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This study presents the enantiomeric resolution of three profen drugs, viz., flurbiprofen (FLB), fenoprofen, and zaltoprofen by employing sitafloxacin (SIT) as a chiral selector within a direct thin-layer chromatography (TLC) method. Chromatographic resolution of three drugs was carried out using a mobile phase consisting of acetonitrile‒methanol‒trimethylamine (6:3:1, V/V, pH 8.5), with a stationary phase maintained at pH 5. Analytical validation of the FLB enantiomeric resolution exhibited consistent recovery rates, with coefficient of variation (%CV) values consistently below 2%. Furthermore, the method demonstrated sensitivity, with low limits of detection and quantification values of 0.058 and 0.172 µg per spot, respectively, for FLB enantiomers, indicating reliable detection at low concentrations. The analytical data validate the effectiveness and reliability of the developed TLC method for the enantiomeric resolution of profen drugs, offering significant implications for pharmaceutical research and development. [ABSTRACT FROM AUTHOR]

α-Methylacyl-CoA racemase in M. tuberculosis (MCR) has an essential role in fatty acid metabolism and cholesterol utilization, contributing to the bacterium's survival and persistence. Understanding the enzymatic activity and structural features of MCR provides insights into its physiological and pathological significance and potential as a therapeutic target. Here, we report high-resolution crystal structures for wild-type MCR in a new crystal form (at 1.65 Å resolution) and for three active-site mutants, H126A, D156A and E241A, at 2.45, 1.64 and 1.85 Å resolutions, respectively. Our analysis of the new wild-type structure revealed a similar dimeric arrangement of MCR molecules to that previously reported and details of the catalytic site. The determination of the structures of these H126A, D156A and E241A mutants, along with their detailed kinetic analysis, has now allowed for a rigorous assessment of their catalytic properties. No significant change outside the enzymatic active site was observed in the three mutants, establishing that the diminution of catalytic activity is mainly attributable to disruption of the catalytic apparatus involving key hydrogen bonding and water-mediated interactions. The wild-type structure, together with detailed mutational and biochemical data, provide a basis for understanding the catalytic properties of this enzyme, which is important for the design of future anti-tuberculosis drug molecules. [ABSTRACT FROM AUTHOR]

The aim and objective of this investigation focus on the formulation of mouth-dissolving tablets of Fenoprofen calcium dihydrate spray dried solid dispersions. Materials and methods. Spray drying is a well-recognized manufacturing technique that can be used to create amorphous solid dispersions, which are an effective delivery method for poorly water-soluble pharmaceuticals such as Fenoprofen calcium dihydrate (FCD). In addition to skimmed milk powder (SMP) and FCD, the carrier β-cyclodextrin was used to produce solid dispersions. Results and discussion. The production of solid dispersions yielded reproducible results. Solid dispersion with β-cyclodextrin and skimmed milk powder is one way to increase disintegration time by increasing the water solubility of inadequately water-soluble FCD. In-vitro dissolution experiments of FCD mouth-dissolving tablets revealed significant differences. Stability studies should evaluate drug product characteristics that are susceptible to change during storage and are anticipated to impact quality, safety, and efficacy to demonstrate that the optimal formulations remain stable over the course of the study. The results of stability experiments were statistically significant at p<0.05 using one-way ANOVA followed by Dunnet's test. During in-vivo anti-inflammatory experiments, the formulation SDC6 demonstrated a greater percentage of inhibition than the purified drug and super disintegrant, and the results were statistically significant using one-way ANOVA followed by the Bonferroni test. Conclusions. The solid dispersions were prepared with β-cyclodextrin, and skimmed milk powder improved the solubility of the poorly water-soluble fenoprofen calcium dihydrate. In vitro dissolution experiments of fenoprofen calcium dihydrate mouth dissolving tablets and controlled tablets revealed significant differences [ABSTRACT FROM AUTHOR]

Objective: To confirm the relevance of upper and lower airway inflammation in eosinophilic chronic rhinosinusitis (ECRS), the effects of endoscopic sinus surgery (ESS) on lower airway functions and inflammation need to be examined in ECRS patients. Methods: Chronic rhinosinusitis patients with nasal polyps (25 non-ECRS, 28 ECRS) were enrolled. The 12 patients in the ECRS group had comorbid asthma, in contrast to none in the non-ECRS group. We divided ECRS patients into 2 groups of ECRS with and without asthma. Clinical markers, including fraction of exhaled nitric oxide (FeNO), respiratory functions, and the Asthma Control Test (ACT) questionnaire, were investigated before and after ESS. Results: The FeNO levels in the ECRS with asthma group decreased after ESS. The mean FeNO levels in this group were 56.3 ppb before ESS and 24.9, 25.1, 25.0, and 15.5 ppb 1, 2, 3, and 4 months, respectively, after ESS. The mean forced expiratory rates in 1 second before and after ESS were 67.6% and 73.0%, respectively. The mean maximal expiratory flow rates at 50% of the vital capacity before and after ESS were 45.8% and 58.0%, respectively. Significant differences were observed in respiratory functions before and after ESS. The mean ACT scores in the ECRS with asthma group before and after ESS were 17.5 and 23.5, respectively. The ACT scores were significantly higher after than before ESS. Conclusions: The present results indicate that ECRS and bronchial asthma are common eosinophilic airway inflammatory diseases, and ESS for eosinophilic sinusitis may improve lower airway function. [ABSTRACT FROM AUTHOR]

Aim: The study's goal was to develop and characterize a new type of Fenoprofen tablet that can float. Materials and Methods: Research on the drug's performulation was carried out to evaluate its organoleptic qualities, solubility, melting point, and partition coefficient. Bulk and pharmaceutical formulations of the medication were evaluated using UV spectroscopy to identify Fenoprofen in accordance with ICH Guidelines. Fenoprofen floating tablets were made utilizing the direct compression method with different concentrations of HPMC K100 M, Xanthan gum, and guar gum. Furthermore, a QbD method was used to manufacture the Fenoprofen tablets. To find the optimal formulation of the solid dispersed drug material in Fenoprofen tablets, a 23-full factorial Design of Experiment (DoE) was carried out using Design-Expert 22.0.2.0 software. Results: The produced tablets were subjected to a micromeritics research, which included both a pre- and post-compression phase. Using a USP Dissolution test device type II (Paddle), an in vitro dissolution research was conducted. There were three months of stability testing done at high temperatures. The research confirmed that Fenoprofen had a distinct odor and a white color look. Its melting point (MP) was 171°C, and it was soluble in DMSO without any difficulty. We measured 0.31gm/cm3 for the optimized formulation's bulk density, 0.46gm/cm3 for the tapped density, 14.78 for the Carr index, 1.42 for the hausner ratio, and 30.17 degrees for the angle of repose. The optimized batch (F4) including polymers and excipients floated for a long duration and had a short lag time for buoyancy. There was a 99.12 percent drug release rate after 12 hours in in vitro dissolution tests. Conclusion: The stability showing that formulation was stable for months of storage and minimal change was found in color, shape, appearance, drug content, in vitro dissolution studies and floating lag time value. [ABSTRACT FROM AUTHOR]

The presence of a chiral or chirally perturbed chromophore in the molecule under investigation is a fundamental requirement for the appearance of a circular dichroism (CD) spectrum. For native and for most of the substituted cyclodextrins, this condition is not applicable, because although chiral, cyclodextrins lack a chromophore group and therefore have no characteristic CD spectra over 220 nm. The reason this method can be used is that if the guest molecule has a chromophore group and this is in the right proximity to the cyclodextrin, it becomes chirally perturbed. As a result, the complex will now provide a CD signal, and this phenomenon is called induced circular dichroism (ICD). The appearance of the ICD spectrum is clear evidence of the formation of the complex, and the spectral sign and intensity is a good predictor of the structure of the complex. By varying the concentration of cyclodextrin, the ICD signal changes, resulting in a saturation curve, and from these data, the stability constant can be calculated for a 1:1 complex. This article compares ICD and NMR spectroscopic and molecular modeling results of cyclodextrin complexes of four model compounds: nimesulide, fenbufen, fenoprofen, and bifonazole. The results obtained by the different methods show good agreement, and the structures estimated from the ICD spectra are supported by NMR data and molecular modeling. [ABSTRACT FROM AUTHOR]

α-Methylacyl-CoA racemase in M. tuberculosis (MCR) has an essential role in fatty acid metabolism and cholesterol utilization, contributing to the bacterium’s survival and persistence. Understanding the enzymatic activity and structural features of MCR provides insights into its physiological and pathological significance and potential as a therapeutic target. Here, we report high-resolution crystal structures for wild-type MCR in a new crystal form (at 1.65 Å resolution) and for three active-site mutants, H126A, D156A and E241A, at 2.45, 1.64 and 1.85 Å resolutions, respectively. Our analysis of the new wild-type structure revealed a similar dimeric arrangement of MCR molecules to that previously reported and details of the catalytic site. The determination of the structures of these H126A, D156A and E241A mutants, along with their detailed kinetic analysis, has now allowed for a rigorous assessment of their catalytic properties. No significant change outside the enzymatic active site was observed in the three mutants, establishing that the diminution of catalytic activity is mainly attributable to disruption of the catalytic apparatus involving key hydrogen bonding and water-mediated interactions. The wild-type structure, together with detailed mutational and biochemical data, provide a basis for understanding the catalytic properties of this enzyme, which is important for the design of future anti-tuberculosis drug molecules.

The stability of host–guest complexes of two NSAID drugs with similar physicochemical properties, fenbufen and fenoprofen, was investigated by comparing induced circular dichroism and 1H nuclear magnetic resonance methods using eight cyclodextrins of different degrees of substitution and isomeric purity as guest compounds. These cyclodextrins include native β-cyclodextrin (BCyD), 2,6-dimethyl-β-cyclodextrin 50 (DIMEB50), 80 (DIMEB80) and 95% (DIMEB95) isomerically pure versions, low-methylated CRYSMEB, randomly methylated β-cyclodextrin (RAMEB) and 4.5 and 6.3 average substitution grade hydroxypropyl-β-cyclodextrin (HPBCyD). The stability constants obtained by the two methods show good agreement in most cases. For fenbufen complexes, there is a clear trend that the stability constant increases with the degree of substitution while isomer purity has a smaller effect on the magnitude of stability constants. A significant difference was found in the case of DIMEB50 when compared to DIMEB80/DIMEB95, while the latter two are similar. In the fenbufen–fenoprofen comparison, fenbufen, with its linear axis, gives a more stable complex, while fenoprofen shows lower constants and poorly defined trends. [ABSTRACT FROM AUTHOR]

The presence of a chiral or chirally perturbed chromophore in the molecule under investigation is a fundamental requirement for the appearance of a circular dichroism (CD) spectrum. For native and for most of the substituted cyclodextrins, this condition is not applicable, because although chiral, cyclodextrins lack a chromophore group and therefore have no characteristic CD spectra over 220 nm. The reason this method can be used is that if the guest molecule has a chromophore group and this is in the right proximity to the cyclodextrin, it becomes chirally perturbed. As a result, the complex will now provide a CD signal, and this phenomenon is called induced circular dichroism (ICD). The appearance of the ICD spectrum is clear evidence of the formation of the complex, and the spectral sign and intensity is a good predictor of the structure of the complex. By varying the concentration of cyclodextrin, the ICD signal changes, resulting in a saturation curve, and from these data, the stability constant can be calculated for a 1:1 complex. This article compares ICD and NMR spectroscopic and molecular modeling results of cyclodextrin complexes of four model compounds: nimesulide, fenbufen, fenoprofen, and bifonazole. The results obtained by the different methods show good agreement, and the structures estimated from the ICD spectra are supported by NMR data and molecular modeling.

Indisputable importance of drug solubility in various industrial perspectives has motivated the scientists to evaluate different techniques to improve it. Fenoprofen is a significant nonsteroidal anti-inflammatory drug (NSAID), that is the orally administered to relieve mild to moderate pain and the unfavorable symptoms of osteoarthritis and rheumatoid arthritis (i.e., inflammation and stiffness). Supercritical fluids (SCFs) belong to a certain type of fluids, in which their temperature and pressure are higher than the critical point. This property allows the CO2SCF to simultaneously possess the characteristics of both a liquid and a gas. The prominent target of this paper is to mathematically develop three predictive models via machine learning (ML) technique to optimize the solubility of Fenoprofen in CO2SCF. In this study, we have 32 data vectors in each dataset, including two input features of pressure and temperature. The output target is solubility, which we are going to model and analyze. Models are constructed through the use of Modular ANN (MANN), Gaussian processes regression (GPR), and the K-Nearest Neighbor technique (KNN) in this body of work. The glowworm swarm optimization (GSO) swarm-based method is utilized in order to carry out the process of model optimization. The root mean squared error (RMSE) rates for GSO-KNN, GSO-MANN, and GSO-GPR are respectively 5.25E-04, 5.46E-04, and 3.01E-05. The aforementioned models were also judged according to a number of other criteria, and since the GSO-GPR model was found to be the most effective according to all of these standards, it is being treated as the conclusive model of this investigation. In addition, the maximum error has been brought down to 5.02E-05 with the help of this model, which has an R2-score of 0.999.

The stability of host–guest complexes of two NSAID drugs with similar physicochemical properties, fenbufen and fenoprofen, was investigated by comparing induced circular dichroism and 1H nuclear magnetic resonance methods using eight cyclodextrins of different degrees of substitution and isomeric purity as guest compounds. These cyclodextrins include native β-cyclodextrin (BCyD), 2,6-dimethyl-β-cyclodextrin 50 (DIMEB50), 80 (DIMEB80) and 95% (DIMEB95) isomerically pure versions, low-methylated CRYSMEB, randomly methylated β-cyclodextrin (RAMEB) and 4.5 and 6.3 average substitution grade hydroxypropyl-β-cyclodextrin (HPBCyD). The stability constants obtained by the two methods show good agreement in most cases. For fenbufen complexes, there is a clear trend that the stability constant increases with the degree of substitution while isomer purity has a smaller effect on the magnitude of stability constants. A significant difference was found in the case of DIMEB50 when compared to DIMEB80/DIMEB95, while the latter two are similar. In the fenbufen–fenoprofen comparison, fenbufen, with its linear axis, gives a more stable complex, while fenoprofen shows lower constants and poorly defined trends.

The most effective anticancer drugs currently entail substantial and formidable side effects, and resistance of tumors to chemotherapeutic agents is a further challenge. Thus, the search for new anticancer drugs as well as novel therapeutic methods is still extremely important. Non-steroidal anti-inflammatory drugs (NSAIDs) can inhibit COX (cyclooxygenase), overexpressed in some tumors. Carboranes are emerging as promising pharmacophores. We have therefore combined both moieties in a single molecule to design drugs with a dual mode of action and enhanced effectiveness. The NSAIDs ibuprofen, flurbiprofen, and fenoprofen were connected with 1,2-dicarba-closo-dodecaborane(12) via methylene, ethylene or propylene spacers. Three sets of carborane-NSAID conjugates were synthesized and analyzed through multinuclear (1H, 11B, and 13C) NMR spectroscopy. Conjugates with methylene spacers exhibited the most potent COX inhibition potential, particularly conjugates with flurbiprofen and fenoprofen, displaying higher selectivity towards COX-1. Furthermore, conjugates with methylene and ethylene spacers were more efficient in suppressing the growth of human cancer cell lines than their propylene counterparts. The carborane-flurbiprofen conjugate with an ethylene spacer was the most efficient and selective toward the COX-2-negative cell line HCT116. Its mode of action was basically cytostatic with minor contribution of apoptotic cell death and dominance of cells trapped in the division process., (© 2024 Wiley‐VCH GmbH.)

Fenoprofen belongs to Biopharmaceutical Classification System (BCS) class II drugs which are poorly soluble in water. The objective of present research work was to prepare fast dissolving tablets of fenoprofen using varying concentrations of three different sublimating agents to improve the dissolution rate. Seven formulations were prepared containing different concentrations of camphor, ammonium bicarbonate and thymol as sublimating agent along with primogel as a superdisintegrant. Tablets were manufactured by direct compression method. The prepared tablets were evaluated for pre-compression and post-compression parameters result, for all formulations result was within official limits. DSC studies revealed that there were no interactions between the drug and the excipients used. From in vitro drug release studies the dissolution studies, cumulative percentage of drug release versus time was evaluated. It also reflects that the formulations F4 and F15 containing 45 mg and 67.5 mg of thymol respectively showed fast drug release of 100.00% and 99.56 % respectively in 30 minutes as compared with formulations containing other sublimating agents. Among all the formulations, F6 and F7 tablets showed complete drug release within 30 minutes and rapid dissolution. [ABSTRACT FROM AUTHOR]

Introduction: Polycystic ovary syndrome (PCOS) is a common illness worldwide and increases infertility risk. PCOS has an inflammatory syndrome that changes inflammatory markers. This experiment aims to evaluate the effect of the anti-inflammatory drug fenoprofen on the Omentin-1 gene expression levels. Methods and Materials: To do this, we categorized 25 Wistar rats into five experimental groups, including the control, PCOS, and treatment group. PCOS model induced by intramuscular injection of estradiol valerate in the estrus cycle to the experimental groups. After one month, the animals were treated with intraperitoneal (ip) injections in 5, 10, and 20 doses of fenoprofen for one week. After the treatment, rats were anesthetized by ip injection of ketamine and xylazine mixture, and the ovaries of rats were removed for Omentin-1 gene expression. The Omentin-1 levels were measured by real-time PCR. Results: The gene level of Omentin-1 in the PCOS group was lower than in comparison with the control group. Also, treatment with fenoprofen 20 doses showed a significant rise in the gene expression level of Omentin-1 in comparison of the PCOS group (p<0.05). Conclusion: In conclusion, in this experimental study, treatment with fenoprofen showed a significant effect in rats with PCOS. [ABSTRACT FROM AUTHOR]

Non-steroidal anti-inflammatory drugs (NSAIDs) have become important as an analgesic, antipyretic and antiinflammatory medications throughout the world. The main mechanism of NSAIDs action is inhibition both isoforms of the enzyme cyclooxygenase COX-1 andCOX-2, which catalyzes the synthesis of PGH2 from arachidonic acid. Some NSAIDs possess antimicrobial activity besides their anti-inflammatory activity. In order to design new derivative of Fenoprofen with antibacterial activity, its carboxylic group has been converted into hydrazone moiety, which have antimicrobial activity. The compounds then evaluated for their anti-bacterial activity by means of well- diffusionmethod. All the synthesized target compounds were characterized by FT-IR spectroscopy, 1HNMR analysis. The synthesis of the target compounds (H1-H4) was accomplished by multistep reaction procedures. The compounds were tested for antibacterial activity against two gram-positive bacteria (Staphylococcus aureus and Bacillus subtilis) and two gram-negatives bacteria (Escherichia coli and Klebsiella pneumoniae). The highest activity was established by compound B, which found to be highly active against both E. coli and Staph. aureus. [ABSTRACT FROM AUTHOR]

This work provides a comprehensive DFT study on the conversion mechanism and photoisomerization of the effective and commonly used nonsteroidal anti-inflammatory medicine fenoprofen. The results obtained exhibit that the rearrangement procedure of (R)-fenoprofen to its (S)-enantiomer occurs in [1,3]-hydrogen shifts with inversion of configuration at chiral center C8. According to the computed energies, we can find out that the excitation of (R)-fenoprofen methyl ester in its primary form to the first excited singlet state S1 at λ = 240 nm is the rate-limiting step of photoisomerization of fenoprofen. In order to obtain further insight into the isomerization process occurring upon excitation, this process was studied by scanning the C8-H11 distance for the excited singlet. Our calculations revealed that the isomerization process requires passing a barrier of approximately 84 kcal/mol. Furthermore, the more photostability of (S)-fenoprofen methyl ester than that of its related (R)-enantiomer can be attributed to the − 1.34 kcal/mol of thermodynamic stability of the (S)-fenoprofen methyl ester. [ABSTRACT FROM AUTHOR]

In the article, the author discusses the Darya Program to raise awareness about water safety at beaches, lakes, dams and inland rivers in Iran to ensure public safety, particularly children. Also cited are how the use of physical barriers like pool covers, fences and water entry alarms could prevent drowning in children, as well as the percentage of children who died due to unintentional drowning in the country annually.

The presence of a chiral or chirally perturbed chromophore in the molecule under investigation is a fundamental requirement for the appearance of a circular dichroism (CD) spectrum. For native and for most of the substituted cyclodextrins, this condition is not applicable, because although chiral, cyclodextrins lack a chromophore group and therefore have no characteristic CD spectra over 220 nm. The reason this method can be used is that if the guest molecule has a chromophore group and this is in the right proximity to the cyclodextrin, it becomes chirally perturbed. As a result, the complex will now provide a CD signal, and this phenomenon is called induced circular dichroism (ICD). The appearance of the ICD spectrum is clear evidence of the formation of the complex, and the spectral sign and intensity is a good predictor of the structure of the complex. By varying the concentration of cyclodextrin, the ICD signal changes, resulting in a saturation curve, and from these data, the stability constant can be calculated for a 1:1 complex. This article compares ICD and NMR spectroscopic and molecular modeling results of cyclodextrin complexes of four model compounds: nimesulide, fenbufen, fenoprofen, and bifonazole. The results obtained by the different methods show good agreement, and the structures estimated from the ICD spectra are supported by NMR data and molecular modeling.

The presence of various classes of pharmaceutical drugs in different environmental compartments has been reported worldwide. In South Africa, the detection of pharmaceuticals especially the non-steroidal anti-inflammatory drugs is recent, and more studies are being done in order to fully understand their fate in the aquatic environment. With considerations for the need of better sample preparation techniques, this study synthesized a molecularly imprinted polymer for the selective extraction of a non-steroidal anti-inflammatory drug, fenoprofen in aqueous environmental samples. Batch adsorption studies showed that adsorption of fenoprofen onto the cavities of the polymer followed a Langmuir isotherm as well as a pseudo second order model implying formation of a monolayer on the surface through chemisorption. The polymer had a maximum adsorption capacity of 38.8 mg g−1 and a Langmuir surface area of 1607 m2 g−1. The imprinted polymer was then used as the selective sorbent for solid phase extraction in the analysis of fenoprofen from wastewater followed by chromatographic determination. The analytical method gave a detection limit of 0.64 ng mL−1 and recovery of 99.6%. The concentration of fenoprofen detected in influent and effluent samples from two wastewater treatment plants ranged from 24 to 58 ng mL−1. The ability of the treatment plants to remove fenoprofen during wastewater processing based on the difference in concentrations in influent and effluent samples was found to be 41%. This work has shown that there is a possibility of release of fenoprofen from wastewater treatment plants into surface water sources. [ABSTRACT FROM AUTHOR]

Infiltration of treated wastewater (TWW) to recharge depleted aquifers, often referred to as managed aquifer recharge, is a solution to replenish groundwater resources in regions facing water scarcity. We present a mass balance approach to infer the amounts of five pharmaceuticals (carbamazepine, diclofenac, fenoprofen, gemfibrozil, and naproxen) degraded in column experiments based on concentrations of pharmaceuticals in the aqueous and solid (sorbed) phases. Column experiments were conducted under three different conditions: continuous infiltration, wetting and drying cycles, and wetting and drying cycles with elevated concentrations of antibiotics (which may reduce microbially aided degradation of other compounds). A mass balance comparing pharmaceutical mass in the water phase over the 16-month duration of the experiments to mass sorbed to the soil was used to infer the mass of pharmaceuticals degraded. Results show sorption as the main attenuation mechanism for carbamazepine. About half of the mass of diclofenac was degraded with wetting and drying cycles, but no significant degradation was found for continuous infiltration, while 32% of infiltrated mass sorbed. Fenoprofen was degraded in the shallow and aerobic part of the soil, but degradation appeared to cease beyond 27 cm depth. Gemfibrozil attenuated through a combination of degradation and sorption, with slight increases in attenuation with depth from both mechanisms. Naproxen degraded progressively with depth, resulting in attenuation of >90% of the mass. In the column with elevated concentrations of antibiotics, the antibiotics attenuated to about 50% or less of inflow concentrations by 27 cm depth and within this zone, less degradation of the other compounds was observed. [ABSTRACT FROM AUTHOR]

The aim of this study was to investigate microemulsion (ME) based topical delivery system for fenoprofen calcium (FPCa) to eliminate its oral gastrointestinal adverse effects. ME was prepared by the water titration method using oleic acid as oil phase, tween 80 as a surfactant and propylene glycol as a cosurfactant. Oleic acid was selected as oil phase due to its good solubilizing capacity. ME existence region was determined using pseudo-ternary phase diagrams for preparing different formulations. Six different formulations were selected with various values of oil (25-68%), water (2-3%), and the mixture of surfactant and cosurfactant (1:1) (24-67%). The selected ME formulae were characterized for optical birefringence, transmission electron microscopy (TEM), pH, % transmittance, electronic conductivity, drug content, droplet size, rheological properties and stability evaluation. In vitro release study of FPCa from ME s through the synthetic membrane and hairless rat skin were evaluated. The optimized formula ME5 consisting of 5% w/w FPCa, 60% w/w oleic acid as oil phase, 3% w/w aqueous phase, and 32% w/w of surfactant phase containing Tween 80 and propylene glycol (1: 1) showed the highest transdermal flux and highest skin permeation rate. Finally, the % inhibition of carrageenan-induced rat paw edema of the optimized formula ME5 was highly significant (p < 0.001) as compared to plain gel of FPCa. In conclusion, ME is a promising technique for topical delivery of FPCa. [ABSTRACT FROM AUTHOR]

Simple, accurate and robust spectrophotometric method was developed for determination of fenoprofen calcium drug (FPC). The proposed method was based on the charge transfer (CT) reaction of FPC drug (as n-electron donor) with 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ), 2,4,6-trinitrophenol (picric acid, PA) or 1,2,5,8-tetrahydroxyanthraquinone (Quinalizarin, QZ) (as π-acceptors) to give highly colored charge transfer complexes. Different variables affecting the reaction such as reagent concentration, temperature and time have been carefully optimized to achieve the highest sensitivity. Beer's law was obeyed over the concentration ranges of 2–60, 0.6–90 and 4–30 μg mL − 1 using DDQ, PA and QZ CT reagents, respectively, with correlation coefficients of 0.9986, 0.9989 and 0.997 and detection limits of 1.78, 0.48 and 2.6 μg mL − 1 for the CT reagents in the same order. Elucidation of the chemical structure of the solid CT complexes formed via reaction between the drug under study and π-acceptors was done using elemental, thermal analyses, IR, 1 H NMR and mass spectrometry. X-ray diffraction was used to estimate the crystallinity of the CT complexes. Their biological activities were screened against different bacterial and fungal organisms. The method was applied successfully with satisfactory results for the determination of FPC drug in fenoprofen capsules. The method was validated with respect to linearity, limit of detection and quantification, inter- and intra-days precision and accuracy. The proposed method gave comparable results with the official method. [ABSTRACT FROM AUTHOR]

The occurrence of pharmaceuticals used as non-steroidal anti-inflammatory drugs (NSAIDs) and analgesics in the aquatic environment is a threat to humans and aquatic species at large. The primary route of these pharmaceuticals to aquatic environment is through human waste such as urine and faeces. The application of molecularly imprinted polymers (MIPs) in the solid-phase extraction (SPE) of such pollutants from environmental and biological samples is important for the pre-concentration of compounds and selectivity of the analytical methods. To date, there are still limited commercial suppliers of MIPs. However, it is easy to synthesize such polymers via non-covalent imprinting approach using easily available and affordable reagents. Therefore, the applications of MIPs in the SPE of NSAIDs and analgesics from environmental and biological samples are reviewed. This is very important because despite the fact that review articles on applications of MIPs for organic compounds have been reported, very little has focussed on NSAIDs and analgesics which are the major studied pharmaceuticals in the environment and biological samples. The review also brings out important aspects of common reagents used including the template molecules during MIP synthesis. Application and future trends are also discussed. Gaps such as little use of environmental friendly reagents such as ionic liquids have been identified. Also, the lack of MIP applications to some compounds such as fenoprofen has been observed which is likely to be developed in the near future. [ABSTRACT FROM AUTHOR]

Background: Fenoprofen calcium dehydrate (FCD) is counted as a non-steroidal, anti-inflammatory, anti-arthritic drug. FCD is slightly water soluble. It is indicated for mild pain relief, where the suggested dosage is 200 mg orally every 4 to 6 h. Aim: Reduce dissolution efficiency, reach an extended therapeutic effect and reduce the frequency of the drug side effects. Method: Combination of the co-evaporated drug:triacetyl-β-cyclodextrin complex prepared in a ratio of 1:3 and either of two polymers--hydroxylpropylmethyl cellulose (HPMC) or ethyl cellulose (EC)--in the same formulation. In vitro dissolution studies were carried in simulated gastric (pH 1.2) and intestinal (pH 6.8) fluids, by using the USP dissolution tester (rotating paddle apparatus). The FCD in vitro release from EC/drug complex was markedly retarded. Interaction between fenoprofen, TA-β-CD, EC, HPMC in the solid state were confirmed by FT-IR, DSC, XRD and SEM. In vivo studies assessed the anti-inflammatory and analgesic activities and the results were compared with the market product Nalfosab® Capsules. Results: Remarkable inhibition of inflammation and nociception after 24 h was attained for EC/drug complex. Conclusions: EC/drug complex has a sustained effect due to high remaining amount after elapsing with remarkable inhibition of inflammation. [ABSTRACT FROM AUTHOR]

The efficiency of drug research and development has paradoxically declined over the last decades despite major scientific and technological advances, promoting new cost-effective strategies such as drug repositioning by systematic screening for new actions of known drugs. Here, we performed a screening for positive allosteric modulators (PAMs) at melanocortin (MC) receptors. The non-steroidal anti-inflammatory drug fenoprofen, but not the similar compound ibuprofen, presented PAM activity at MC, MC, and MC receptors. In a model of inflammatory arthritis, fenoprofen afforded potent inhibition while ibuprofen was nearly inactive. Fenoprofen presented anti-arthritic actions on cartilage integrity and synovitis, effects markedly attenuated in Mc3r−/− mice. Fenoprofen displayed pro-resolving properties promoting macrophage phagocytosis and efferocytosis, independently of cyclooxygenase inhibition. In conclusion, combining repositioning with advances in G-protein coupled receptor biology ( allosterism) may lead to potential new therapeutics. In addition, MC PAMs emerged as a viable approach to the development of innovative therapeutics for joint diseases. [ABSTRACT FROM AUTHOR]

The aim of this work was to evaluate the effect of fenoprofen on the labeling of blood constituents with technetium-99m, on the morphology of red blood cells and on the plasmid DNA. Blood samples from Wistar rats were incubated with fenoprofen and the assay of labeling of blood constituents with technetium-99m (99mTc) was performed. Blood cells, plasma, soluble and insoluble fractions of blood cells and plasma were separated. The radioactivity in each fraction was counted and percentage of incorporated radioactivity (%ATI) was determined. Blood smears were prepared, fixed, stained and the qualitative and quantitative morphology of the red blood cells (RBC) was evaluated. Plasmid (pBSK) was incubated with fenoprofen with stannous chloride, and agarose gel electrophoresis procedure was carried out to evaluate genotoxic and the protection of this drug against stannous chloride effect on DNA. In conclusion, under the conditions used in this work, our data suggest that fenoprofen would not (i) affect the fixation of the 99mTc on the blood constituents, (ii) alter the RBC membrane and (iii) present genotoxic and redox effects.O objetivo deste trabalho foi avaliar o efeito do fenoprofeno na marcação de constuintes sanguíneos com tecnécio-99m (99mTc), na morfologia de hemácias e no DNA plasmidial. Amostras de sangue de ratos Wistar foram incubadas com fenoprofeno e a marcação de constituintes sangüíneos com 99mTc foi realizada. Células sangüíneas (CS) e plasma (P) foram isolados. Alíquotas de CS e P foram precipitadas, frações insolúvel e solúvel foram separadas. A radioatividade em cada fração foi contada e o percentual de radioatividade incorporada (%ATI), determinada. Distensões sangüíneas foram preparadas, fixadas, coradas e análise morfológica, qualitativa e quantitativa, de hemácias foi realizada sob microscopia óptica. Plasmídios pBSK foram incubados com fenoprofeno na presença e ausência de cloreto estanoso, e o procedimento de eletroforese em gel de agarose realizado para avaliar o efeito genotóxico deste fármaco e seu efeito sobre a ação do cloreto estanoso no DNA. Os resultados obtidos sugerem que, nas condições utilizadas nesse estudo, o fenoprofeno não poderia: (i) afetar a fixação do 99mTc nos constituintes sanguíneos, (ii) alterar a membrana de hemácias e (iii) apresentar efeitos genotóxicos e redox.

Fenoprofen is a widely used nonsteroidal anti-inflammatory drug (NSAID) against rheumatoid arthritis, degenerative joint disease, ankylosing spondylitis and gout. Like other NSAIDs, fenoprofen inhibits the synthesis of prostaglandins by blocking both cyclooxygenase (COX) isoforms, COX-1 the "house-keeping" enzyme and COX-2 the induced isoform from pathological stimuli. Unselective inhibition of both COX isoforms results in many side effects, but off-target effects have also been reported. The steric modifications of the drugs could afford the desired COX-2 selectivity. Furthermore, NSAIDs have shown promising cytotoxic properties. The structural modification of fenoprofen using bulky dicarba-closo-dodecaborane(12) (carborane) clusters and the biological evaluation of the carborane analogues for COX inhibition and antitumor potential showed that the carborane analogues exhibit stronger antitumor potential compared to their respective aryl-based compounds., (© 2022 The Authors. ChemMedChem published by Wiley-VCH GmbH.)

Indisputable importance of drug solubility in various industrial perspectives has motivated the scientists to evaluate different techniques to improve it. Fenoprofen is a significant nonsteroidal anti-inflammatory drug (NSAID), that is the orally administered to relieve mild to moderate pain and the unfavorable symptoms of osteoarthritis and rheumatoid arthritis (i.e., inflammation and stiffness). Supercritical fluids (SCFs) belong to a certain type of fluids, in which their temperature and pressure are higher than the critical point. This property allows the CO 2 SCF to simultaneously possess the characteristics of both a liquid and a gas. The prominent target of this paper is to mathematically develop three predictive models via machine learning (ML) technique to optimize the solubility of Fenoprofen in CO 2 SCF. In this study, we have 32 data vectors in each dataset, including two input features of pressure and temperature. The output target is solubility, which we are going to model and analyze. Models are constructed through the use of Modular ANN (MANN), Gaussian processes regression (GPR), and the K-Nearest Neighbor technique (KNN) in this body of work. The glowworm swarm optimization (GSO) swarm-based method is utilized in order to carry out the process of model optimization. The root mean squared error (RMSE) rates for GSO-KNN, GSO-MANN, and GSO-GPR are respectively 5.25E-04, 5.46E-04, and 3.01E-05. The aforementioned models were also judged according to a number of other criteria, and since the GSO-GPR model was found to be the most effective according to all of these standards, it is being treated as the conclusive model of this investigation. In addition, the maximum error has been brought down to 5.02E-05 with the help of this model, which has an R2-score of 0.999. [ABSTRACT FROM AUTHOR]

The possibility of removing representative nonsteroidal anti-inflammatory drugs (NSAIDs) from water was tested using Octolig®, a commercially available material with polyethylenediimine moieties covalently attached to high-surface area silica gel. The effectiveness of removal should depend on selected NSAIDs having appropriate anionic functional groups. NSAIDs selected had aromatic carboxylic groups: diclofenac, fenoprofen, indomethacin, ketoprofen, mefenamic acid, naproxen, and sulindac. These substances in deionized (DI) water were removed by passage over Octolig columns with removal values approaching 90% at environmental pH values, e.g., ca pH 6. Fenoprofen, however, was only removed to an extent of 80% in DI water and 62% in well water, presumably a result of competition with bicarbonate ions. [ABSTRACT FROM PUBLISHER]