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Local forms of non-steroidal anti-inflammatory drugs (NSAIDs) are characterized by a high safety profile due to low systemic absorption. They do not increase the risk of developing class-specific gastrointestinal, cardiovascular and kidney adverse events (AEs), which makes it possible to prescribe them even in severe comorbid pathology, which is typical for patients with osteoarthritis (OA).Objective: to evaluate the efficacy and safety of Artoxan gel (tenoxicam) 1% in comparison with Diclofenac gel 1% in patients with knee OA in a prospective comparative randomized trial.Material and methods. The study included 60 patients with Kellgren–Lawrence stages II–III knee OA, aged 41 to 78 years. The patients were randomly divided into two groups: the 1st group received Artoxan gel 1%, 5 cm 2 times a day for 14 days; 2nd – Diclofenac gel 1% according to the same scheme. During therapy, we assessed pain using a visual analog scale, the WOMAC index, quality of life using the EQ-5D questionnaire, satisfaction with therapy, and time to effect.Results and discussion. It has been demonstrated that local forms of NSAIDs have a positive effect on all clinical manifestations of OA: effectively reduce pain, stiffness, improve the functional state of the joints and quality of life. They also have a good safety profile and a fast symptomatic response. Comparison of the two groups showed that in patients receiving the local form of tenoxicam, there was a tendency to a more rapid and pronounced analgesic effect.Conclusion. The results of the study confirm the good efficacy and safety of local forms of NSAIDs.

Abstract Background Temporomandibular joint osteoarthritis (TMJ-OA) is a degenerative disease and manifests itself with pain and limitation of movement in the jaws. Arthrocentesis alone or in combination with intraarticular injections is one of the most commonly used treatment methods in these patients. The aim of the study is to examine the effectiveness of arthrocentesis plus tenoxicam injection and to compare it with arthrocentesis alone in patients with TMJ-OA. Methods Thirty patients with TMJ-OA who were treated randomly with either arthrocentesis plus tenoxicam injection (TX group) or arthrocentesis alone (control group) were examined. Maximum mouth opening (MMO), visual analog scale (VAS) pain values, and joint sounds were the outcome variables, which were evaluated at pre-treatment and at 1, 4, 12, and 24 weeks after treatment. Statistical significance was set at p

This study presents a new dual drug delivery system (DDDS) of poly(lactic acid) (PLA) with different morphologies (spheres and fibers). One approach for delivering Norfloxacin-Tenoxicam (NOR-TENO) drugs based on PLA microspheres was prepared by encapsulating TENO into PLA via emulsion-evaporation method to form TENO/microspheres then NOR was then adsorbed onto the surface of these microspheres by loading process. Another approach was designed by integrating a mixture of NOR-TENO drugs into the PLA matrix, then through the electrospinning process; NOR-TENO/electrospun fibers were fabricated. The microspheres and electrospun fibers had been characterized through FTIR, XRD, and SEM. Release behaviors of NOR-TENO were determined at pH (5.4, 6.7 and 7.4), where the release of the two drugs was faster in the two systems at pH 7.4. Antimicrobial activity of NOR-TENO/microspheres and NOR-TENO/electrospun fibers against S. aureus, B. cereus, and E. coli bacteria was examined in vitro, and NOR-TENO/electrospun fibers have better potential in killing bacteria. In vitro cytotoxicity assay of NOR-TENO/microspheres against HepG2, MCF-7, and HCT116 tumor cells were tested, and NOR-TENO/microspheres was highly cytotoxic to MCF-7 cells (IC50 = 21.87 μg・ml–1) with the lowest cytotoxic effect on WI-38 normal cells (the half maximal inhibitory concentration IC50 = 58.12 μg・ml–1). In vivo study of DMBA-induced breast cancer in rats had been accomplished for NOR-TENO/microspheres, which offer promising results in breast cancer treatment.

Purpose of the study – to study the efficacy and safety of tenoxicam (Texared®) in patients with active axial spondyloarthritis.Material and methods. The study included 35 patients with active axial spondyloarthritis with BASDAI≥4.0. Patients were given continuous oral tenoxicam (Texared®, Dr. Reddy’s Laboratories) at a dosage of 20 mg/day. Subsequently, 5 patients were excluded from the study due to discontinuation of the drug after 5–10 days of administration. 30 patients were included in the final analysis. Initially and after 30 days, to assess the severity of pain and stiffness, activity, patients filled out questionnaires in electronic form using Google forms, a general assessment of pain in the lower back and the intensity of night pain by the patient, subjective sleep characteristics were carried out. The doctor calculated the BASDAI, ASDAS-CRP, BASMI indices, and evaluated the activity according to the doctor’s opinion. The baseline blood pressure level was determined, and a patient diary was issued for ambulatory blood pressure measurement in the morning/evening for 30 days. After 30 days, the patient’s ambulatory blood pressure control was assessed. At baseline and after 30 days, biochemical blood parameters were studied, including a complete blood and urine test.Results and conclusion. In patients with axial spondyloarthritis with high and very high activity, a positive effect of tenoxicam (Texared®) therapy on disease activity was noted. The effect of Texared® develops with regular use already during the first 2 weeks, and after 4 weeks there is a clear decrease in the severity of pain in the lower back, a decrease in the duration of morning stiffness. The drug is well tolerated, has a favorable safety profile, no serious adverse events and few side effects that do not require discontinuation of therapy.

Tenoxicam, a selective cyclooxygenase (COX)-2 inhibitor, has potent analgesic and anti-inflammatory effects and is frequently used for out-of-hospital pain control. Even though other non-steroidal anti-inflammatory drugs were incriminated in Stevens–Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN) appearance, the literature is scarce regarding this agent. We report a case of tenoxicam-induced toxic epidermal necrolysis, detailing the multidisciplinary approach in a patient presenting skin detachment of 90% of the total body surface area, with concomitant ocular, oral, nasal, and vaginal mucosae involvement. A skin biopsy confirmed the diagnosis. The immediate cessation of the incriminated drug and rapid initiation of systemic steroids, along with topical therapies, and isolation into a specific environmental condition to limit skin infection were the cornerstones of therapeutic management. The patient was discharged with skin hyperpigmentation area and mild anxiety as long-term sequels. This report emphasized that severe or complicated cases should be transferred to a specialized burn center to reduce mortality risk and long-term morbidity.

The search for effective systems to facilitate the release of poorly bioavailable drugs is a forefront topic for the pharmaceutical market. Materials constituted by inorganic matrices and drugs represent one of the latest research strategies in the development of new drug alternatives. Our aim was to obtain hybrid nanocomposites of Tenoxicam, an insoluble nonsteroidal anti-inflammatory drug, with both layered double hydroxides (LDHs) and hydroxyapatite (HAP). The physicochemical characterization on the base of X-ray powder diffraction, SEM/EDS, DSC and FT-IR measurements was useful to verify the possible hybrids formation. In both cases, the hybrids formed, but it seemed that the drug intercalation in LDH was low and, in fact, the hybrid was not effective in improving the pharmacokinetic properties of the drug alone. On the contrary, the HAP–Tenoxicam hybrid, compared to the drug alone and to a simple physical mixture, showed an excellent improvement in wettability and solubility and a very significant increase in the release rate in all the tested biorelevant fluids. It delivers the entire daily dose of 20 mg in about 10 min.

The solution mixture of the non-steroidal anti-inflammatory drugs ketoprofen, meloxicam and tenoxicam was degraded through systems, composed of different photocatalysts based on TiO2 (Fe and Cu) and the hydrogen peroxide oxidant. The monitoring was performed by UV-Vis spectroscopy. Under sunlight radiation, a reduction in peaks was observed with the use of impregnated photocatalysts. After 60 min, the sun/H2O2/Fe-TiO2 system reached degradations of 46.5% and 93.2% at 260 and 367 nm, respectively, and was selected for further studies. The degradation kinetic reached 92 and 96% of degradation after 180 min, for the λ of 260 and 367 nm, respectively. The kinetic curve could be represented by the empirical model proposed by Nichela and co-authors, indicating that besides the heterogeneous photocatalysis that occurs at the surface of the TiO2 there is also the joint effect of the photo-Fenton process. After the treatment, there was no toxicity to cress and lettuce seeds. However, a sensitivity of the thyme seeds to the compounds formed during the treatment was verified. After the fifth treatment cycle, the supported photocatalyst showed degradation higher than 82%. These results indicate that this system is suitable for the treatment of effluents containing pharmaceutical compounds.

Transdermal delivery of non-steroidal anti-inflammatory drugs (NSAIDs) is an effective route of drug administration, as it directs the drug to the inflamed site with reduced incidence of systemic adverse effects such as gastric hemorrhage and ulcers. Tenoxicam (TNX) is a member of NSAIDs that are marketed only as oral tablets due to very poor absorption through the skin. The current study intended to formulate and characterize a hydrogel loaded with nanostructured lipid carriers (NLCs) to enhance the transdermal delivery of TNX. Six formulations of TNX were formulated by slight modifications of high shear homogenization and ultrasonication method. The selected formula was characterized for their particle size, polydispersity index (PDI), zeta potential, entrapment efficiency (EE), in-vitro drug release and ex-vivo skin permeation studies. Moreover, the effectiveness of the developed formula was studied in-vivo using carrageenan-induced paw edema and hyperalgesia model in irradiated rats. Formula F4 was chosen from six formulations, as the average diameter was 679.4 ± 51.3 nm, PDI value of about 0.02, zeta potential of −4.24 mV, EE of 92.36%, globules nanoparticles without aggregations and absence of interactions in the developed formula. Additionally, the in-vivo study showed the efficacy of formula F4 (TNX-NLCs hydrogel) equivalent to oral TNX in reducing the exaggerated inflammatory response induced by carrageenan after irradiation. In conclusion, the present findings suggest that TNX-NLCs hydrogel could be a potential transdermal drug delivery system alternative to the oral formulation for the treatment of various inflammatory conditions.

Tenoxicam (TNX) is a new non-steroidal anti-inflammatory drug that shows a superior anti-inflammatory effect and has the advantages of a long half-life period, a fast onset of action, a small dose, complete metabolism, and good tolerance. Some compounds often have tautomerism, and different tautomers exist in different crystalline forms. TNX is such a compound and has three tautomers. TNX always exists as the zwitterionic form in cocrystals. When the salt is formed, TNX exists in the enol form, which exhibits two conformations depending on whether a proton is gained or lost. Currently, the crystal structure of the keto form is not in the Cambridge Structural Database (CSD). Based on the analysis of existing crystal structures, we derived a simple rule for what form of TNX exists according to the pKa value of the cocrystal coformer (CCF) and carried out validation tests using three CCFs with different pKa values, including p-aminosalicylic acid (PAS), 3,5-dinitrobenzoic acid (DNB), and 2,6-dihydroxybenzoic acid (DHB). The molecular surface electrostatic potential (MEPS) was combined with the pKa rule to predict the interaction sites. Finally, two new cocrystals (TNX-PAS and TNX-DNB) and one salt (TNX-DHB) of TNX were obtained as expected. The differences between the cocrystals and salt were distinguished by X-ray diffraction, vibration spectra, thermal analysis, and dissolution measurements. To further understand the intermolecular interactions in these cocrystals and salt, the lattice energy and energy decomposition analysis (EDA) were used to explain them from the perspective of energy. The results suggest that the melting point of the CCF determines that of the cocrystal or salt, the solubility of the CCF itself plays an important role, and the improvement of the solubility after salt formation is not necessarily better than that of API or its cocrystals.

Polymorphism is a relatively common phenomenon among pharmaceutical compounds, and one of the main aspects to be considered in the production and development of medications. The investigation of polymorphism associated with oxicams, a group belonging to the class of non-steroidal anti-inflammatory drugs (NSAIDs) has increased in recent years and, in the case of tenoxicam, the existence of four polymorphic forms is reported in the literature. The objective of this study was to characterize the presence of different polymorphic forms of tenoxicam in active pharmaceutical ingredient and oral pharmaceutical formulations, as well as to evaluate the influence on in vitro dissolution. The characterization of the three samples of pharmaceutical ingredient of tenoxicam from different suppliers by X-Ray Diffraction (XRD), Infrared (IR) and dissolution profile indicated the presence of a form III crystalline structure, without presenting significant differences between the in vitro dissolution profiles analyzed, and a Dissolution Efficiency (DE%) of 60.30%, 60.70% and 72.34%, respectively. When the four pharmaceutical specialties of tenoxicam were submitted to XRD analysis, they also presented form III crystalline structures. Despite this, the formulations presented different dissolution profiles and a DE% of 75.23%, 83.69%, 78.19% and 90.63%, respectively, without compromising their quality. However, often polymorphism affects physico-chemical properties of drugs, showing the importance of studying this phenomenon, by correlating the presence of crystalline structures to alterations in the quality of active ingredients and pharmaceutical products.

Nonsteroidal anti-inflammatory drugs (NSAIDs) are one of the most important therapeutic agents used for the treatment of a variety of inflammation. Tenoxicam (TNX), which is used to relieve inflammation, swelling, and pain associated with rheumatoid arthritis, is a member of NSAIDs. In this study, copper(II), zinc(II), platinum(II) and palladium(II) complexes of TNX were synthesized and characterized by analytical and instrumental techniques (Ultraviolet and visible absorption spectra (UV–Vis), Liquid chromatography–mass spectrometry (LC-MS), Inductively coupled plasma - optical emission spectrometry (ICP-OES), Differential thermal analysis-Thermogravimetric analysis (DTA-TG)). Fourier-transform infrared (FT-IR) spectra of the complexes were measured and the outcome were supported by density functional theory computations. The proposed structure of these metal complexes are [Cu(TNX)2], [Zn(TNX)2], [Pt(TNX)2] and [Pd(TNX)Cl2]. The anti-inflammatory activities of the synthesized complexes, compared with the drug, were demonstrated for the first time. All metal complexes of the TNX acted more efficiently on the reduction of pro-inflammatory tumor necrosis factor (TNF)-alpha production than that of TNX. The highest anti-inflammatory potential was detected with [Cu(TNX)2]. The receptor-ligand interactions between TNX complexes and TNF-α were revealed by molecular docking calculations.

Aim: The objective of this study is comparing the effects of intra-articular hyaluronic acid (HA) and tenoxicam aplications on joint range of motion (ROM) and pain in patients with gonarthrosis.Patients and Method: This study was designed as prospective, non-randomized controlled, and single-blinded trial. 60 patients diagnosed with Grade II and Grade III osteoarthritis (OA) according to the American College of Rheumatology (ACR) criteria were consecutively enrolled. Patients were divided into two groups whereby the first group received intra-articular HA three times a week and the other group received a single dose intra-articular tenoxicam. Pre-treatment and after-treatment VAS and ROM values of the groups were compared.Results: In the HA Group, 20 patients (66.6%) were female, 10 patients (33.3%) were male and the mean age of them was 59.6 years (range 45-75 years). In the Tenoxicam Group, 24 patients (80%) were female, 6 (20%) patients were male, and the average age of this group was 61.5 years (range 45-75 years). VAS scores knee flexion and extension ROM values on the 1st day, the 15th day, the 1st month,the2nd month, and the 3rd month after the treatment, significantly improved in both groups (p 0.05). Conclusion: It was seen that intra-articular HA and tenoxicam administration seem to be effective and reliable methods in Grade 2-3 knee OA patients; but tenoxicam was more effective in reducing pain and relieving joint movements compared to HA injection in the early periods.

The first-line treatment of osteoarthritis is based on anti-inflammatory drugs, the most currently used being nonsteroidal anti-inflammatory drugs, selective cyclooxygenase 2 (COX-2) inhibitors and corticoids. Most of them present cytotoxicity and low bioavailability in physiological conditions, making necessary the administration of high drug concentrations causing several side effects. The goal of this work was to encapsulate three hydrophobic anti-inflammatory drugs of different natures (celecoxib, tenoxicam and dexamethasone) into core-shell terpolymer nanoparticles with potential applications in osteoarthritis. Nanoparticles presented hydrodynamic diameters between 110 and 130 nm and almost neutral surface charges (between −1 and −5 mV). Encapsulation efficiencies were highly dependent on the loaded drug and its water solubility, having higher values for celecoxib (39–72%) followed by tenoxicam (20–24%) and dexamethasone (14–26%). Nanoencapsulation reduced celecoxib and dexamethasone cytotoxicity in human articular chondrocytes and murine RAW264.7 macrophages. Moreover, the three loaded systems did not show cytotoxic effects in a wide range of concentrations. Celecoxib and dexamethasone-loaded nanoparticles reduced the release of different inflammatory mediators (NO, TNF-α, IL-1β, IL-6, PGE2 and IL-10) by lipopolysaccharide (LPS)-stimulated RAW264.7. Tenoxicam-loaded nanoparticles reduced NO and PGE2 production, although an overexpression of IL-1β, IL-6 and IL-10 was observed. Finally, all nanoparticles proved to be biocompatible in a subcutaneous injection model in rats. These findings suggest that these loaded nanoparticles could be suitable candidates for the treatment of inflammatory processes associated with osteoarthritis due to their demonstrated in vitro activity as regulators of inflammatory mediator production.

ABSTRACTBACKGROUND AND OBJECTIVES:Tenoxicam is widely used in osteoarthritis treatment and we aimedto compare the effectivity of oral and intra-articular administration of tenoxicam in osteoarthri-tis treatment.METHODS: This study was performed between 2011 and 2012 by retrospectively analyzing andcomparing the findings of 60 patients who were clinically and radiologically diagnosed with kneedegenerative osteoarthritis in Bünyan state hospital pain policlinic. 60 patients included in thestudy were divided into two groups. The first group (tenoxicam IA, n = 30) included patientfindings of those subjected to intra-articular injection of 20 mg tenoxicam to the knee oncea week for three weeks and the second group (oral tenoxicam, n = 30) included patients whowere administered 20 mg oral tenoxicam once a day for three weeks. All patients were clini-cally evaluated pre-treatment and in the 1st week, 1st month and 3rd month post-treatmentaccording to specified criteria.RESULTS AND CONCLUSIONS: Twenty two of 60 patients included in the study were male and 38were female. In both groups significant improvements were detected in all of the observedparameters: visual analog scale, Western Ontario McMaster Osteoarthritis Index (pain, physicalactivity, knee stiffness) and Lequesne index scores and in the evaluations performed in 1st week,1st month and 3rd month with respect to pre-treatment values. Besides, a better complianceto treatment and gastrointestinal system tolerability in tenoxicam IA group was also observed.Intra-articular tenoxicam administration could be thought as an alternative treatment methodin patients with knee osteoarthritis who cannot use oral tenoxicam especially due to systemicgastrointestinal system side effects and those who have difficulties in adapting to treatment.

OBJETIVO: Analisar os efeitos do tenoxicam, um antiinflamatório não hormonal, na cicatrização da parede abdominal de ratos. MÉTODOS: Foram utilizados 40 ratos adultos, submetidos à laparotomia mediana e distribuídos, aleatoriamente, em um grupo controle (C), constituído de 20 animais que receberam solução de NaCl a 0,9 %; e um grupo tratado (T), constituído de 20 animais que receberam o tenoxicam. Os animais de cada grupo foram divididos, conforme a data de sacrifício, em subgrupos de 10 animais, denominados C7, C14, T7 e T14. As inscrições 7 e 14 determinaram o sacrifício dos animais no sétimo e décimo quarto dia pós-operatório, respectivamente. As soluções de tenoxicam (1mg/ml) e de NaCl a 0,9% foram administradas no pós-operatório imediato e nos quatro dias seguintes, por via intramuscular, na dose volume de 0,6 ml/kg/dia. No dia do sacrifício, realizou-se a ressecção de dois fragmentos da parede abdominal (1cm x 3cm), que foram utilizados para determinação da concentração de hidroxiprolina e avaliação da força de ruptura. RESULTADOS: Não foram observadas complicações da ferida operatória, incluindo infecção ou deiscência, nos quatro subgrupos de animais. Na análise comparativa dos quatro subgrupos de animais, não foi evidenciada diferença estatisticamente significante no estudo da força de ruptura (p=0,262) e na concentração de hidroxiprolina (p=0,392). CONCLUSÃO: A administração de tenoxicam, por via intramuscular, não interfere na cicatrização da parede abdominal de ratos.

The treatment of pain before it initiates may prevent the persistent pain-induced changes in the central nervous system that amplify pain long after the initial stimulus. The effects of pre- or postoperative intraperitoneal administration of morphine (2 to 8 mg/kg), dipyrone (40 and 80 mg/kg), diclofenac (2 to 8 mg/kg), ketoprofen (10 and 20 mg/kg), and tenoxicam (10 and 20 mg/kg) were studied in a rat model of post-incisional pain. Groups of 5 to 8 male Wistar rats (140-160 g) were used to test each drug dose. An incision was made on the plantar surface of a hind paw and the changes in the withdrawal threshold to mechanical stimulation were evaluated with Von Frey filaments at 1, 2, 6 and 24 h after the surgery. Tenoxicam was given 12 or 6 h preoperatively, whereas the remaining drugs were given 2 h or 30 min preoperatively. Postoperative drugs were all given 5 min after surgery. No drug abolished allodynia when injected before or after surgery, but thresholds were significantly higher than in control during up to 2 h following ketoprofen, 6 h following diclofenac, and 24 h following morphine, dipyrone or tenoxicam when drugs were injected postoperatively. Significant differences between pre- and postoperative treatments were obtained only with ketoprofen administered 30 min before surgery. Preoperative (2 h) intraplantar, but not intrathecal, ketoprofen reduced the post-incisional pain for up to 24 h after surgery. It is concluded that stimuli generated in the inflamed tissue, rather than changes in the central nervous system are relevant for the persistence of pain in the model of post-incisional pain.