RESUMEN
The widespread occurence of pharmaceutical pollutants seriously threatens the environment and human well-being. In the present study, zinc ferrite nanoparticles (ZnFe2O4 NPs) have been synthesized by co-precipitation method and used as photocatalyst for the degradation of two most commonly prescribed painkillers, piroxicam (PXM) and paracetamol (PCM), via heterogeneous Fenton process under the solar light. The synthesized ZnFe2O4 NPs showed a narrower band gap i.e. 1.87 eV, signifying the ability to efficiently work in visible light range. In context of photocatalytic applications, the operational conditions were optimized to achieve maximum degradation. PCM and PXM were completely degraded (100%) at the optimized photocatalytic dose (20 mg L-1), reaction time (180 min), initial drug concentration (10 mg L-1), and pH (6.0), which is close to the natural environment. The extent of mineralization as estimated by the reduction of total organic carbon (TOC) was observed to be â¼91 and 82% for PCM and PXM respectively. Kinetic studies revealed that photocatalytic degradation followed pseudo-first-order kinetics. Moreover, the ZnFe2O4 NPs retained â¼90 % of photocatalytic activity after five consecutive reaction cycles, showing remarkable reusability and stability of catalyst.
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Acetaminofén , Peróxido de Hidrógeno , Piroxicam , Luz Solar , Contaminantes Químicos del Agua , Acetaminofén/química , Piroxicam/química , Catálisis , Contaminantes Químicos del Agua/química , Peróxido de Hidrógeno/química , Fotólisis , Hierro/química , Compuestos Férricos/química , Cinética , Zinc/químicaRESUMEN
Aim: This study focused on developing a topical gel incorporating lornoxicam-loaded poly(lactic-co-glycolic acid) and polyethylene glycol (PLGA-PEG) blend nanoparticles to mitigate gastrointestinal (GIT) side effects and enhance therapeutic efficacy. Materials & methods: Synthesized nanoparticles were subjected to in vitro characterization, ex vivo permeation studies, and acute oral toxicity analysis post-incorporation into the gel using a S/O/W double emulsion solvent. Results & conclusion: The nanoparticles displayed a smooth, spherical morphology (170-321 nm) with increased entrapment efficiency (96.2%). LOX exhibited a permeation rate of 70-94% from the nanoparticle-infused gel, demonstrating favorable biocompatibility at the cellular level. The formulated gel, enriched with nanoparticles, holds promising prospects for drug-delivery systems and promising improved therapeutic outcomes for LOX.
[Box: see text].
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Administración Cutánea , Nanopartículas , Piroxicam , Polietilenglicoles , Copolímero de Ácido Poliláctico-Ácido Poliglicólico , Piroxicam/análogos & derivados , Piroxicam/administración & dosificación , Piroxicam/química , Polietilenglicoles/química , Animales , Copolímero de Ácido Poliláctico-Ácido Poliglicólico/química , Nanopartículas/química , Humanos , Portadores de Fármacos/química , Tamaño de la Partícula , Inflamación/tratamiento farmacológico , Sistemas de Liberación de Medicamentos , Antiinflamatorios no Esteroideos/administración & dosificación , Antiinflamatorios no Esteroideos/química , Antiinflamatorios no Esteroideos/farmacología , Ratones , Ácido Láctico/química , Masculino , Ratas , Ácido Poliglicólico/química , Piel/metabolismo , Piel/efectos de los fármacosRESUMEN
Piroxicam (PX) is a nonsteroidal anti-inflammatory drug (NSAID) commonly associated with gastrointestinal (GI) injuries, including dyspepsia, heartburn, inflammation, bleeding, ulceration, and life-threatening perforation. The ß-cyclodextrin (ß-CD)-based PX formulation (PX@CD) has been shown to reduce gastric side effects by improving PX's solubility and dissolution rates. However, the solubility of PX can only be increased to a limited extent by ß-CD, due to the low binding constant between PX and ß-CD (â¼100 M-1). As a result, adverse reactions such as epigastric pain and pyrosis are still commonly reported. Cucurbit[7]uril (CB[7]) is a synthetic macrocyclic host compound that binds strongly to various drugs. In this study, we demonstrated that CB[7] forms complexes with PX in the gastric acid environment with a binding constant approximately 70 times higher than that between ß-CD and PX. The PX@CB[7] inclusion complexes exhibited rapid dissolution rates in the gastric environment. In addition, PX@CB[7] showed significantly higher oral bioavailability and maximum concentration (Cmax) compared to PX and PX@CD (1:2.5), resulting in improved anti-inflammatory effects in both mouse and rat models. Moreover, PX@CB[7] (1:2.5) had the least adhesion to the gastric mucosa and caused the mildest gastric side effects in rat models when compared to PX, PX@CD (1:2.5), and PX@CB[7] (1:1). Lastly, CB[7] demonstrated good oral biocompatibility in a subacute toxicity evaluation study. These findings indicate that CB[7] could be used as an excipient to improve treatment effectiveness and decrease adverse reactions in orally administered formulations with a favorable safety profile.
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Antiinflamatorios no Esteroideos , Disponibilidad Biológica , Hidrocarburos Aromáticos con Puentes , Imidazoles , Piroxicam , Solubilidad , beta-Ciclodextrinas , Animales , Piroxicam/administración & dosificación , Piroxicam/química , Piroxicam/farmacocinética , Piroxicam/efectos adversos , Imidazoles/química , Imidazoles/administración & dosificación , Imidazoles/farmacocinética , Imidazoles/efectos adversos , Hidrocarburos Aromáticos con Puentes/química , Hidrocarburos Aromáticos con Puentes/administración & dosificación , Hidrocarburos Aromáticos con Puentes/farmacocinética , Antiinflamatorios no Esteroideos/administración & dosificación , Antiinflamatorios no Esteroideos/química , Antiinflamatorios no Esteroideos/farmacocinética , Antiinflamatorios no Esteroideos/efectos adversos , beta-Ciclodextrinas/química , beta-Ciclodextrinas/administración & dosificación , Masculino , Ratones , Ratas Sprague-Dawley , Ratas , Liberación de Fármacos , Administración Oral , Compuestos Heterocíclicos con 2 Anillos , Compuestos Macrocíclicos , ImidazolidinasRESUMEN
OBJECTIVES: In this research paper, an investigation has been made to assess the simultaneous effect of a solubility enhancement approach, i.e., hydrotropy on the solubility and apparent permeability of piroxicam. The solubility of piroxicam (PRX) a BCS (biopharmaceutics classification system) class II drug has been increased using a mixed hydrotropy approach. This study is based on identifying the pattern of solubility-permeability interplay and confirming whether every solubility gain results in a concomitant decrease in permeability or permeability remains unaffected. METHOD: Solid dispersions of PRX were formulated using two hydrotropes, viz., sodium benzoate (SB) and piperazine (PP) by solvent evaporation method. A comprehensive 32factorial design was employed to study the effect of hydrotropes on the solubility and permeability of PRX. Subsequently, PRX tablets containing these solid dispersions were formulated and evaluated. KEY FINDINGS: SB and PP displayed a significant increase in the solubility of PRX ranging from 0.99 to 2.21 mg/mL for F1-F9 batches attributed to the synergistic effect of hydrotropes. However, there is a reduction in PRX permeability with increasing hydrotrope levels. The decline in permeability was notably less pronounced compared to the simultaneous rise in aqueous solubility of PRX. CONCLUSION: An evident tradeoff between permeability and solubility emerged through the mixed hydrotropic solubilization for PRX. As PRX has generally higher intrinsic permeability, it has been assumed that this permeability loss will not affect the overall absorption of PRX. However, it may affect the absorption of drugs with limited permeability. Therefore, solubility permeability interplay should be investigated during solubility enhancement.
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Permeabilidad , Piroxicam , Solubilidad , Piroxicam/química , Química Farmacéutica/métodos , Comprimidos , Excipientes/química , Solventes/químicaRESUMEN
This study introduces two innovative nanocarrier systems to improve oral drug delivery. Desosomes and desimicelles combine Deep eutectic solvent (DES) with vesicular or micellar nanosystems, respectively. These novel nanosystems integrate the DES solubilization potency for administering drugs with low aqueous solubility and the vesicular and micellar systems to bypass physiological barriers and improve poor drug bioavailability. Lornoxicam (LRX) is a BCS class II anti-inflammatory with limited aqueous solubility and rapid clearance. Desosomes and desimicelles were prepared and successfully optimized. The optimization depended on particle size, zetapotential, entrapment efficiency, and solubility. The optimized desosomes (LRX-DES-V) and desimicelles (LRX-DES-M) were pictured by transmission electron microscope. Differential scanning calorimetry (DSC) and FTIR analysis indicated the successful inclusion of LRX inside each system. Invitro LRX release profiles revealed controlled release of LRX-DES-V and LRX-DES-M, with more sustained release by the later one. In-vivo study, inflammation was induced using a carrageenan rat model, and the anti-inflammatory effect of LRX-pure, marketed product, traditional niosomes, LRX-DES-V & LRX-DES-M were determined using inhibition %, serum inflammatory cytokines, and histopathology. After 4 h of induction, LRX-DES-M (68.05%) showed a significant inhibition compared to LRX-DES-V (63.57%). LRX-DES-M also showed a better reduction in COX2, PGE2, and TNF-α (1.25-fold, 1.24-fold, and 1.36-fold inhibition), respectively, compared to LRX-DES-V. We can conclude that LRX-DES-V and LRX-DES-M showed better effects than all other groups and that LRX-DES-M might be more effective than LRX-DES-V.
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Micelas , Tamaño de la Partícula , Piroxicam , Solubilidad , Animales , Ratas , Administración Oral , Piroxicam/administración & dosificación , Piroxicam/farmacocinética , Piroxicam/análogos & derivados , Piroxicam/química , Masculino , Sistemas de Liberación de Medicamentos/métodos , Portadores de Fármacos/química , Disponibilidad Biológica , Liberación de Fármacos , Antiinflamatorios no Esteroideos/administración & dosificación , Antiinflamatorios no Esteroideos/farmacocinética , Antiinflamatorios no Esteroideos/farmacología , Antiinflamatorios no Esteroideos/química , Liposomas , Ratas Wistar , Nanopartículas/química , Solventes/química , Carragenina , Rastreo Diferencial de CalorimetríaRESUMEN
Introduction: The close relationship between inflammatory processes and epileptic seizures is already known, although the exact pathophysiological mechanism is unclear. In this study, the anticonvulsant capacity of piroxicam, an anti-inflammatory drug, was evaluated. A rat pentylenetetrazole kindling model was used.Methods: Male Wistar rats, 8-9 weeks old, received piroxicam (0.15 and 0.30 mg/kg), diazepam (2 mg/kg) or saline for 14 days, and PTZ, on alternate days. Intraperitoneal was chosen as the route of administration. The intensity of epileptic seizures was assessed using a modified Racine scale. The open field test and object recognition analysis were performed at the beginning of the study to ensure the safety of the drugs used. At the end of the protocol, the animals were euthanized to measure the levels of inflammatory (TNF-a and IL-6) and anti-inflammatory (IL-10) cytokines in the cortex, hippocampus, and serum.Results:There were no changes in the open field test and object recognition analysis. Piroxicam was found to decrease Racine scale scores at both concentrations. The reported values for IL-6 levels remained steady in all structures, whereas the TNF-alpha level in the cortex was higher in animals treated with piroxicam than in the saline and diazepam subjects. Finally, animals treated with the anti-inflammatory drug presented reduced IL-10 levels in the cortex and hippocampus.onclusions: Using inflammation as a guiding principle, the anticonvulsant effect of PIRO could be associated with the hippocampal circuits, since this structure showed no increase in inflammatory cytokines.
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Anticonvulsivantes , Modelos Animales de Enfermedad , Excitación Neurológica , Piroxicam , Ratas Wistar , Animales , Piroxicam/farmacología , Masculino , Excitación Neurológica/efectos de los fármacos , Anticonvulsivantes/farmacología , Ratas , Pentilenotetrazol , Convulsiones/tratamiento farmacológico , Citocinas/metabolismo , Diazepam/farmacología , Hipocampo/efectos de los fármacos , Hipocampo/metabolismo , Antiinflamatorios no Esteroideos/farmacología , Antiinflamatorios no Esteroideos/administración & dosificación , Relación Dosis-Respuesta a Droga , Epilepsia/tratamiento farmacológicoRESUMEN
OBJECTIVE: To describe the effect of different substance combinations administered through mesotherapy in dogs with hip osteoarthritis. ANIMALS: 104 dogs. METHODS: In this retrospective study, 4 groups (dogs treated with a combination of lidocaine, piroxicam, and thiocolchicoside [MG]; dogs treated with lidocaine, piroxicam, and Traumeel [TG]; dogs treated with lidocaine, piroxicam, and glucosamine [GG]; and dogs treated with the same combination as in MG combined with a photobiomodulation session [MPG]) were set. For all groups, the same treatment frequency was followed. Response to treatment was measured with the Canine Brief Pain Inventory (divided into pain interference score and pain severity score), Liverpool Osteoarthritis in Dogs (LOAD), and Canine Orthopedic Index (divided into function, gait, stiffness, and quality of life) before treatment and 15, 30, 60, 90, and 120 days after treatment. Cox proportional hazard regression analysis was used to investigate the influence of treatment, age, sex, body weight, breed, and Orthopedic Foundation for Animals score. RESULTS: Dogs had a mean age of 7.6 ± 3.1 years and body weight of 28.6 ± 5.5 kg. Hip osteoarthritis was classified as mild (4), moderate (70), or severe (30). Greater improvements were observed in MG and MPG. Kaplan-Meier estimators showed MG and MPG had longer periods with clinically significant results. Treatment was the covariable that contributed more frequently to the outcomes observed. CLINICAL RELEVANCE: The combination used in MG, particularly combined with photobiomodulation, produced longer-lasting clinically significant results.
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Enfermedades de los Perros , Mesoterapia , Piroxicam , Animales , Perros , Enfermedades de los Perros/tratamiento farmacológico , Enfermedades de los Perros/terapia , Estudios Retrospectivos , Masculino , Femenino , Piroxicam/uso terapéutico , Piroxicam/administración & dosificación , Piroxicam/análogos & derivados , Mesoterapia/veterinaria , Colchicina/uso terapéutico , Colchicina/administración & dosificación , Lidocaína/uso terapéutico , Lidocaína/administración & dosificación , Quimioterapia Combinada/veterinaria , Osteoartritis/veterinaria , Osteoartritis/tratamiento farmacológico , Glucosamina/uso terapéutico , Glucosamina/administración & dosificación , Extractos Vegetales/uso terapéutico , Extractos Vegetales/administración & dosificación , Osteoartritis de la Cadera/veterinaria , Osteoartritis de la Cadera/tratamiento farmacológico , Antiinflamatorios no Esteroideos/uso terapéutico , Antiinflamatorios no Esteroideos/administración & dosificación , Terapia por Luz de Baja Intensidad/veterinariaRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Opuntia monacantha belongs to the cactus family Cactaceae and is also known by cochineal prickly pear, Barbary fig or drooping prickly pear. It was traditionally used to treat pain and inflammation. O. monacantha cladodes showed pharmacological effects such as antioxidant potential owing to the presence of certain polysaccharides, flavonoids, and phenols. AIM OF THE STUDY: This research aimed to evaluate the anti-inflammatory as well as the anti-arthritic potential of ethanol extract of Opuntia monacantha (E-OM). MATERIALS AND METHODS: In vivo edema in rat paw was triggered by carrageenan and used to evaluate anti-inflammatory activity, while induction of arthritis by Complete Freund's Adjuvant (CFA) rat model was done to measure anti-arthritic potential. In silico studies of the previously High performance liquid chromatography (HPLC) characterized metabolites of ethanol extract was performed by using Discovery Studio 4.5 (Accelrys Inc., San Diego, CA, USA) within active pocket of glutaminase 1 (GLS1) (PDB code: 3VP1; 2.30 Å). RESULTS: EOM, particularly at 750 mg/kg, caused a reduction in the paw edema significantly and decreased arthritic score by 80.58% compared to the diseased group. It revealed significant results when histopathology of ankle joint was examined at 28th day as it reduced inflammation by 18.06%, bone erosion by 15.50%, and pannus formation by 24.65% with respect to the diseased group. It restored the altered blood parameters by 7.56%, 18.47%, and 3.37% for hemoglobin (Hb), white blood count (WBC), and platelets, respectively. It also reduced rheumatoid factor RF by 13.70% with concomitant amelioration in catalase (CAT) and superoxide dismutase (SOD) levels by 19%, and 34.16%, respectively, in comparison to the diseased group. It notably decreased mRNA expression levels of COX-2, IL-6, TNF-α, IL-1, NF-κß and augmented the levels of IL-4 and IL-10 in real time PCR with respect to the diseased group and piroxicam. HPLC analysis previously performed showed that phenolic acids and flavonoids are present in E-OM. Molecular docking studies displayed pronounced inhibitory potential of these compounds towards glutaminase 1 (GLS1), approaching and even exceeding piroxicam. CONCLUSIONS: Thus, Opuntia monacantha could be a promising agent to manage inflammation and arthritis and could be incorporated into pharmaceuticals.
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Artritis Experimental , Opuntia , Ratas , Animales , Citocinas/metabolismo , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Extractos Vegetales/análisis , Glutaminasa , Piroxicam/uso terapéutico , Simulación del Acoplamiento Molecular , Ratas Sprague-Dawley , Artritis Experimental/inducido químicamente , Artritis Experimental/tratamiento farmacológico , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Etanol/química , Inflamación/tratamiento farmacológico , Edema/inducido químicamente , Edema/tratamiento farmacológico , Edema/metabolismo , Flavonoides/uso terapéuticoRESUMEN
Overview of: Li RHW, Lo SST, Gemzell-Danielsson K, et al. Oral emergency contraception with levonorgestrel plus piroxicam: a randomised double-blind placebo-controlled trial [correction appears in Lancet 2023;402:850]. Lancet 2023;402:851-8.
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Anticoncepción Postcoital , Humanos , Levonorgestrel/uso terapéutico , Levonorgestrel/farmacología , Piroxicam , Método Doble CiegoRESUMEN
Four piroxicam metal complexes; NiL2 , PtL2 , PdL2 , and AgL were synthesized and characterized by different techniques with enhanced antibacterial and anticancer activity. Regarding in vitro antimicrobial activity, complex NiL2 displayed potent antibacterial effect against Escherichia coli and Pseudomonas aeruginosa that was 1.9-folds higher than piroxicam (minimum inhibitory concentration [MIC] = 31.85, 65.32 µM), respectively. In case of G+ve bacteria, complex PtL2 had potent activity on Staphylococcus aureus which was 2.1-folds higher than piroxicam (MIC = 43.12 µM), while activity of complex AgL against Enterococcus faecalis was threefolds higher than piroxicam (MIC = 74.57 µM. Complexes PtL2 and PdL2 exhibited higher inhibition of DNA gyrase than piroxicam (IC50 = 6.21 µM) in the range of 1.9-1.7-folds. The in vitro antiproliferative activity depicted that all investigated complexes showed better cytotoxic effect than piroxicam, specifically Pt and Pd complexes which had lower IC50 values than piroxicam on human liver cancer cell line HepG2 by 1.8 and 1.7-folds, respectively. While Pd and Ag complexes showed 2 and 1.6-folds better effect on human colon cancer cell line HT-29 compared with piroxicam. Molecular modeling studies including docking on Stranded DNA Duplex (1juu) and DNA gyrase enzyme (1kzn) that gave good insight about interaction of complexes with target molecules, calculation of electrostatic potential map and global reactivity descriptors were performed.
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Antineoplásicos , Complejos de Coordinación , Humanos , Piroxicam/farmacología , Complejos de Coordinación/farmacología , Girasa de ADN , Antibacterianos/farmacología , Antineoplásicos/farmacología , Pruebas de Sensibilidad Microbiana , Simulación del Acoplamiento MolecularRESUMEN
OBJECTIVE: To evaluate the analgaesic efficacy of tenoxicam and dexketoprofen in patients admitted to the Emergency Medicine (EM) Clinic with severe acute pain due to primary dysmenorrhea (PD). STUDY DESIGN: Randomised-controlled trial. Place and Duration of the Study: Emergency Medicine Clinic, Health Sciences University, Adana City Training and Research Hospital, Adana, Turkiye, from January to December 2022. METHODOLOGY: Patients presenting with PD, were divided into two groups of 60 each, administered 50 mg dexketoprofen and 20 mg tenoxicam intravenously. Visual analogue scale (VAS) scores were recorded at the 15th, 30th, 60th, and 120th minutes. VAS scores and ΔVAS scores were compared with the effectiveness of drugs, the need for rescue drugs and its side-effects. RESULTS: Intravenous (IV) dexketoprofen was administered to 60 of the patients and IV tenoxicam was administered to another 60. At the time of admission, mean VAS scores of the patients were 8.8 ± 0.9 for the dexketoprofen group and 8.6 ± 0.8 for the tenoxicam group. The VAS scores of the dexketoprofen group were found to be statistically significantly lower after 30 minutes with lower need for rescue analgaesics. ΔVAS scores of the dexketoprofen group were statistically significantly higher from the 30th minute. CONCLUSION: According to the VAS scoring, IV dexketoprofen was a more effective drug than IV tenoxicam in patients who were admitted to the EM clinic with severe pain due to PD. KEY WORDS: Dexketoprofen, Primary dysmenorrhea, VAS score.
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Dolor Agudo , Antiinflamatorios no Esteroideos , Cetoprofeno , Piroxicam , Trometamina , Femenino , Humanos , Dolor Agudo/tratamiento farmacológico , Antiinflamatorios no Esteroideos/uso terapéutico , Método Doble Ciego , Dismenorrea/tratamiento farmacológico , Cetoprofeno/análogos & derivados , Dolor Postoperatorio/tratamiento farmacológico , Piroxicam/análogos & derivadosRESUMEN
Due to tenoxicam (TX)'s poor aqueous solubility (0.072 mg/ml), it is poorly absorbable in the GIT, and the long-term oral administration of TX may cause severe GIT disturbances. Topical administration of TX can help in bypassing the GIT adverse effects. Therefore, in the present work, we constructed different pluronic/lecithin organogels (PLOs) for topical delivery of TX. PLO was constructed simply via direct mixing of an aqueous pluronic solution with lecithin solution. The prepared PLO formulations were characterized for their physicochemical properties including pH, drug content, visual inspection, viscosity, and spreadability. Also, the in vitro release and kinetic studies were carried out to investigate the mechanism of drug release. Moreover, the in vivo studies were carried out by investigating the anti-inflammatory and analgesic activities using albino male rats. The results showed that the modified PLOs have good physicochemical properties. The viscosity of the modified gels is a direct proportionality with both lecithin and pluronic concentrations. Also, subsequently, the drug release rate is directly proportional to gel viscosity. Moreover, the in vivo studies showed that the modified PLOs (F19) showed a significant ( < 0.05%) paw edema inhibition and pain analgesia compared with other investigated groups. Also, the results indicated that the increase in dose is accompanied by higher activity and a longer duration of action which extended to 12 h. Hence, the modified PLOs are promising safe candidates or vehicles for effective TX loading with sustained delivery behavior.
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Lecitinas , Piroxicam/análogos & derivados , Poloxámero , Animales , Ratas , Cinética , Inflamación , DolorRESUMEN
This study explored the antimicrobial effects of ketoprofen, piroxicam, and celecoxib alone or combined with calcium hydroxide (CH) against two strains of Enterococcus faecalis (E. faecalis) and assessed the influence of such combinations on the pH of CH. Minimum inhibitory concentrations (MICs) of the three tested NSAIDs were determined. Tested pastes were placed into wells punched in seeded agar plates and the bacterial inhibition zones were measured. Antibiofilm activity was assessed against 3 weeks of biofilm induced in bovine dentine blocks. The pH of the pastes was measured at four-time intervals. MIC values were 3.12, 25, and 25 mg/ml for ketoprofen, piroxicam, and celecoxib, respectively, and were similar for both bacterial strains except for celecoxib, which showed 8% growth at the highest tested concentration against vancomycin-resistant E. faecalis. Ketoprofen had the largest mean inhibition zone that was comparable to CH. None of the six tested pastes exhibited antibiofilm activity of a significant level in comparison to CH. A noticeable increase in the antibiofilm activity was found when 20% NSAIDs were added to CH while maintaining an alkaline pH. Ketoprofen was found to be the most effective among the tested NSAIDs. Although its effect was comparable to CH, adding ketoprofen at a ratio of 20% resulted in 50% higher antimicrobial action than CH alone. Accordingly, incorporating NSAIDs in inter-appointment dressing has the potential to utilize their anti-inflammatory, local analgesic, and antibacterial actions, which overcome the limitations of CH and improve the outcome of root canal treatment.
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Antiinflamatorios no Esteroideos , Biopelículas , Hidróxido de Calcio , Enterococcus faecalis , Pruebas de Sensibilidad Microbiana , Hidróxido de Calcio/farmacología , Enterococcus faecalis/efectos de los fármacos , Antiinflamatorios no Esteroideos/farmacología , Animales , Bovinos , Biopelículas/efectos de los fármacos , Técnicas In Vitro , Piroxicam/farmacología , Cetoprofeno/farmacología , Celecoxib/farmacología , Concentración de Iones de Hidrógeno , Irrigantes del Conducto Radicular/farmacologíaRESUMEN
Osteoarthritis is a bone and joint condition characterized pathologically by articular cartilage degenerative damage and can develop into a devastating and permanently disabling disorder. This investigation aimed to formulate the anti-inflammatory drug lornoxicam (LOR) into bile salt-enriched vesicles loaded in an in situ forming hydrogel as a potential local treatment of osteoarthritis. This was achieved by formulating LOR-loaded bilosomes that are also loaded with superparamagnetic iron oxide nanoparticles (SPIONs) for intra-muscular (IM) administration to improve joint targeting and localization by applying an external magnet to the joint. A 31.22 full factorial design was employed to develop the bilosomal dispersions and the optimized formula including SPION (LSB) was loaded into a thermosensitive hydrogel. Moreover, in vivo evaluation revealed that the IM administration of LSB combined with the application of an external magnet to the joint reversed carrageen-induced suppression in motor activity and osteoprotegerin by significantly reducing the elevations in mitogen-activated protein kinases, extracellular signal-regulated kinase, and receptor activator of nuclear factor kappa beta/osteoprotegerin expressions. In addition, the histopathological evaluation of knee joint tissues showed a remarkable improvement in the injured joint tissues. The results proved that the developed LSB could be a promising IM drug delivery system for osteoarthritis management.
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Hidrogeles , Osteoartritis , Piroxicam , Animales , Osteoartritis/tratamiento farmacológico , Hidrogeles/administración & dosificación , Hidrogeles/química , Piroxicam/administración & dosificación , Piroxicam/análogos & derivados , Piroxicam/farmacocinética , Masculino , Ligando RANK/metabolismo , Ratas , Nanopartículas Magnéticas de Óxido de Hierro/química , Nanopartículas Magnéticas de Óxido de Hierro/administración & dosificación , Antiinflamatorios no Esteroideos/administración & dosificación , Antiinflamatorios no Esteroideos/química , Modelos Animales de Enfermedad , Liposomas , Ratas Wistar , Sistemas de Liberación de MedicamentosRESUMEN
OBJECTIVE: The objective of this study was to evaluate the effectiveness of preoperative analgesics on inferior alveolar nerve blocks (IANB) during root canal treatment in patients with symptomatic irreversible pulpitis of the mandibular molars. METHODS: This study was a randomized, double-blinded, superiority trial with a parallel study design. A total of 120 subjects with symptomatic irreversible pulpitis were randomly assigned to one of four groups: group A (con- trol, Vitamin E, Evion 400 mg), group B (Diclofenac sodium, Voltral SR100 100 mg), group C (Piroxicam, Feldene 20 mg), and group D (Tramadol, Tramal 50 mg). The patients recorded preoperative pain levels, and after admin- istration of local anaesthesia intraoperative pain levels using the Heft-Parker visual analogue scale before and after the oral administration of the analgesics. Statistical analysis was performed using the Kruskal-Wallis test. RESULTS: All the analgesic groups showed a significant effect on the efficacy of the inferior alveolar nerve block in contrast to the control group (p<0.05). However, no significant difference was found between the drug groups on the effectiveness of the inferior alveolar nerve block (p>0.05). No side effects were reported in the present study. CONCLUSION: Preoperative analgesics significantly increase the effectiveness of inferior alveolar nerve block in patients with symptomatic irreversible pulpitis. Therefore, preoperative analgesics should be considered to increase the effectiveness of inferior alveolar nerve block in patients with symptomatic irreversible pulpitis on the mandibular molars. (EEJ-2023-02-033).
Asunto(s)
Bloqueo Nervioso , Pulpitis , Tramadol , Humanos , Pulpitis/tratamiento farmacológico , Pulpitis/cirugía , Nervio Mandibular , Analgésicos/uso terapéutico , Analgésicos/farmacología , Tramadol/farmacología , Tramadol/uso terapéutico , Piroxicam/farmacología , Piroxicam/uso terapéutico , Dolor/tratamiento farmacológico , Dolor/cirugíaRESUMEN
The study investigated the effects of different processed products of Polygonati Rhizoma(black bean-processed Polygonati Rhizoma, BBPR; stewed Polygonati Rhizoma, SPR) on the urinary metabolites in a rat model of Alzheimer's disease(AD). Sixty SPF-grade male SD rats were randomized into a control group, a model group, a donepezil group, a BBPR group, and a SPR group, with twelve rats in each group. Other groups except the control group were administrated with D-galactose injection(100 mg·kg~(-1)) once a day for seven weeks. The control group was administrated with an equal volume of normal saline once a day for seven consecutive weeks. After three weeks of D-galactose injection, bilateral hippocampal Aß_(25-35) injections were performed for modeling. The rats were administrated with corresponding drugs(10 mL·kg~(-1)) by gavage since week 2, and the rats in the model and control group with an equal volume of double distilled water once a day for 35 continuous days. The memory behaviour and pathological changes in the hippocampal tissue were observed. The untargeted metabolites in the urine were detected by ultra-high-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry(UPLC-Q/TOF-MS). Principal component analysis(PCA) and orthogonal partial least square-discriminant analysis(OPLS-DA) were employed to characterize and screen differential metabolites and potential biomarkers, for which the metabolic pathway enrichment analysis was conducted. The results indicated that BBPR and SPR increased the new object recognition index, shortened the escape latency, and increased the times of crossing the platform of AD rats in the Morris water maze test. The results of hematoxylin-eosin(HE) staining showed that the cells in the hippocampal tissue of the drug administration groups were closely arranged. Moreover, the drugs reduced the content of interleukin-6(IL-6, P<0.01) and tumor necrosis factor-α(TNF-α) in the hippocampal tissue, which were more obvious in the BBPR group(P<0.05). After screening, 15 potential biomarkers were identified, involving two metabolic pathways: dicoumarol pathway and piroxicam pathway. BBPR and SPR may alleviate AD by regulating the metabolism of dicoumarol and piroxicam.
Asunto(s)
Enfermedad de Alzheimer , Ratas , Masculino , Animales , Enfermedad de Alzheimer/tratamiento farmacológico , Cromatografía Líquida de Alta Presión/métodos , Ratas Sprague-Dawley , Dicumarol , Galactosa , Piroxicam , Metabolómica/métodos , Biomarcadores/orinaRESUMEN
Este trabajo se fundamenta en la evaluación de la actividad antiinflamatoria de extractos de sofrito de tomate, así como de compuestos estándares de la dieta mediterránea, usando un modelo experimental optimizado basado en larvas de pez cebra. La migración de neutrófilos en larvas de pez cebra de 96 horas post fertilización se indujo mediante una lesión y se potenció añadiéndole lipopolisacárido, dicha migración se visualizó y cuantificó mediante análisis de imagen. El efecto antiinflamatorio del extracto de tomate y de los compuestos utilizados fue correlacionado porcentualmente por la disminución de la migración de los neutrófilos. Los resultados muestran que el extracto de tomate presentó una reducción en la migración de neutrófilos de 40 % respecto al grupo control. Por otra parte, el ácido clorogénico y la cianidina presentes en el sofrito de tomate utilizados como estándares presentaron una disminución de la migración de neutrófilos de un 66,7 % y 62,5 % respectivamente. Estos porcentajes son comparables a los resultados observados en ensayos con drogas antiinflamatorias como la indometacina y piroxicam. Los resultados muestran que el extracto de sofrito de tomate presenta posible actividad antinflamatoria demostrada por la reducción de la migración de neutrófilos, además el modelo se mostró sensible y válido para ser aplicado en matrices alimentarias complejas(AU)
The main of this study was to evaluate the anti-inflammatory activity of tomato sofrito extracts, as well as standard compounds present in the Mediterranean diet, using an optimized experimental model based on zebrafish larvae. Neutrophil migration in zebrafish larvae 96 hours post fertilization was induced by a cut in the caudal fin and enhanced by adding lipopolysaccharide and was visualized and quantified by image analysis. The anti-inflammatory effect of tomato extract and the compounds used was correlated by the percentage decrease in the migration of neutrophils. The results showed that, tomato extract showed a reduction in neutrophil migration of 40% compared to the control group. Moreover, chlorogenic acid and cyanidin present in tomato sofrito sauce showed a decrease in neutrophil migration of 66.7% and 62.5% respectively. These percentages are comparable to the results observed in trials with anti-inflammatory drugs such as indomethacin and piroxicam. The results show that tomato sofrito extract has possible anti-inflammatory activity demonstrated by the reduction of neutrophil migration, furthermore the model was sensitive and valid to be applied in complex food matrices(AU)
Asunto(s)
Antiinflamatorios no Esteroideos , Solanum lycopersicum , Dieta Mediterránea , Antiinflamatorios , Neutrófilos , Pez Cebra , Carotenoides , Piroxicam , IndometacinaRESUMEN
Abstract This clinical trial evaluated the effect of preemptive use of the non-steroidal anti-inflammatory drug piroxicam in a single dose 30 min prior to in-office bleaching on the prevention of tooth sensitivity (TS) reported by patients. Fifty patients were submitted to two sessions of in-office tooth bleaching with 35% hydrogen peroxide used for 2 sessions, each consisting of a single 45-min application, with an interval of 7 days between session. Thirty minutes prior to the procedure, the patient randomly received a single dose of piroxicam (200 mg) or placebo in a double-blind, randomized, crossover design. The TS was evaluated using verbal rate (VRS) and visual analog (VAS) scales during the bleaching procedure and at 24 h after each session. The color changes were assessed by the Vita Bleachedguide scale 1 week after each bleaching session. Risk of TS was calculated from the VRS and analyzed by the McNemar test, while the level of TS was analyzed by the Mann-Whitney test. For the VAS, t-tests were used to compare data from the treatments at each assessment time. Data regarding color changes were subjected to Wilcoxon and Mann-Whitney tests (α=0.05). The preemptive administration of piroxicam did not affect the risk and level of TS compared to placebo, irrespective of the assessment time. The treatment sequence did not affect bleaching effectiveness. In conclusion, the administration of a single dose of piroxicam prior to in-office tooth bleaching was unable to significantly reduce the risk and level of TS.
Resumo Este ensaio clínico avaliou o efeito do uso preemptivo do anti-inflamatório não-esteroidal piroxicam em dose única 30 minutos antes do clareamento de consultório na prevenção de sensibilidade dentária (SD) relatada pelos pacientes. Cinquenta pacientes foram submetidos a duas sessões de clareamento dental em consultório com peróxido de hidrogênio a 35% por 2 sessões, consistindo de aplicação única de 45 minutos, com um intervalo de 7 dias entres as sessões. Trinta minutos antes do procedimento, o paciente recebia aleatoriamente dose única de piroxicam (200 mg) ou do placebo em um desenho duplo-cego, randomizado e cruzado. A SD foi avaliada usando a escalas de gradação verbal (EGV) e visual analógica (EVA) durante o procedimento clareador e 24h após o procedimento. As mudanças de cor foram avaliadas usando a escala Vita Bleachedguide uma semana após cada sessão de clareamento. O risco de SD foi calculado a partir de EGV a analisado pelo teste de McNemar, enquanto o nível de SD foi analisada pelo teste de Mann-Whitney. Para EVA, testes T foram usados para comparar dados dos tratamentos em cada tempo de avaliação. Dados de mudança de cor foram submetidos aos testes de Wilcoxon e Mann-Whitney (α=0.05). A administração preemptiva de piroxicam não afetou o risco e nível de SD quando comparado ao placebo, independentemente do tempo de avaliação. A sequencia de tratamento não afetou a efetividade do clareamento. Como conclusão, a administração de dose única de piroxicam previamente ao clareamento dental de consultório não foi efetiva em reduzir significantemente o risco e nível de SD.