Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 20 de 743
Filter
1.
An Acad Bras Cienc ; 96(suppl 1): e20231110, 2024.
Article in English | MEDLINE | ID: mdl-39046057

ABSTRACT

The present study modeled the adsorption process of the drug diclofenac sodium on activated charcoal. For this purpose, a mass balance-based model was used considering a fixed bed column. The mass transfer rate in the solid phase was represented by a driving force model proposed in this study, and a gamma exponent with a range of 0 > γ ≤ 2 was assigned to the model. Different isotherms were adopted to represent the equilibrium at the solid/liquid interface: the Langmuir, Freundlich, Sips and Redlich-Peterson isotherms. The modeling was approached from the perspective of Bayesian statistics, and the Markov chain Monte Carlo method was used for parameter estimation. Model validation was performed with experimental data obtained under different operating conditions of initial concentration ($C_{0.


Subject(s)
Bayes Theorem , Charcoal , Diclofenac , Diclofenac/chemistry , Adsorption , Charcoal/chemistry , Monte Carlo Method , Models, Chemical
2.
Environ Sci Pollut Res Int ; 31(35): 48650-48662, 2024 Jul.
Article in English | MEDLINE | ID: mdl-39037628

ABSTRACT

The presence of pharmaceuticals in wastewater resulting from human activities has driven researchers to explore effective treatment methods such as adsorption using activated carbon (AC). While AC shows promise as an adsorbent, further studies are essential to comprehend its entire interaction with pharmaceuticals. This article investigates the adsorption of potassium diclofenac (PD) onto AC using experimental and modeling approaches. Batch adsorption studies coupled with Fourier transform infrared spectroscopy (FTIR) were employed to clarify the adsorption mechanism of PD on AC. Various kinetic and isotherm adsorption models were applied to analyze the adsorbent-adsorbate interaction. The kinetics were best described by Avrami's fractional order (AFO) nonlinear model. Also, the intraparticle diffusion (IP) model reveals a three-stage adsorption process. The experimental equilibrium data fitted well with the three-parameter nonlinear Liu model, indicating a maximum adsorption capacity (Qmax) of 88.45 mg g-1 and suggesting monolayer or multilayer adsorption. Thermodynamic analysis showed favorable adsorption (ΔG° < 0), with an enthalpy change (ΔH° = -30.85 kJ mol-1) characteristic of physisorption involving hydrogen bonds and π-π interactions. The adsorption mechanism was attributed to forming a double layer (adsorbate-adsorbent and adsorbate-adsorbate).


Subject(s)
Charcoal , Diclofenac , Water Pollutants, Chemical , Diclofenac/chemistry , Adsorption , Charcoal/chemistry , Water Pollutants, Chemical/chemistry , Kinetics , Thermodynamics , Spectroscopy, Fourier Transform Infrared , Wastewater/chemistry , Carbon/chemistry
3.
Clin Pharmacol Drug Dev ; 13(8): 907-914, 2024 Aug.
Article in English | MEDLINE | ID: mdl-38716761

ABSTRACT

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 (50 mg)/diclofenac sodium (50 mg) 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 36 hours after dosing for tramadol and 12 hours 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.


Subject(s)
Acute Pain , Analgesics, Opioid , Area Under Curve , Biological Availability , Cross-Over Studies , Diclofenac , Drug Combinations , Drugs, Generic , Therapeutic Equivalency , Tramadol , Humans , Male , Tramadol/pharmacokinetics , Tramadol/administration & dosage , Diclofenac/pharmacokinetics , Diclofenac/administration & dosage , Female , Adult , Drugs, Generic/pharmacokinetics , Drugs, Generic/administration & dosage , Drugs, Generic/adverse effects , Young Adult , Acute Pain/drug therapy , Analgesics, Opioid/pharmacokinetics , Analgesics, Opioid/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Middle Aged , Brazil , Pain Management/methods , Healthy Volunteers , Tandem Mass Spectrometry
4.
J Appl Oral Sci ; 32: e20240017, 2024.
Article in English | MEDLINE | ID: mdl-38775598

ABSTRACT

OBJECTIVE: To compare the effect of submucosal cryotherapy using cold saline to dexamethasone sodium phosphate and diclofenac sodium injections on substance P and interleukin 6 release in experimentally induced pulpal inflammation in rabbits' molar teeth. METHODOLOGY: Fifteen rabbits were randomly classified into 3 groups according to the submucosal injection given: cold saline, dexamethasone sodium phosphate, and diclofenac sodium. A split-mouth design was adopted, the right mandibular molars were experimental, and the left molars served as the control without injections. Intentional pulp exposures were created and left for 6 hours to induce pulpitis. Pulpal tissue was extracted and examined for SP and IL-6 levels using ELISA. Within each group, the level of cytokines released was measured for both control and experimental groups for intragroup comparison to determine the effect of injection. The percentage reduction of each mediator was calculated compared with the control side for intergroup comparison then the correlation between SP and IL-6 levels was analyzed using Spearman's rank order correlation coefficient. Statistical analysis was performed, and the significance level was set at p<0.05. RESULTS: Submucosal cryotherapy, dexamethasone sodium phosphate, and diclofenac sodium significantly reduced SP and IL-6 pulpal release. Submucosal cryotherapy significantly reduced SP more than and IL-6 more than dexamethasone sodium phosphate and diclofenac sodium. Pulpal reduction of SP and IL-6 showed a strong positive significant correlation. CONCLUSIONS: Submucosal cryotherapy reduces the pulpal release of SP and IL-6 and could be tested as an alternative to premedication to potentiate the effect of anesthesia and control postoperative endodontic pain.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal , Cryotherapy , Dental Pulp , Dexamethasone , Diclofenac , Enzyme-Linked Immunosorbent Assay , Interleukin-6 , Pulpitis , Random Allocation , Substance P , Animals , Rabbits , Pulpitis/therapy , Diclofenac/pharmacology , Dexamethasone/pharmacology , Dexamethasone/analogs & derivatives , Interleukin-6/analysis , Cryotherapy/methods , Substance P/analysis , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Dental Pulp/drug effects , Time Factors , Reproducibility of Results , Treatment Outcome , Male , Statistics, Nonparametric , Disease Models, Animal , Anti-Inflammatory Agents/pharmacology , Saline Solution , Reference Values
5.
Chemosphere ; 358: 142222, 2024 Jun.
Article in English | MEDLINE | ID: mdl-38714249

ABSTRACT

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.


Subject(s)
Diclofenac , Hydrogen Peroxide , Ibuprofen , Machine Learning , Neural Networks, Computer , Diclofenac/chemistry , Hydrogen Peroxide/chemistry , Ibuprofen/chemistry , Kinetics , Water Pollutants, Chemical/chemistry , Water Pollutants, Chemical/analysis , Caffeine/chemistry , Oxidation-Reduction , Pharmaceutical Preparations/chemistry , Pharmaceutical Preparations/analysis , Ozone/chemistry , Support Vector Machine , Cost-Benefit Analysis , Ultraviolet Rays , Catalysis , Photolysis
6.
J Control Release ; 370: 392-404, 2024 Jun.
Article in English | MEDLINE | ID: mdl-38663750

ABSTRACT

The toxicity for the human body of non-steroidal anti-inflammatory drugs (NSAIDs) overdoses is a consequence of their low water solubility, high doses, and facile accessibility to the population. New drug delivery systems (DDS) are necessary to overcome the bioavailability and toxicity related to NSAIDs. In this context, UiO-66(Zr) metal-organic framework (MOF) shows high porosity, stability, and load capacity, thus being a promising DDS. However, the adsorption and release capability for different NSAIDs is scarcely described. In this work, the biocompatible UiO-66(Zr) MOF was used to study the adsorption and release conditions of ibuprofen, naproxen, and diclofenac using a theoretical and experimental approximation. DFT results showed that the MOF-drug interaction was due to an intermolecular hydrogen bond between protons of the groups in the defect sites, (µ3 - OH, and - OH2) and a lone pair of oxygen carboxyl functional group of the NSAIDs. Also, the experimental results suggest that the solvent where the drug is dissolved affects the adsorption process. The adsorption kinetics are similar between the drugs, but the maximum load capacity differs for each drug. The release kinetics assay showed a solvent dependence kinetics whose maximum liberation capacity is affected by the interaction between the drug and the material. Finally, the biological assays show that none of the systems studied are cytotoxic for HMVEC. Additionally, the wound healing assay suggests that the UiO-66(Zr) material has potential application on the wound healing process. However, further studies should be done.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal , Drug Delivery Systems , Drug Liberation , Metal-Organic Frameworks , Naproxen , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Metal-Organic Frameworks/chemistry , Naproxen/administration & dosage , Naproxen/chemistry , Naproxen/pharmacokinetics , Ibuprofen/administration & dosage , Ibuprofen/chemistry , Ibuprofen/pharmacokinetics , Humans , Adsorption , Drug Carriers/chemistry , Diclofenac/administration & dosage , Diclofenac/chemistry , Diclofenac/pharmacokinetics , Cell Survival/drug effects , Phthalic Acids
7.
J Sci Food Agric ; 104(10): 5964-5972, 2024 Aug 15.
Article in English | MEDLINE | ID: mdl-38437521

ABSTRACT

BACKGROUND: Seafood consumers are widely exposed to diclofenac due to the high contamination levels often present in aquatic organisms. It is a potential risk to public health due its endocrine disruptor properties. Limited information is available about diclofenac behavior after food digestion to enable a more realistic scenario of consumer exposure. This study aimed to evaluate cooking effects on diclofenac levels, and determine diclofenac bioaccessibility by an in vitro digestion assay, using commercial fish species (seabass and white mullet) as models. The production of the main metabolite 4'-hydroxydiclofenac was also investigated. Fish hamburgers were spiked at two levels (150 and 1000 ng g-1) and submitted to three culinary treatments (roasting, steaming and grilling). RESULTS: The loss of water seems to increase the diclofenac levels after cooking, except in seabass with higher levels. The high bioaccessibility of diclofenac (59.1-98.3%) observed in both fish species indicates that consumers' intestines are more susceptible to absorption, which can be worrisome depending on the level of contamination. Contamination levels did not affect the diclofenac bioaccessibility in both species. Seabass, the fattest species, exhibited a higher bioaccessibility of diclofenac compared to white mullet. Overall, cooking decreased diclofenac bioaccessibility by up to 40% in seabass and 25% in white mullet. The main metabolite 4'-hydroxydiclofenac was not detected after cooking or digestion. CONCLUSION: Thus, consumption of cooked fish, preferentially grilled seabass and steamed or baked white mullet are more advisable. This study highlights the importance to consider bioaccessibility and cooking in hazard characterization studies. © 2024 The Authors. Journal of The Science of Food and Agriculture published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.


Subject(s)
Cooking , Diclofenac , Digestion , Food Contamination , Seafood , Diclofenac/metabolism , Diclofenac/chemistry , Animals , Food Contamination/analysis , Seafood/analysis , Fishes/metabolism , Bass/metabolism , Humans , Water Pollutants, Chemical/metabolism , Water Pollutants, Chemical/chemistry , Smegmamorpha/metabolism , Models, Biological
8.
Drug Res (Stuttg) ; 74(4): 171-179, 2024 Apr.
Article in English | MEDLINE | ID: mdl-38503307

ABSTRACT

BACKGROUND: Diclofenac is the non-steroidal anti-inflammatory drug (NSAID) mostly prescribed worldwide, but it is highly associated with hypertension and acute kidney injury. Despite that, little information is available about the renal effects of diclofenac in hypertensive individuals, which led us to carry out this comparative study between the renal effects of this NSAID in normotensive (NTR) and spontaneously hypertensive rats (SHR). METHODS: Male Wistar NTR and SHR were orally treated with vehicle (V: 10 mL/kg) or diclofenac sodium (D: 100 mg/kg) once a day for 3 days. Urine volume, electrolytes excretion (Na+, K+, Cl-, and Ca2+), urea, creatinine, pH, and osmolarity were evaluated. Furthermore, blood samples and renal tissue were collected to perform biochemical and histological analysis. RESULTS: Diclofenac increased the renal corpuscle and bowman's space in the SHR, while no microscopic changes were observed in the renal tissue of NTR. Regarding the urinary parameters, diclofenac reduced urine volume, pH, osmolarity, and all electrolytes excretion, followed by decreased urea and creatinine levels in both lineages. Moreover, it also induced hyponatremia, hypokalemia, and hypocalcemia in SHR, while reduced glutathione-S-transferase activity, lipid hydroperoxides, and nitrite levels in renal tissue. CONCLUSIONS: The data presented herein demonstrated that diclofenac induces renal damage and impaired renal function in both NTR and SHR, but those effects are exacerbated in SHR, as seen by the histological changes and electrolytes balance disturbance, therefore, reinforcing that diclofenac may increase the risks of cardiovascular events in hypertensive patients.


Subject(s)
Diclofenac , Hypertension , Humans , Rats , Male , Animals , Diclofenac/toxicity , Creatinine , Rats, Wistar , Hypertension/chemically induced , Hypertension/drug therapy , Kidney , Blood Pressure , Rats, Inbred SHR , Anti-Inflammatory Agents, Non-Steroidal/toxicity , Electrolytes , Urea
9.
Environ Res ; 251(Pt 2): 118733, 2024 Jun 15.
Article in English | MEDLINE | ID: mdl-38521353

ABSTRACT

The presence of emerging contaminants in wastewater poses a global environmental challenge, requiring the development of innovative materials or methods for their treatment. This study focused on the production of green functionalized carbon nanotubes (CNTs) and using them in the adsorption of the pharmaceuticals Losartan (LOS) and Diclofenac (DIC). The efficiency of the methodology was verified by characterization techniques. Elemental composition analysis indicated a significant increase in the iron content after the green functionalization, proving the effectiveness of the method. Thermogravimetric analysis showed similar thermal degradation profiles for pristine CNTs and functionalized CNTs, indicating better post-functionalization thermal stability. BET analysis revealed mesoporous characteristics of CNTs, with increased surface area and pore volumes after functionalization. X-Ray diffraction confirmed the preservation of the lattice structure of the CNTs post-functionalization and post-adsorption, with changes in peak broadening suggesting surface modifications. LOS and DIC adsorption were evaluated via kinetic studies at four different concentrations (0.1-0.4 mmol/L) that were best represented by the pseudo-second order model, suggesting chemisorption mechanisms, with faster and higher uptakes for DIC (0.084-0.261 mmol/g; teq = 5 min) when compared to LOS (0.058-0.235 mmol/g; teq = 20 min). The curves were also studied via artificial neural networks (ANN) and revealed that the best ANN architecture for representing the experimental data is a network with [3 5 5 2] neurons trained using the Bayesian-Regularization algorithm and the Log-sigmoid (hidden layers) and Linear (output layer) transfer functions. The desorption study showed that CaCl2 had better performance in CNT regeneration, reaching its removal capacity above 50% up to 3 cycles, for both pharmaceuticals. These findings reveal the potential of the developed material as a promising adsorbent for targeted removal of pollutants, contributing to advances in the remediation of emerging contaminants and the application of artificial intelligence in adsorption research.


Subject(s)
Diclofenac , Iron , Losartan , Nanotubes, Carbon , Water Pollutants, Chemical , Diclofenac/chemistry , Nanotubes, Carbon/chemistry , Adsorption , Losartan/chemistry , Kinetics , Water Pollutants, Chemical/chemistry , Iron/chemistry , Green Chemistry Technology/methods , Neural Networks, Computer , Coffee/chemistry , Biomass , Metal Nanoparticles/chemistry
10.
Int Endod J ; 57(5): 520-532, 2024 May.
Article in English | MEDLINE | ID: mdl-38279778

ABSTRACT

AIM: The anaesthetic success rate of an inferior alveolar nerve block (IANB) in mandibular molars with irreversible symptomatic pulpitis can be low, and postoperative pain control in teeth with this diagnosis can be challenging. This study aimed to evaluate the influence of preemptive use of dexamethasone and oral potassium diclofenac on the success of IANB. The influence of these drugs on the intensity of postoperative pain was assessed as a secondary outcome. METHODOLOGY: Eighty-four patients with mandibular molars diagnosed with irreversible symptomatic pulpitis recorded preoperative pain intensity using a cold thermal test and a modified Numerical Rating Scale (mNRS). Sixty minutes before the anaesthetic procedure, patients were randomly assigned to one of three groups based on the medication they received: dexamethasone (4 mg), diclofenac potassium (50 mg), or placebo. All patients received IANB with 4% articaine (1:200 000 epinephrine), and 15 min later, they were evaluated for pain intensity using the cold thermal test. Anaesthetic success was analysed. The pain intensity was then recorded, and endodontic treatment and provisional restoration of the tooth were executed in a single session. Patients were monitored for 6, 12, 24, 48 and 72 h using the mNRS to assess the intensity of postoperative pain. RESULTS: There was a statistically significant increase in anaesthetic success when 4 mg dexamethasone (39.3%) or 50 mg diclofenac potassium (21.4%) was used compared to the placebo group (3.6%) (p < .001), with no significant difference between the two drugs. Regarding postoperative pain, dexamethasone was superior to placebo at 6 h (p < .001), with diclofenac having an intermediate behaviour, not differing between dexamethasone and placebo (p > .05). There was no significant difference amongst the groups at 12 h (p > .05). At 24, 48 and 72 h, the effectiveness of dexamethasone and diclofenac were comparable, and both were superior to placebo (p < .001). CONCLUSION: The use of dexamethasone or diclofenac potassium was favourable in terms of increasing the success rate of inferior alveolar nerve block in cases of mandibular molars with irreversible symptomatic pulpitis and decreased the occurrence of postoperative pain when compared to the use of a placebo.


Subject(s)
Anesthesia, Dental , Anesthetics , Nerve Block , Pulpitis , Humans , Anesthesia, Dental/methods , Anesthetics/pharmacology , Anesthetics, Local , Anti-Inflammatory Agents/pharmacology , Dexamethasone/pharmacology , Diclofenac/pharmacology , Double-Blind Method , Lidocaine , Mandibular Nerve , Molar/surgery , Nerve Block/methods , Pain, Postoperative/drug therapy , Pain, Postoperative/prevention & control , Pulpitis/surgery
12.
Rev. cuba. med. mil ; 52(4)dic. 2023. tab
Article in Spanish | LILACS, CUMED | ID: biblio-1559857

ABSTRACT

Introducción: El uso de fármacos con potencial cardiotóxico para tratar enfermedades no cardiovasculares coexistentes resulta un agravante evitable. Objetivo: Evaluar la prescripción de 5 fármacos cardiotóxicos en pacientes con enfermedades cardiovasculares. Métodos: Se realizó un estudio descriptivo transversal (enmarcado en los estudios de utilización de medicamentos) de marzo a diciembre de 2020 en el Policlínico Santa Cruz (Artemisa, Cuba), en una población de 234 sujetos con enfermedades cardiovasculares que habían sido tratados con domperidona, azitromicina, ciprofloxacina, ibuprofeno y diclofenaco. Las variables estudiadas fueron: sexo, edad, consumo de fármacos cardiotóxicos, motivo de indicación, enfermedades cardiovasculares, forma farmacéutica, dosis diaria, intervalo de las dosis y duración del tratamiento. Se realizó un análisis estadístico descriptivo. Resultados: Los fármacos más prescritos fueron la azitromicina (n= 63), el ibuprofeno (n= 59) y la ciprofloxacina (n= 57). Sus principales motivos de indicación fueron, respectivamente, la neumonía adquirida en la comunidad (38,1 por ciento), las infecciones de piel y tejidos blandos (28,8 por ciento), y las infecciones del tracto urinario (43,8 por ciento). La principal enfermedad cardiovascular fue la hipertensión arterial. Para los 5 fármacos seleccionados se reportó su esquema terapéutico (forma farmacéutica, dosis diaria, intervalo de dosis y duración del tratamiento). Conclusiones: Aunque en todos los casos el motivo de indicación es el adecuado, los fármacos pueden sustituirse por otros de menor riesgo cardiovascular. En su mayoría, los esquemas terapéuticos son correctos, salvo en los casos de la domperidona (duración prolongada) y el diclofenaco (altas dosis)(AU)


Introduction: The use of drugs with cardiotoxic potential to treat coexisting noncardiovascular diseases results in avoidable aggravation. Objective: To assess the prescription of 5 cardiotoxic drugs in patients with cardiovascular disease. Methods: A cross-sectional descriptive study (framed in the studies of drug utilization) was carried out from March to December 2020 in the Policlínico Santa Cruz (Artemisa, Cuba), in a population of 234 subjects with cardiovascular diseases who had been treated with domperidone, azithromycin, ciprofloxacin, ibuprofen and diclofenac. The variables studied were: sex, age, consumption of cardiotoxic drugs, reason for indication, cardiovascular disease, pharmaceutical form, daily dose, dose interval, and duration of treatment. Descriptive statistical analysis was performed. Results: The most prescribed drugs were azithromycin (n= 63), ibuprofen (n= 59) and ciprofloxacin (n= 57). Their main reasons for indication were, respectively, community-acquired pneumonia (38.1 percent), skin and soft tissue infections (28.8 percent), and urinary tract infections (43.8 percent). The main cardiovascular disease was arterial hypertension. For the 5 selected drugs, their therapeutic scheme (pharmaceutical form, daily dose, dose interval and duration of treatment) was reported. Conclusions: Although in all cases the reason for indication was adequate, the drugs can be substituted by others of lower cardiovascular risk. For the most part, the therapeutic regimens are correct, except in the cases of domperidone (prolonged duration) and diclofenac (high doses)(AU)


Subject(s)
Humans , Drug Prescriptions , Cardiovascular Diseases/drug therapy , Cardiotoxins/toxicity , Pharmacovigilance , Ciprofloxacin/therapeutic use , Diclofenac/therapeutic use , Ibuprofen/therapeutic use , Epidemiology, Descriptive , Cross-Sectional Studies , Azithromycin/therapeutic use , Domperidone/therapeutic use
13.
Environ Pollut ; 338: 122628, 2023 Dec 01.
Article in English | MEDLINE | ID: mdl-37783413

ABSTRACT

Pharmaceuticals and endocrine disrupting compounds are organic micropollutants that can cause adverse effects at low concentrations. Their occurrence in surface waters has been reported in several countries, including Brazil, at concentrations on the order of ngL-1, while the concentrations at which toxic effects are observed are often in the range of mg.L-1 to µg.L -1, however few studies have been undertaken to characterize risks they represent in Brazilian surface waters. Thus, the objective of this study was to evaluate the ecological risk to Brazilian surface waters caused by the presence of pharmaceuticals and natural and environmental estrogens. Twenty-nine pharmaceuticals, hormones and environmental estrogens were included in the risk assessment while twelve were discarded due to insufficient data availability. The endocrine disrupting compounds were the most frequently detected (39.8% of the reported concentrations), followed by non-steroidal anti-inflammatory drugs (16.3%), antibiotics (6.6%), antiseptics (5.1%), analgesics (5.1%), antihypertensives (4.6%), and to a lesser extent, lipid controllers, anticonvulsants, antidepressants, antihistamines, antivirals and corticosteroids. Bisphenol-A was the most frequently detected compound, followed by diclofenac, 17-ß-estradiol, 17-α-ethynilestradiol, naproxen, triclosan and 4-n-nonylphenol. Acute ecological risk was predicted in two thirds and chronic risk in one third of the water bodies surveyed. The presence of diclofenac or triclosan was determinant for acute risk while estrogenic hormones proved to be decisive for chronic risk. In addition to natural and synthetic endocrine disruptors, the pharmacological groups estimated to have the highest average associated risks were non-steroidal anti-inflammatory drugs, followed by anticonvulsants. No discharge limits exist for most of the compounds found to contribute to ecological risks, indicating the need for regulatory action by the proper Brazilian authorities.


Subject(s)
Endocrine Disruptors , Triclosan , Water Pollutants, Chemical , Endocrine Disruptors/analysis , Brazil , Diclofenac , Anticonvulsants , Water Pollutants, Chemical/analysis , Estrogens/analysis , Estradiol/analysis , Anti-Inflammatory Agents, Non-Steroidal , Risk Assessment , Pharmaceutical Preparations , Environmental Monitoring
14.
Environ Sci Pollut Res Int ; 30(46): 102641-102652, 2023 Oct.
Article in English | MEDLINE | ID: mdl-37668780

ABSTRACT

This study was intended to valorize a floated sludge of a poultry slaughterhouse using it as a precursor to producing char and activated carbon, which were tested as adsorbents in removing ketoprofen and diclofenac sodium from the water. The addition of zinc chloride or calcium hydroxide was determinant for forming a porous carbonaceous structure with a high surface area in AC-FSP (656.54 m2 g-1), differently from that exhibited by the CHAR-FSP (8.11 m2 g-1). Kinetic and equilibrium studies indicated that the pseudo-second-order and the Sips models were suitable. The AC- FSP maximum adsorption capacity for ketoprofen and diclofenac sodium was 124.98 mg g-1 and 138.32 mg g-1, respectively. The adsorption was a spontaneous and endothermic process. It was concluded that AC-FSP is a more efficient and promising adsorbent than CHAR-FSP for the adsorption of drugs in contaminated wastewater. In addition, AC-FSP can be reused, maintaining good adsorption levels for about 5 cycles. Therefore, this study is aligned with the 2030 Agenda for global sustainability since converting waste (valueless) into an adsorbent is also directly linked to the circular economy and neutral carbon.


Subject(s)
Ketoprofen , Water Pollutants, Chemical , Animals , Sewage , Diclofenac , Charcoal/chemistry , Adsorption , Poultry , Water Pollutants, Chemical/analysis , Kinetics , Pharmaceutical Preparations , Hydrogen-Ion Concentration
15.
Molecules ; 28(13)2023 Jul 05.
Article in English | MEDLINE | ID: mdl-37446881

ABSTRACT

Diclofenac is the most prescribed nonsteroidal anti-inflammatory drug worldwide and is used to relieve pain and inflammation in inflammatory arthritis. Diclofenac is associated with serious adverse effects, even in regular-dose regimens. Drug delivery systems can overcome this issue by reducing adverse effects and optimizing their efficacy. This study evaluated the activity of lipid-core nanocapsules loaded with diclofenac (DIC-LNCs) in an experimental model of adjuvant-induced arthritis. The diclofenac nanoformulation was obtained via self-assembly. A stereological analysis approach was applied for the morphological quantification of the volume, density, and cellular profile count of the metatarsophalangeal joints of rats. Proinflammatory cytokines and biochemical profiles were also obtained. Our results showed that the diclofenac nanocapsule DIC-LNCs were able to reduce arthritis compared with the control group and the DIC group. DIC-LNCs efficiently reduced proinflammatory cytokines, C-reactive protein, and xanthine oxidase levels. Additionally, DIC-LNCs reduced the loss of synoviocytes and chondrocytes compared with the DIC (p < 0.05) and control groups (p < 0.05). These data suggest that DIC-LNCs have anti-arthritic activity and preserve joint components, making them promising for clinical use.


Subject(s)
Arthritis, Experimental , Nanocapsules , Rats , Animals , Diclofenac/pharmacology , Diclofenac/therapeutic use , Arthritis, Experimental/drug therapy , Lipids/therapeutic use , Cytokines
17.
Bull Environ Contam Toxicol ; 110(6): 106, 2023 Jun 07.
Article in English | MEDLINE | ID: mdl-37284985

ABSTRACT

In this study we evaluated the acute (immobility/mortality) and chronic (survival and reproduction) effects of the drugs caffeine, diclofenac sodium salt, ketoprofen, paracetamol and salicylic acid on the cladoceran Ceriodaphnia silvestrii. The environmental risks of these substances for tropical freshwaters were estimated from the risk quotient MEC/PNEC. Sensitivity in acute exposures varied up on the drug as follows: salicylic acid (EC50 = 69.15 mg L- 1) < caffeine (EC50 = 45.94 mg L- 1) < paracetamol (EC50 = 34.49 mg L- 1) < ketoprofen (EC50 = 24.84 mg L- 1) < diclofenac sodium salt (EC50 = 14.59 mg L- 1). Chronic toxicity data showed negative effects of the drugs on reproduction. Paracetamol and salicylic acid caused reduction in fecundity in concentrations starting from 10 mg L- 1 and 35 mg L- 1, respectively. Ketoprofen caused total inhibition at 5 mg L- 1. MEC/PNEC values were relatively low for all drugs. The risk was estimated as low or insignificant, except for caffeine, whose MEC/PNEC value was greater than 1 (moderate risk).


Subject(s)
Cladocera , Ketoprofen , Water Pollutants, Chemical , Animals , Acetaminophen , Diclofenac , Caffeine , Ketoprofen/pharmacology , Fresh Water , Risk Assessment , Salicylic Acid/pharmacology , Water Pollutants, Chemical/toxicity
18.
Chemosphere ; 336: 139156, 2023 Sep.
Article in English | MEDLINE | ID: mdl-37290514

ABSTRACT

A Surface Plasmon Resonance (SPR) biosensor based on an inhibition immunoassay was developed for the detection of diclofenac (DCF) in aqueous solution. Due to the small size of DCF, an hapten-protein conjugate was produced by coupling DCF to bovine serum albumin (BSA). DCF-BSA conjugate formation was confirmed via MALDI-TOF mass spectrometry. The resulting conjugate was immobilized onto the surface of a sensor fabricated via e-beam deposition of a 2 nm chromium adhesion layer followed by a 50 nm gold layer onto precleaned BK7 glass slides. Immobilization onto the nano thin gold surface was accomplished by covalent amide linkage through a self-assembled monolayer. Samples were composed of a mixture of antibody at a fixed concentration and DCF at different known concentrations in deionized water, causing the inhibition of anti-DCF on the sensor. The DCF-BSA was obtained with a ratio of 3 DCF molecules per BSA. A calibration curve was performed using concentrations between 2 and 32 µg L-1. The curve was fitted using the Boltzmann equation, reaching a limit of detection (LOD) of 3.15 µg L-1 and limit of quantification (LOQ) of 10.52 µg L-1, the inter-day precision was calculated and an RSD value of 1.96% was obtained; and analysis time of 10 min. The developed biosensor is a preliminary approach to the detection of DCF in environmental water samples, and the first SPR biosensor developed for DCF detection using a hapten-protein conjugate.


Subject(s)
Biosensing Techniques , Surface Plasmon Resonance , Surface Plasmon Resonance/methods , Biosensing Techniques/methods , Diclofenac , Water , Immunoassay/methods , Haptens , Serum Albumin, Bovine , Gold/chemistry
19.
Reprod Toxicol ; 120: 108422, 2023 09.
Article in English | MEDLINE | ID: mdl-37330176

ABSTRACT

Cadmium (Cd) is often detected in the environment due to its wide use in industry; also, NSAIDs are one of the most consumed pharmaceuticals, particularly diclofenac (DCF). Several studies have reported the presence of both contaminants in water bodies at concentrations ranging from ng L-1 to µg L-1; in addition, they have shown that they can induce oxidative stress in aquatic species and disturb signal transduction, cell proliferation, and intercellular communication, which could lead to teratogenesis. Spirulina has been consumed as a dietary supplement; its antioxidant, anti-inflammatory, neuroprotective, and nutritional properties are well documented. This work aimed to evaluate if Spirulina reduces the damage induced by Cd and DCF mixture in Xenopus laevis at early life stages. FETAX assay was carried out: 20 fertilized oocytes were exposed to seven different treatments on triplicate, control, Cd (24.5 µg L-1), DCF (149 µg L-1), Cd + DCF, Cd+DCF+Spirulina (2 mg L-1), Cd+DCF+Spirulina (4 mg L-1), Cd+DCF+Spirulina (10 mg L-1), malformations, mortality, and growth were evaluated after 96 h, also lipid peroxidation, superoxide dismutase and catalase activity were determined after 192 h. Cd increased DCF mortality, Cd and DCF mixture increased the incidence of malformations as well as oxidative damage; on the other hand, the results obtained show that Spirulina can be used to reduce the damage caused by the mixture of Cd and DCF since it promotes growth, reduce mortality, malformations, and oxidative stress in X. laevis.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal , Spirulina , Animals , Anti-Inflammatory Agents, Non-Steroidal/toxicity , Spirulina/metabolism , Xenopus laevis , Cadmium/toxicity , Diclofenac/toxicity , Oxidative Stress , Antioxidants/pharmacology , Metals
20.
Article in English | MEDLINE | ID: mdl-37128145

ABSTRACT

Diclofenac is an emerging pollutant: toxic, persistent, and bioaccumulative, present in several environmental niches in a concentration of parts per million. This pharmaceutical's biological removal was reported with various fungal species, showing promissory results. This work aimed at diclofenac removal by individually challenging the fungal species Pleurotus ostreatus, Aspergillus niger, and Penicillium roquefortii but triying to lower the biosorption nature of cell walls by NaCl addition. P. ostreatus removed 100% of the initial diclofenac concentration, whereas A. niger and P. roqueforti removed 74% and 32%, respectively. In all three cases, biosorption by polar interactions was negligible. We demonstrated that stressful environments, such as mineral media, force the fungus to take advantage of its metabolic tools to survive, hence showing higher removal capacity when limiting growth conditions. Bioremediation is an excellent alternative to give residual fungal biomass a secondary use.


Subject(s)
Diclofenac , Pleurotus , Biodegradation, Environmental , Aspergillus niger/metabolism , Biomass , Pleurotus/metabolism , Fungi
SELECTION OF CITATIONS
SEARCH DETAIL