF), and caffeine (CAF) within a stirred reactor featuring a flotation cell with two non-concentric ultraviolet lamps. A total of 438 datapoints were collected from published works and distributed into 70% training and 30% test datasets while cross-validation was utilized to assess the training reliability. The models incorporated 15 input variables concerning reaction kinetics, molecular properties, hydrodynamic information, presence of radiation, and catalytic properties. It was observed that the Support Vector Regression (SVR) presented a poor performance as the ε hyperparameter ignored large error over low concentration levels. Meanwhile, the Artificial Neural Networks (ANN) model was able to provide rough estimations on the expected degradation of the pollutants without requiring information regarding reaction rate constants. The multi-objective optimization analysis suggested a leading role due to ozone kinetic for a rapid degradation of the contaminants and most of the results required intensification with hydrogen peroxide and Fenton process. Although both models were affected by accuracy limitations, this work provided a lightweight model to evaluate different Advanced Oxidation Processes (AOPs) by providing general information regarding the process operational conditions as well as know molecular and catalytic properties.

In-situ construct CuInS2/Bi/Bi2MoO6 S-scheme/Schottky dual heterojunctions catalyst for enhanced photocatalytic degradation of diclofenac sodium

In this paper, the S-scheme/Schottky heterojunction photocatalyst (CuInS2/Bi/Bi2MoO6, CIS/Bi/BMO) was successfully constructed via a facile in-situ solvothermal method, aimed at enhancing its photocatalytic performance. The results of the study on the photocatalytic degradation of diclofenac sodium (DCF) under simulated solar light irradiation revealed that the as-prepared composite exhibited remarkable catalytic efficiency in comparison to the pristine Bi2MoO6 and CuInS2. The plasmonic bismuth (Bi) was formed during the solvothermal process. Subsequently, CuInS2 and Bi were grown on the surface of Bi2MoO6 leading to forming CIS/BMO S-scheme heterojunction, along with a Schottky junction between Bi and Bi2MoO6. The use of ethylene glycol as a support was the main reason for the significant improvement in photocatalytic efficiency in the degradation of DCF. Moreover, the probable photocatalytic mechanisms for the degradation of DCF had been proposed based on the active species quenching experiments. The eleven degradation products were detected by HPLC-MS, and the degradation reaction pathway of DCF was deduced. Additionally, the CIS/Bi/BMO photocatalyst exhibited a consistently high removal rate after four cycles. This study proposes a new strategy for designing efficient S-scheme/Schottky heterojunction photocatalysts for solar energy conversion.

Nanoarchitectonics of an acetogenin-enriched nanosystem mediated by an aqueous extract ofAnnona cherimolaMill with anti-inflammatory and proapoptotic activity against HepG2 cell line.

For the first time, this study shows the nanoarchitectonic process to obtain an acetogenin-enriched nanosystem (AuNPs-Ac) using an aqueous extract from Annona cherimola Mill (ACM) composed of gold nanoparticles embedded in an organic matrix that acts as stabilizing agent and presents anti-inflammatory activity and cytotoxical effect against HepG2 cell line, promoting apoptosis. The synthesis of AuNPs-Ac was confirmed by X-ray diffraction analysis, showing metallic gold as the only phase, and the scanning transmission microscope showed an organic cap covering the AuNPs-Ac. Fourier-transformed infrared suggests that the organic cap comprises a combination of different annonaceous acetogenins, alkaloids, and phenols by the presence of bands corresponding to aromatic rings and hydroxyl groups. High-Performance Liquid Chromatography has demonstrated the presence of annonacin, a potent acetogenin, in the extract of ACM. An in vitro anti-inflammatory activity of the extract of ACM and the AuNPs-Ac was performed using the albumin denaturation method, showing a nonlinear response, which is better than sodium diclofenac salt in a wide range of concentrations that goes from 200 to 400 µg/mL with both samples. The viability assay was studied using trypan blue, treating IMR90 and HepG2 at different concentrations of AuNPs-Ac. The results defined a median lethal dose of 800 µg/mL against HepG2 through apoptosis according to the ratio of caspase-cleaved 9/alpha-tubulin evaluated. It was also demonstrated that the nanosystem presents a higher cytotoxic effect on the HepG2 cell line than in IMR90, suggesting a targeted mechanism. In addition, the nanosystem performs better than using only the extract of ACM in the anti-inflammatory or antiproliferative test, attributed to their higher surface area.

Anti-inflammatory activity of the phenol rich fraction of Garcinia pedunculata Roxb (ex. Buch Ham): an in vitro and in vivo study.

Garcinia pedunculata, a tropical plant found abundantly in the north-east region of India, has been used by many traditional healers for various gastrointestinal ailments. Studies are being carried out for the proper pharmacological identification of the compounds as well as the mode of action for the treatment of various diseases. In this study, phytochemistry of the fruit was evaluated, followed by a quantitative analysis of the total phenolic and flavonoid content of the methanolic crude extract as well as different fractions (n-hexane, chloroform, ethyl acetate, and n-butanol). The fraction with the most potent flavonoid and phenolic content was evaluated for its anti-inflammatory activity using both in vitro and in vivo assays. The chloroform fraction of G. pedunculata fruit extract was found to have a substantial amount of phenols and flavonoids. This fraction inhibited the denaturation of BSA and significantly stabilized human RBC membrane compared to the standard drug Diclofenac sodium. The fraction also significantly reduced the formaldehyde-induced paw edema in mice and normalized the blood parameters. This study provides evidence that G. pedunculata fruit extract plays a critical role in anti-inflammatory activity, indicating that it can be a potential candidate for further investigation in the treatment of inflammation-related diseases.

Oxidative Coupling Assembly Induced Bio-engineered Quercetin Microspheres for the Gastrosparing Delivery of Diclofenac Sodium.

The study aimed to develop microspheres of quercetin by oxidative coupling assembly and these microspheres were used to deliver diclofenac sodium without causing gastrotoxicity. The oxidative coupling assembly of quercetin was carried out in the presence of copper sulfate to yield quercetin microspheres. The microsphere of quercetin was loaded with diclofenac sodium (QP-Diclo). The carrageenan induced paw edema in rats was used for anti-inflammatory action was studied by using and acetic acid-induced writhing in mice was used to study the analgesic potential of the QP loaded microspheres. The ulcerogenecity and gastrotoxicity comparison was made between diclofenac and QP-Diclo. The oxidative coupling assembly of quercetin resulted in microspheres of 10-20 μm in size, which were loaded with diclofenac sodium (QP-Diclo). The marked anti-inflammatory activity was observed by QP-Diclo treatment using carrageenan induced paw edema (in rats) and better analgesic activity than diclofenac sodium in mice. The administration of QP-Diclo significantly elevated the diminished overall nitrite/nitrate extent and thiobarbituric acid reactive and significantly increased the diminished superoxide dismutase activity in comparison to diclofenac sodium in gastric mucosa. The results suggested that dietary polyphenol quercetin can be converted to microspheres by oxidative coupling assembly and can be used to deliver diclofenac sodium without causing gastrotoxicity.

Tuning the wettability of alginate-based nanocomposite beads for efficient removal of pharmaceuticals from water

Long-term exposure to pharmaceuticals, such as diclofenac (DCF) and tetracycline (TC), poses various risks to human health, including antibiotic resistance and endocrine disruption. In this work, we investigated the removal of DCF and TC from water and probed the removal performance of contaminants in a complex matrix consisting of DCF and TC mixtures using alginate (AL)-based nanocomposite beads with tunable wettability. We improved the selectivity of the beads towards hydrophobic contaminants by reducing graphene oxide (GO) to rGO in the presence of AL using a mild and green reducing agent (Vitamin C). Thein-situchemical reduction of GO in AL matrix resulted in amphiphilic rGO-containing beads,as confirmed by several characterization techniques.Thein-situreduction, apart from restoring the sp2hybridized carbon, greatly improved the mechanical properties and stability of the nanocomposite, ensuring reusability beyond 10 adsorption/desorption cycles.Compared to neat AL beads, the addition of only 3.5% rGO (AL:3.5rGO) improved the beads adsorption capacity for TC and DCF by 660% and 747%, respectively. The beads exhibited remarkable performance in the simultaneous removal of TC and DCF from contaminant mixtures. The superior performance of AL:3.5rGO beads is attributed to the enhanced π-π interactions between the aromatic rings of the contaminants and the sp2domains of rGO-containing adsorbents.

Effects of root-derived organic acids on sorption of pharmaceutically active compounds in sandy topsoil

The presence and fate of pharmaceutically active compounds (PhACs) in agricultural fields are rarely investigated. The present study highlights that root-derived low-molecular-weight organic acids (LWMOAs) affect the mobility of PhACs in cultivated humic Arenosol. Sorption experiments are conducted using three PhACs characterised by different physicochemical properties: carbamazepine (CBZ), 17α-ethinylestradiol (EE2), and diclofenac-sodium (DFC). The results suggest that the adsorption of EE2 is more intense than the other two PhACs, whereas DFC and CBZ are primarily dominated by desorption. LMWOAs mainly provide additional low-energy adsorption sites for the PhACs, and slight pH changes do not significantly affect the sorption mechanism. During competitive adsorption, the high-energy sites of the adsorbents are initially occupied by EE2 owing to its high adsorption energy (∼15 kJ/mol). The new low-energy binding sites enhance the adsorption of DFC (from 8.5 % to 72.0 %) and CBZ (from 31 % to 70.0 %) during multicomponent adsorption. LMWOAs not only affect adsorption by modifying the pH but also provide additional binding sites that allow the PhACs to remain in the root environment for a longer period. As the concentration of LMWOAs temporarily changes, so does the availability of PhACs in the root zone. Environmental changes in the humic horizon enhance the mobility of the adsorbed PhACs, which renders them continuously available for uptake by plants, thus increasing the possibility of PhACs entering the human food chain.

Oxygen and phosphorus-enriched mesoporous biowaste-based carbonaceous material: A sustainable solution for efficient removal of diclofenac and chromium (VI) from polluted water

In response to the current environmental crisis, this study focuses on converting biowaste into phosphorus-oxygen-rich activated hydrochar (AH) for removing persistent pollutants such as Diclofenac (DCF) and chromium (VI) (Cr (VI)) from polluted water. The AH was prepared via hydrothermal carbonization of argan nut shells followed by H3PO4 activation under an oxygen-rich atmosphere. The obtained AH was characterized by a high specific surface area of 1879 m2g−1, remarkable mesoporosity, and wide pore diameters. The AH was further analyzed revealing its highly aromatic nature, as well as the abundance of phosphorus and oxygen functional groups on its surface. These properties led to high adsorption capacities of diclofenac and chromium (VI) of 240 mgg−1 and 539 mgg−1, respectively. The investigations indicated that the AH applied physical and chemical forces for removing Cr (VI), while the uptake of DCF molecules was governed by physical forces. Indeed, the high aromaticity and oxygen functionality of AH facilitated the DCF adsorption through hydrogen bonding, π-π interactions, and pore-filling. Meanwhile, the oxygen functionality and the oxygen and phosphorus electron-providing sites on the AH’ surface favor the removal of Cr (VI) ions through physical and chemical interactions, including electrostatic attractions, ion exchange, complexation, and oxidation–reduction reactions. These findings highlight the effectiveness of AH in the elimination of DCF and Cr (VI) from polluted water.

Trace compounds in the urban water cycle in the Freiberg region, Germany

Urban water contamination has become a pressing concern due to the surge in urbanization, industrialization, and population growth, resulting in increased pollution levels and the introduction of emerging contaminants (ECs) into the environment. The widespread use of pharmaceuticals (PhACs), driven by medical advancements and economic progress, has led to their presence in aquatic systems, posing risks to both ecosystems and human health. These compounds are released into the environment via effluent of wastewater treatment plants (WWTPs) as they are inefficient in totally removing PhACs. This study focused on PhACs in wastewater, surface water and groundwater of a small city like Freiberg region in Germany. Samples were collected along Münzbach’s path, encompassing hospital discharges and WWTP. Analysis for the measurement of PhACs was conducted via Ultra-high-performance liquid chromatography coupled with tandem mass spectrometry (UHPLC–MS/MS). Results revealed that about 46 out of 54 analyzed PhACs were detected across matrices, with positive findings of 46 substances in wastewater, 37 in surface water, and 19 in groundwater. Among 54 analyzed PhACs, six of the active pharmaceutical ingredients (APIs) like atenolol (ATL), carbamazepine (CBZ), caffeine (CAF), diclofenac (DCF), metformin (MET), and sulfamethoxazole (SMX) were focused in this study. Five of the six APIs were present in all matrices, with MET and CAF widely distributed in an aqueous system. CBZ and DCF were found in wastewater and surface water, ATL was scarce in surface water, while SMX was absent in groundwater. It was observed that PhAC concentration was reduced from wastewater to groundwater, with the highest levels near the WWTP, decreasing as effluents flowed through surface water Münzbach and Freiberger Mulde. It was also observed that the groundwater near the surface water shows the presence of APIs mainly due to the hyporheic zone connecting the surface water and groundwater. Overall, PhAC compounds reflect the city population and their age, the water cycle, and the hydrochemical processes of the compounds themselves.

Investigation on antioxidant, antimicrobial, anti-inflammatory, and neuropsychiatry potential of phyto-mediated ZnONPs using Colebrookea oppositifolia

The present study reports the phyto-mediated synthesis of ZnONPs using methanol extracts and n-Butanol fractions from the roots and leaves of C. oppositifolia. The synthesized nanoparticles were characterized using XRD, FE-SEM, HR-TEM, and XPS techniques to determine their crystallite structure, elemental composition, surface topography, and physio-chemical properties. Furthermore, the biological potential of ZnONPs was evaluated for antioxidant, antimicrobial, anti-inflammatory, and in vitro cytotoxic potential on SH-SY5Y neuroblastoma cell lines. Notably, LEME-ZnONPs exhibited exceptional antioxidant activity with an IC50 of 30.200μg/mL in the DPPH assay. The antimicrobial efficacy was also remarkable, displaying high maximum activity against bacterial strains, evidenced by zones of inhibition (ZOI) measuring 15.67±0.58mm (E. coli) and 14.67±0.58mm (S. aureus) for RTME-ZnONPs, attributable to their small crystallite size. Similarly, against antifungal strains, LEBF-ZnONPs (60.94±0.83%) and RTBF-ZnONPs (60.85±0.74%) exhibited potency to inhibit both F. oxysporum and R. necatrix due to their small particle size. Furthermore, LEBF-ZnONPs demonstrated superior anti-inflammatory properties, registering an impressive 98.681%, outperforming Diclofenac sodium (96.835%). Importantly, the phyto-mediated ZnONPs exhibited minimal cytotoxicity on SH-SY5Y cell lines at 62.5μg/mL, a concentration employed as an experimental model to assess neuronal function. The multifaceted applications of phyto-mediated ZnONPs extend across various fields, including pharmaceutical sciences, agriculture, and the treatment of neurological diseases.

Acute heat trauma model in rats, gender-dependent thermoresistance, and screening of potential thermoprotectors

Heat trauma (HT) is an urgent medical and social problem. Heat damage is a widespread effect of the environment on humans, driven by global warming, military conflicts, technological disasters, work in hot environments, and engagement in extreme sports and tourism. The aim of the study: to propose a model of acute HT in rats that does not cause the death of animals, to determine the dependence of thermoresistance on gender, and to compare the effectiveness of the thermoprotective effects of a range of non-steroidal anti-inflammatory drugs (NSAIDs), paracetamol, and glucosamine hydrochloride in this model. Materials and Methods: The experiment was conducted on adult white rats of both genders. Acute HT was modelled by using a specially developed method involving heat exposure to animals at +55 °C for 30 minutes, followed by a recovery period of 60 minutes. Rectal temperature was measured every 15 minutes. The degree of hyperthermia in males and females was determined. The presence and intensity of the thermoprotective effect of glucosamine hydrochloride (G h/ch), diclofenac sodium, acetylsalicylic acid (ASA), nimesulide, etoricoxib, celecoxib, and paracetamol were evaluated through intragastric administration 60 minutes before heat exposure. The results were analyzed using the STATISTICA 12.0 program. Results: It was established that heat exposure at +55 °C for 30 minutes effectively replicates acute HT in rats without causing animal fatalities, adhering to bioethical requirements. Body temperature increases by 10-13 %, characterized as a heat stroke. Occasionally, thermoresistant animals are encountered, where the temperature increase during the first 15 minutes of exposure is less than 1 °C. These animals should not be used for further modelling of heat trauma. Male rats are more sensitive to the effect of high environmental temperatures than females, exhibiting greater hyperthermia (temperature increase of 5.03±0.39°C compared to 3.72±0.22 °C in females, p<0.01). The thermoprotective effect of glucosamine hydrochloride depends on gender, being more pronounced in males. Among the 6 tested COX inhibitors, the most significant thermoprotective effect was observed in the highly selective COX-2 inhibitor celecoxib and the weakly selective central inhibitor paracetamol, warranting in-depth research into their impact on organ and system states following heat trauma, as well as the mechanisms of their thermoprotective action. The thermoprotective effect is not associated with selectivity towards COX (cyclooxygenase): it is not observed in the highly selective COX-2 inhibitor etoricoxib and moderately selective COX-2 inhibitor nimesulide, as well as in non-selective COX inhibitors such as diclofenac sodium and aspirin, which also slows down the recovery of body temperature after heat exposure. Conclusions: A convenient and simple model of acute HT in rats is proposed, demonstrating higher thermosensitivity and a more pronounced thermoprotective effect of glucosamine hydrochloride in males. A significant thermoprotective effect was identified in celecoxib and paracetamol, surpassing other investigated NSAIDs. The mechanism and specific features of this effect require further clarification

Single and binary adsorption of paracetamol and diclofenac onto biochar produced from pepper stem: Which adsorption properties change in the binary system?

The importance of combating the contamination of water resources with emerging pollutants must be kept all the more in view by scientists, since such pollutants are harmful and pose challenges for traditional water treatment methods. The current study was designed to scrutinize the adsorption properties of a low-cost biochar for two pharmaceuticals in both single and binary systems. The work was focused on understanding how paracetamol (PARA) and diclofenac (DIC) co-adsorb, and it can serve as a beacon for similar studies, especially in modeling the adsorption processes of such systems. Using a low-cost biochar from pepper stem (PS) with a high surface area = 727.5 m2/g as adsorbent, experiments were carried out in both the single and binary systems to investigate the adsorption behavior of the mentioned pharmaceuticals. Results showed that, in the single system, the PS biochar demonstrates a slightly greater adsorption capability for both PARA and DIC, with a capacity of 354.66 and 256.10 mg/g, respectively, compared to its capacity for each pharmaceutical in the presence of the other in the solution. Interestingly, the effect of the presence of one of the pharmaceuticals on the thermodynamic parameters (ΔGº, ΔSº, and ΔHº) of the other was ignorable, and interactions such as hydrogen bonding, π-π, n-π, and anion-π interactions were at work for the adsorption processes, with different extends in each pharmaceutical-biochar case. On the other hand, the presence of one of the pharmaceuticals was effective on the kinetics of the adsorption process of the other and caused a decrease in its adsorption rate, especially in the initial stage of the process. Overall, in addition to the suitability of pepper stem biochar for PARA and DIC, results showed that the presence of one pharmaceutical is not influential on all the adsorption properties of the other, and the results can be exploited for studding similar systems.