ABSTRACT
In this study, we have utilized theoretical calculations to predict the reaction active sites of naproxen when reacting with radicals and to further study the thermodynamics and kinetics of the reactions with ·OH and SO4-·. The evidence, derived from the average local ionization energy and electrostatic potential, points to the naphthalene ring as the preferred site of attack, especially for the C2, C6, C9, and C10 sites. The changes in Gibbs free energy and enthalpy of the reactions initiated by ·OH and SO4-· ranged between -19.6 kcal/mol - 26.3 kcal/mol and -22.3 kcal/mol -18.5 kcal/mol, respectively. More in-depth investigation revealed that RA2 pathway for ·OH exhibited the lowest free energy of activation, suggesting this reaction is more inclined to proceed. The second-order rate constant results indicate the ·OH attacking reaction is faster than reactions initiated by SO4·-, yet controlled by diffusion. The consistency between theoretical findings and experimental data underscores the validity of this computational method for our study.
Subject(s)
Hydroxyl Radical , Naproxen , Sulfates , Thermodynamics , Naproxen/chemistry , Kinetics , Hydroxyl Radical/chemistry , Sulfates/chemistry , Water/chemistry , Models, ChemicalABSTRACT
Colorectal cancer is a life-threatening and prevalent type of cancer. However, a number of current treatments have serious side effects, which increase the need for alternatives. Non-steroidal anti-inflammatory drugs have potential chemopreventive capabilities. The present study aimed to confirm this, as well as to investigate potential pathways and reasons for this trait. To accomplish this, cancerous Colo320 and healthy CCD-18 cells were treated with various concentrations of naproxen sodium (NS). A caspase-3 assay revealed a statistically significant increase in caspase-3 activity in Colo320 cells (300%; P<0.01), but not in CCD-18 cells. This chemical was also associated with a significant decrease in Colo320 cell survival (-72.888%; P<0.01), but not CCD-18 cell survival. Furthermore, NS was found to significantly decrease the migration of Colo320 cells (86.58%; P<0.01). Finally, RNA sequencing of cells treated with NS revealed the statistically significant downregulation of the mucin 5B, oligomeric mucus/gel-forming, S100 calcium binding protein A9 and mucin 5AC, oligomeric mucus/gel-forming genes, which are upregulated in colorectal cancer and are known to contribute to cancer proliferation, stemness and drug resistance. These novel biological pathway results were further confirmed using ELISAs. The present study identified a novel molecular mechanism of the anti-colorectal cancer activity of NS.
ABSTRACT
In this study, magnetic graphene oxide coated with poly(8-hydroxyquinoline) was successfully synthesized, characterized, and utilized as a novel sorbent for the ultrasonic-assisted dispersive magnetic solid-phase extraction of naproxen and ibuprofen. These analytes served as representative analytes for two nonsteroidal anti-inflammatory drugs in various real samples. Characterization techniques, such as IR, X-ray powder diffraction, field emission scanning electron microscopy, energy-dispersive X-ray-mapping, and Brunauer-Emmett-Teller (BET), were used to confirm the correctness synthesis and preparation of the nanocomposites. Effective parameters on the extraction efficiency were investigated to maximize the analytical performance of the developed method. The dynamic range (1-1000 µg L-1), coefficients of determination (R2 ≥ 0.997), the limits of detection (0.3-1.0 µg L-1), and limit of quantification (1.0-3.0 µg L-1), intra-day and inter-day precisions (3.5%-7.2%) were achieved. The method validation results showed extraction recovery ranging from 80.4% to 96.0% and preconcentration factors ranging from 137 to 140.
ABSTRACT
Pharmaceutical active compounds (PhACs) are detected pollutants in aquatic environments worldwide at concentrations ranging from ng L-1 to µg L-1. Currently, PhAC monitoring is poorly realized in Mexico. This study proposes a priority list of PhACs in Mexican aquatic environments, considering their occurrence and environmental and human health risks. Ecological risks were assessed as Risk Quotients (RQ) values using the PhAC concentrations detected in surface water, obtaining high risks (RQ > 1) against aquatic organisms, especially of naproxen, ibuprofen, diclofenac, acetaminophen, 17ß-estradiol, carbamazepine, ketoprofen, caffeine. In contrast, potential human health risks (RQH) were assessed on the Mexican population using the concentrations quantified in groundwater, demonstrating potential risks (RQH > 0.2) on the population, particularly of DCF and CBZ. Thus, a priority list of PhACs can be used as a reference for environmental monitoring in Mexican water supplies as well as PhACs monitoring in countries of the Caribbean region and Central America.
ABSTRACT
The close association between inflammation and cancer inspired the synthesis of a series of 1,3,4-oxadiazole derivatives (compounds H4-A-F) of 6-methoxynaphtalene. The chemical structures of the new compounds were validated utilizing Fourier-transform infrared, proton nuclear magnetic resonance, and carbon-13 nuclear magnetic resonance spectroscopic techniques and CHN analysis. Computer-aided drug design methods were used to predict the compounds biological target, ADMET properties, toxicity, and to evaluate the molecular similarities between the design compounds and erlotinib, a standard epidermal growth factor receptor (EGFR) inhibitor. The antiproliferative effects of the new compounds were evaluated by the 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide assay, cell cycle analysis, apoptosis detection by microscopy, quantitative reverse transcription-polymerase chain reaction, and immunoblotting, and EGFR enzyme inhibition assay. In silico analysis of the new oxadiazole derivatives indicated that these compounds target EGFR, and that compounds H4-A, H4-B, H4-C, and H4-E show similar molecular properties to erlotinib. Additionally, the results indicated that none of the synthesized compounds are carcinogenic, and that compounds H4-A, H4-C, and H4-F are nontoxic. Compound H4-A showed the best-fit score against EGFR pharmacophore model, however, the in vitro studies indicated that compound H4-C was the most cytotoxic. Compound H4-C caused cytotoxicity in HCT-116 colorectal cancer cells by inducing both apoptosis and necrosis. Furthermore, compounds H4-D, H4-C, and H4-B had potent inhibitory effect on EGFR tyrosine kinase that was comparable to erlotinib. The findings of this inquiry offer a basis for further investigation into the differences between the synthesized compounds and erlotinib. However, additional testing will be needed to assess all of these differences and to identify the most promising compound for further research.
Subject(s)
Antineoplastic Agents , ErbB Receptors , Molecular Docking Simulation , Naproxen , Oxadiazoles , ErbB Receptors/antagonists & inhibitors , Humans , Oxadiazoles/pharmacology , Oxadiazoles/chemistry , Oxadiazoles/chemical synthesis , Naproxen/pharmacology , Naproxen/analogs & derivatives , Naproxen/chemistry , Naproxen/chemical synthesis , Antineoplastic Agents/pharmacology , Antineoplastic Agents/chemistry , Antineoplastic Agents/chemical synthesis , Cell Line, Tumor , Apoptosis/drug effects , Erlotinib Hydrochloride/pharmacology , Erlotinib Hydrochloride/chemistry , Protein Kinase Inhibitors/pharmacology , Protein Kinase Inhibitors/chemistry , Protein Kinase Inhibitors/chemical synthesis , Cell Proliferation/drug effectsABSTRACT
In this study, a new magnetic solid phase extraction based on magnetic composite modified with biochar obtained from pumpkin peel was developed for the enrichment and extraction of Naproxen in lake water, tablet and urine samples. The effects of main parameters such as pH, extraction time, amount of adsorbent and sample volume, which affect magnetic solid phase extraction, were investigated. Under optimal conditions, intraday and interday precision values for naproxen were below 5.9, with accuracy (relative error) better than 7.0â¯%. The detection limit and preliminary concentration factor were 12â¯ng/mL and 10, respectively. The method proposed here can be used for routine analysis of naproxen in lake water, urine and tablets.
Subject(s)
Limit of Detection , Naproxen , Solid Phase Extraction , Tablets , Naproxen/analysis , Naproxen/urine , Solid Phase Extraction/methods , Chromatography, High Pressure Liquid/methods , Tablets/analysis , Lakes/chemistry , Water/chemistry , Water Pollutants, Chemical/analysis , Hydrogen-Ion Concentration , Magnetics , Reproducibility of Results , Adsorption , Charcoal/chemistryABSTRACT
Photochemical and photocatalytic oxidation of naproxen (NPX) with UV-A light and commercial TiO2 under constant flow of oxygen have been investigated. Adsorption experiments indicated that 90% of the solute remained in the solution. Combined chemical analysis of samples on the photochemical degradation indicated that NPX in an aqueous solution (20 ppm) is efficiently transformed into other species but only 18% of the reactant is mineralized into CO2 and water after three hours of reaction. Performing the photocatalytic oxidation in the presence of TiO2, more than 80% of the organic compounds are mineralized by reactive oxidation species (ROS) within four hours of reaction. Analysis of reaction mixtures by a combination of analytical techniques indicated that naproxen is transformed into several aromatic naphthalene derivatives. These latter compounds are eventually transformed into polyhydroxylated aromatic compounds that are strongly adsorbed onto the TiO2 surface and are quickly oxidized into low-molecular-weight acids by an electron transfer mechanism. Based on this and previous studies on NPX photocatalytic oxidation, a unified and complete degradation mechanism is presented.
ABSTRACT
Non-steroidal anti-inflammatory drugs (NSAIDs) are among the most widely utilized pharmaceuticals worldwide. Besides their recognized anti-inflammatory effects, these drugs exhibit various other pleiotropic effects in several cells, including platelets. Within this article, the multifaceted properties of NSAIDs on platelet functions, activation and viability, as well as their interaction(s) with established antiplatelet medications, by hindering several platelet agonists' pathways and receptors, are thoroughly reviewed. The efficacy and safety of NSAIDs as adjunctive therapies for conditions involving inflammation and platelet activation are also discussed. Emphasis is given to the antiplatelet potential of commonly administered NSAIDs medications, such as ibuprofen, diclofenac, naproxen and ketoprofen, alongside non-opioid analgesic and antipyretic medications like paracetamol. This article delves into their mechanisms of action against different pathways of platelet activation, aggregation and overall platelet functions, highlighting additional health-promoting properties of these anti-inflammatory and analgesic agents, without neglecting the induced by these drugs' side-effects on platelets' functionality and thrombocytopenia. Environmental issues emerging from the ever-increased subscription of these drugs are also discussed, along with the need for novel water treatment methodologies for their appropriate elimination from water and wastewater samples. Despite being efficiently eliminated during wastewater treatment processes on occasion, NSAIDs remain prevalent and are found at significant concentrations in water bodies that receive effluents from wastewater treatment plants (WWTPs), since there is no one-size-fits-all solution for removing all contaminants from wastewater, depending on the specific characteristics of the wastewater. Several novel methods have been studied, with adsorption being proposed as a cost-effective and environmentally friendly method for wastewater purification from such drugs. This article also presents limitations and future prospects regarding the observed antiplatelet effects of NSAIDs, as well as the potential of novel derivatives of these compounds, with benefits in other important platelet functions.
ABSTRACT
Sodium hyaluronate (HA) is a natural polysaccharide. This biopolymer occurs in many tissues of living organisms. The regenerating, nourishing, and moisturizing properties as well as the rheological properties of HA enable its application in the pharmaceutical industry as a carrier of medicinal substances. The aim of this work was to assess the release of naproxen sodium (Nap) in the presence of lidocaine hydrochloride (Lid) from the biopolymer-based hydrogels and to determine the respective kinetic parameters of this process. The possible interaction between the HA polysaccharide carrier and the selected drugs was also investigated. Three hydrogels containing Nap and Lid with different concentrations of the biopolymer were prepared. The release of Nap was studied by employing USP apparatus 5. The infrared study and differential scanning calorimetry analysis of physical mixtures and dried formulations were performed. The highest amount of Nap was released from the formulation with the lowest concentration of the biopolymer. The most representative kinetic model that described the dissolution of Nap was obtained through the Korsmeyer-Peppas equation. The release rate constants were in the range of 1.0 ± 0.1 × 10-2 min-n-1.7 ± 0.1 × 10-2 min-n. Lid did not influence the dissolution of Nap from the formulations tested; however, in the desiccated samples of assessed formulations, the interaction between the polysaccharide and both drugs was observed.
ABSTRACT
OBJECTIVE AND SIGNIFICANCE: Reducing the dimensions, when other additives are present, shows potential as a method to improve the dissolution and solubility of biopharmaceutical classification system class II drugs that have poor solubility. In this investigation, the process involved grinding naproxen with nicotinamide with the aim of improving solubility and the rate of dissolution. METHODS: Naproxen was subjected to co-milling with urea, dimethylurea, and nicotinamide using a planetary ball mill for a duration of 90 min, maintaining a 1:1 molar ratio for the excipients (screening studies). The co-milled combinations, naproxen in its pure milled form, and a physical mixture were subjected to analysis using X-ray powder diffraction (XRPD), scanning electron microscopy (SEM), and solubility assessment. The mixture displaying the highest solubility (naproxen-nicotinamide) was chosen for further investigation, involving testing for intrinsic dissolution rate (IDR) and Fourier-transform infrared spectroscopy (FTIR) after co-milling for both 90 and 480 min. RESULTS AND CONCLUSION: The co-milled combination, denoted as S-3b and consisting of the most substantial ratio of nicotinamide to naproxen at 1:3, subjected to 480 min of milling, exhibited a remarkable 45-fold increase in solubility and a 9-fold increase in IDR. XRPD analysis of the co-milled samples demonstrated no amorphization, while SEM images portrayed the aggregates of naproxen with nicotinamide. FTIR outcomes negate the presence of any chemical interactions between the components. The co-milled sample exhibiting the highest solubility and IDR was used to create a tablet, which was then subjected to comprehensive evaluation for standard attributes. The results revealed improved compressibility and dissolution properties.
Subject(s)
Naproxen , Niacinamide , Solubility , Tablets , X-Ray Diffraction , Naproxen/chemistry , Niacinamide/chemistry , X-Ray Diffraction/methods , Excipients/chemistry , Chemistry, Pharmaceutical/methods , Spectroscopy, Fourier Transform Infrared/methods , Drug Compounding/methods , Microscopy, Electron, Scanning/methodsABSTRACT
Nanodrugs offer promising alternatives to conventionally used over the counter drugs. Compared to its free form, therapeutic benefits, and gastric tissue safety of naproxen sodium nanoformulation (NpNF) were recently demonstrated. Essential regulatory safety data for this formulation are, however, not available. To address this, male and female BALB/c mice were subjected to acute and 14-day repeated-oral dose assessments. Our data indicate that NpNF was well tolerated up to 2000 mg/kg b.w. A 14-day subacute toxicity testing revealed that the oral administration of low dose (30 mg/kg) NpNF did not produce any adverse effects on blood profile and serum biochemical parameters. Levels of oxidative stress markers and antioxidant enzymes neared normal. Histology of selected tissues also showed no evidence of toxicity. In contrast, a ten-fold increase in NpNF dosage (300 mg/kg), demonstrated, irrespective of gender, mild to moderate toxicity (p < 0.05) in the brain, stomach, and heart tissues, while ROS, LPO, CAT, SOD, POD, and GSH levels remained unaffected in the liver, kidney, spleen, testis, and seminal vesicles. No effect on serum biochemical parameters, overall indicated a no-observed-adverse-effect level (NOAEL) is 300 mg/kg. Further increase in dosage (1000 mg/kg) significantly altered all parameters demonstrating that high dose is toxic.
Subject(s)
Mice, Inbred BALB C , Naproxen , Toxicity Tests, Acute , Toxicity Tests, Subacute , Animals , Female , Naproxen/toxicity , Naproxen/administration & dosage , Male , Anti-Inflammatory Agents, Non-Steroidal/toxicity , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Mice , Administration, Oral , Oxidative Stress/drug effects , Nanoparticles/toxicity , Dose-Response Relationship, Drug , No-Observed-Adverse-Effect LevelABSTRACT
Patient can be exposed to the photodegradation products of a drug after skin application of topical formulations. NSAIDs, with analgesic and anti-inflammatory properties, are known for the potential photoinstability, and are applied often in the form of creams, gels or liquids, commonly used among athletes, elderly people, geriatric patients and patients treated with multidrug therapies. Susceptibility to photodegradation hazard of those group arises the need for development of a new approach, with the ability to evaluate the patient safety. We planned to use a rapid assessment procedure (RAP) of safety by testing the photostability of popular skin medicinal products. This method, proposed many years ago by WHO, is now reintroduced to analytical applications in industry, when emergency drugs (e.g. for Covid) are implemented to the market in accelerated procedures. In the health care system, qualitative evaluation of drugs is extremely valuable, therefore we have planned to identify photodegradation using the FTIR method - infrared spectroscopy and DSC - differential scanning calorimetry, whilst the risk of formation of genotoxic products using the Ames test. We have successfully demonstrated that changes in the chemical structure and physical form of both pure APIs and drug products containing the API be assessed in a short time. Another advantage of our work is the combination of the developed results from FTIR/NIR spectra with statistical analysis. As a result, full and quick qualitative assessment of the effects of photoexposure of selected NSAIDs is performed, fortunately showing no mutagenicity. Due to the popularity of NSAIDs applied to the skin, a gel containing naproxen and spray with indomethacin were selected for testing. The analysis carried out for various formulations of both preparations allows us to demonstrate the universality of the applied RAP methods in assessing the risk of hazard to the patient, thus we present research results that expand or widen the knowledge and assessment of risks related to the use of drugs on the skin.
Subject(s)
Anti-Inflammatory Agents, Non-Steroidal , Indomethacin , Naproxen , Photolysis , Skin , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Naproxen/chemistry , Naproxen/analysis , Indomethacin/chemistry , Humans , Skin/drug effects , Skin/radiation effects , Spectroscopy, Fourier Transform Infrared/methods , Calorimetry, Differential Scanning/methods , Administration, Cutaneous , Drug StabilityABSTRACT
Naproxen (NPX) as an emerging anthropogenic contaminant was detected in many water sources, which can pose a serious threat to the environment and human health. Peroxymonosulfate (PMS) decomposed by Cu(I) has been considered an effective activation method to produce reactive species. However, this decontamination process is restricted by the slow transformation of Cu(II)/Cu(I) by PMS. Herein, new N-(L-cysteine/triazine)-O-(carboxymethyl)-chitosan/cobalt ferrate-rice hull hybrid biocomposite was constructed to anchor the mixed-valent Cu(I)-Cu (II) (CuI, II-CCCF) for removing pharmaceutical pollutants (i.e., naproxen, ciprofloxacin, tetracycline, levofloxacin, and paracetamol). The structural, morphological, and catalytic properties of the CuI,II-CCCF have been fully identified by a series of physicochemical characterizations. Results demonstrated that the multifunctional, hydrophilic character, and negative ζ-potential of the activator, accelerating the redox cycle of Cu(II)/Cu(I) with hydroxyl amine (HA). The negligible metal leaching, well-balanced thermodynamic-kinetic properties, and efficient adsorption-catalysis synergy are the main reasons for the significantly enhanced catalytic performance of CuI,II-CCCF in the removal of NPX (98.6 % at 7.0 min). The main active species in the catalytic degradation of NPX were identified (âOH > SO4â- > 1O2 > > O2â-) and consequently suggested a degradation path. It can be noted that these types of carbohydrate-based nanocomposite offer numerous advantages, encompassing simple preparation, excellent decontamination capabilities, and long-term stability.
Subject(s)
Chitosan , Cobalt , Copper , Nanocomposites , Naproxen , Water Pollutants, Chemical , Chitosan/chemistry , Chitosan/analogs & derivatives , Nanocomposites/chemistry , Copper/chemistry , Naproxen/chemistry , Kinetics , Catalysis , Adsorption , Cobalt/chemistry , Water Pollutants, Chemical/chemistry , Peroxides/chemistry , Cysteine/chemistry , Water Purification/methods , IronABSTRACT
Soils represent crucial sinks for pharmaceuticals and microplastics, making them hotspots for pharmaceuticals and plastic pollution. Despite extensive research on the toxicity of pharmaceuticals and microplastics individually, there is limited understanding of their combined effects on soil biota. This study focused on the earthworm Eisenia fetida as test organism to evaluate the biotoxicity and bioaccumulation of the typical pharmaceutical naproxen and microplastics in earthworms. Results demonstrated that high concentrations of naproxen (100 mg kg-1) significantly increased the malondialdehyde (MDA) content, inducing lipid peroxidation. Even though the low exposure of naproxen exhibits no significant influence to Eisenia fetida, the lipid peroxidation caused by higher concentration than environmental relevant concentrations necessitate attention due to temporal and spatial concentration variability found in the soil environment. Meanwhile, microplastics caused oxidative damage to antioxidant enzymes by reducing the superoxide dismutase (SOD) activity and MDA content in earthworms. Metabolome analysis revealed increased lipid metabolism in naproxen-treated group and reduced lipid metabolism in the microplastic-treated group. The co-exposure of naproxen and microplastics exhibited a similar changing trend to the microplastics-treated group, emphasizing the significant influence of microplastics. The detection of numerous including lipids like 17-Hydroxyandrostane-3-glucuronide, lubiprostone, morroniside, and phosphorylcholine, serves to identify potential biomarkers for naproxen and microplastics exposure. Additionally, microplastics increased the concentration of naproxen in earthworms at sub-organ and subcellular level. This study contributes valuable insights into the biotoxicity and distribution of naproxen and microplastics in earthworms, enhancing our understanding of their combined ecological risk to soil biota.
Subject(s)
Microplastics , Naproxen , Oligochaeta , Soil Pollutants , Oligochaeta/drug effects , Naproxen/toxicity , Animals , Soil Pollutants/toxicity , Microplastics/toxicity , Ecotoxicology , Soil/chemistry , Environmental MonitoringABSTRACT
Immune response to biomaterials, which is intimately related to their surface properties, can produce chronic inflammation and fibrosis, leading to implant failure. This study investigated the development of magnetic nanoparticles coated with silica and incorporating the anti-inflammatory drug naproxen, aimed at multifunctional biomedical applications. The synthesized nanoparticles were characterized using various techniques that confirmed the presence of magnetite and the formation of a silica-rich bioactive glass (BG) layer. In vitro studies demonstrated that the nanoparticles exhibited bioactive properties, forming an apatite surface layer when immersed in simulated body fluid, and biocompatibility with bone cells, with good viability and alkaline phosphatase activity. Naproxen, either free or encapsulated, reduced nitric oxide production, an inflammatory marker, while the BG coating alone did not show anti-inflammatory effects in this study. Overall, the magnetic nanoparticles coated with BG and naproxen showed promise for biomedical applications, especially anti-inflammatory activity in macrophages and in the bone field, due to their biocompatibility, bioactivity, and osteogenic potential.
Subject(s)
Coated Materials, Biocompatible , Glass , Magnetite Nanoparticles , Naproxen , Naproxen/pharmacology , Naproxen/chemistry , Glass/chemistry , Coated Materials, Biocompatible/chemistry , Coated Materials, Biocompatible/pharmacology , Magnetite Nanoparticles/chemistry , Animals , Mice , Humans , Nitric Oxide/metabolism , Biocompatible Materials/chemistry , Biocompatible Materials/pharmacology , Silicon Dioxide/chemistry , Cell Survival/drug effects , RAW 264.7 Cells , Osteogenesis/drug effectsABSTRACT
Ibuprofen (IBU) and naproxen (NPX), as widely prescribed non-steroidal anti-inflammatory drugs (NSAIDs), are largely produced and consumed globally, leading to frequent and ubiquitous detection in various aqueous environments. Previously, the microbial transformation of them has been given a little attention, especially with the isolated fungus. A yeast-like Apiotrichum sp. IB-1 has been isolated and identified, which could simultaneously transform IBU (5 mg/L) and NPX (2.5 mg/L) with maximum efficiencies of 95.77% and 88.31%, respectively. For mono-substrate, the transformation efficiency of IB-1 was comparable to that of co-removal conditions, higher than most of isolates so far. IBU was oxidized mainly through hydroxylation (m/z of 221, 253) and NPX was detoxified mainly via demethylation (m/z of 215) as shown by UPLC-MS/MS results. Based on transcriptome analysis, the addition of IBU stimulated the basic metabolism like TCA cycle. The transporters and respiration related genes were also up-regulated accompanied with higher expression of several dehydrogenase, carboxylesterase, dioxygenase and oxidoreductase encoding genes, which may be involved in the transformation of IBU. The main functional genes responsible for IBU and NPX transformation for IB-1 should be similar in view of previous studies, which needs further confirmation. This fungus would be useful for potential bioremediation of NSAIDs pollution and accelerate the discovery of functional oxidative genes and enzymes different from those of bacteria.
Subject(s)
Anti-Inflammatory Agents, Non-Steroidal , Biotransformation , Ibuprofen , Naproxen , Ibuprofen/metabolism , Naproxen/metabolism , Anti-Inflammatory Agents, Non-Steroidal/metabolism , Biodegradation, EnvironmentalABSTRACT
Deformable nanovesicles have a crucial role in topical drug delivery through the skin, due to their capability to pass intact the stratum corneum and epidermis (SCE) and significantly increase the efficacy and accumulation of payloads in the deeper layers of the skin. Namely, lipid-based ultradeformable nanovesicles are versatile and load bioactive molecules with different physicochemical properties. For this reason, this study aims to make oleic acid based nanovesicles (oleosomes) for the codelivery of icariin and sodium naproxen and increase their permeation through the skin. Oleosomes have suitable physicochemical properties and long-term stability for a potential dermal or transdermal application. The inclusion of oleic acid in the lipid bilayer increases 3-fold the deformable properties of oleosomes compared to conventional liposomes and significantly improves the percutaneous permeation of icariin and sodium naproxen through the human SCE membranes compared to hydroalcoholic solutions of both drugs. The tolerability studies on human volunteers demonstrate that oleosomes are safer and speed up the recovery of transepidermal water loss (TEWL) baselines compared to saline solution. These results highlight promising properties of icariin/sodium naproxen coloaded oleosomes for the treatment of skin disorders and suggest the potential future applications of these nanovesicles for further in vivo experiments.
ABSTRACT
Cadmium sulfide and zinc oxide nanoparticles were prepared, characterized and used as electrode modifiers for the sensing of two non-steroidal anti-inflammatory drugs (NSAIDs): naproxen and mobic. The structural and morphological characterization of the synthesized nanoparticles was carried out by XRD, UV-Vis spectroscopy, FTIR and scanning electron microscopy. The electrode's enhanced surface area facilitated the signal amplification of the selected NSAIDs. The CdS-modified glassy carbon electrode (GCE) enhanced the electro-oxidation signals of naproxen to four times that of the bare GCE, while the ZnO-modified GCE led to a two-fold enhancement in the electro-oxidation signals of mobic. The oxidation of both NSAIDs occurred in a pH-dependent manner, suggesting the involvement of protons in their electron transfer reactions. The experimental conditions for the sensing of naproxen and mobic were optimized and, under optimized conditions, the modified electrode surface demonstrated the qualities of sensitivity and selectivity, and a fast responsiveness to the target NSAIDs.
ABSTRACT
Photochemical active species generated from photosensitizers, e.g., dissolved organic matter (DOM), play vital roles in the transformation of micropollutants in water. Here, butanedione (BD), a redox-active moiety in DOM and widely found in nature, was employed to photo-transform naproxen (NPX) with peracetic acid (PAA) and H2O2 as contrasts. The results obtained showed that the BD exhibited more applicable on NPX degradation. It works in the lake or river water under UV and solar irradiation, and its NPX degradation efficiency was 10-30 times faster than that of PAA and H2O2. The reason for the efficient transformation of pollutants is that the BD system was proved to be a non-free radical dominated mechanism. The quantum yield of BD (Ф254 nm) was calculated to be 0.064, which indicates that photophysical process is the dominant mode of BD conversion. By adding trapping agents, direct energy transfer from 3BD* to NPX (in anoxic environment) or dissolved oxygen (in aerobic environment) was proved to play a major role (> 91 %). Additionally, the BD process reduces the toxicity of NPX and promotes microbial growth after irradiation. Overall, this study significantly deepened the understanding of the transformation between BD and micropollutants, and provided a potential BD-based process for micropollutants removal under solar irradiation.
Subject(s)
Naproxen , Photolysis , Ultraviolet Rays , Water Pollutants, Chemical , Naproxen/chemistry , Water Pollutants, Chemical/chemistry , Water Pollutants, Chemical/radiation effects , Energy Transfer , Hydrogen Peroxide/chemistry , Peracetic Acid/chemistry , Photochemical ProcessesABSTRACT
Naproxen is a nonsteroidal anti-inflammatory drug used to treat nonrheumatic inflammation, migraine, and gout. Therefore, the determination of naproxen in pharmaceutical and biological samples is of particular importance. In the present work, SrTi0.7Fe0.3O3 perovskite/Chitosan nanosheets were used to modify the surface of a glassy carbon electrode (GCE) for highly sensitive determination of naproxen. To ensure the successful synthesis of the perovskite nanosheets, morphological studies including scanning electron microscopy (SEM), Energy-dispersive X-ray (EDX), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), and X-ray photoelectron spectroscopy (XPS) were carried out. The electrochemical investigations of naproxen on the modified surface of GCE were investigated and the limit of detection (LOD) and limit of quantification (LOQ) were acquired 0.50 and 1.67 µM, respectively. Additionally, the linear range (LR) of 1.99-130.84 µM was obtained for the oxidation of naproxen. The obtained results have been proved that the mentioned method is simple, sensitive, and specific with a short analysis time. The dominant analytical features of the designed sensor are possessing a low detection limit, excellent stability, repeatability, and high selectivity in the presence of naproxen. For investigation of the applicability of the designed assay in real sample analysis, human plasma samples have been examined and a recovery index was acquired 95%.