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1.
J Orthop Res ; 2024 Sep 22.
Artigo em Inglês | MEDLINE | ID: mdl-39306710

RESUMO

Co-administration of mirogabalin besylate and nonsteroidal anti-inflammatory drugs is effective for neuropathic pain; however, mechanism of its action remains unknown. We aimed to evaluate the mechanism of this synergistic effect of the concomitant administration for neuropathic pain using chronic constriction injury model rats. Fifty male Wister rats of 7-week-old were used. Right sciatic nerve ligation was performed in 40 rats and they were sub-divided into four groups: vehicle, mirogabalin, diclofenac sodium and co-administration of them. Ten rats underwent sham surgery. Fluorogold was attached to sciatic nerve during surgery. Von Frey filament and weight bearing tests were performed on postoperative Day 6 as behavioral assessments and drug was administrated intraperitoneally. Half rats in each group underwent behavioral assessment and perfusion fixation using 4% paraformaldehyde on postoperative Day 7 and remaining on postoperative Day 14. Subsequently, dorsal root ganglion at L4 to L6 was collected and examined immunohistochemistry for calcitonin gene-related peptide, and their immunoreactivity in fluorogold-labeled neurons was measured. Spinal cord at lumbar swelling was resected, immunostained for ionized-calcium-binding adapter molecule-1 and glial fibrillary acidic protein, and immunoreactive neurons in dorsal horn of spinal cords were calculated as the occupancy of them. Mirogabalin suppresses the neuropeptide-release from presynaptic afferent neuron directly and it resulted in suppressing glia cells activation. Diclofenac sodium inhibits cyclooxygenase-2 and prostaglandin production, related to allodynia. These effects of mirogabalin and diclofenac sodium, respectively, inhibited glia cells strongly, which is presumed to be one of the mechanisms for the effectiveness of their co-administration for neuropathic pain.

2.
Int J Biol Macromol ; : 135901, 2024 Sep 21.
Artigo em Inglês | MEDLINE | ID: mdl-39313047

RESUMO

This investigation focuses on the extraction, characterization, and evaluation of taro (Colocasia esculenta) stolon polysaccharide (TSP) as a tablet binding agent, which is obtained from edible taro stolon. TSP was subjected to phytochemical screening and characterized by FTIR, DSC, TGA, DTA, XRD, particle size, polydispersity index, zeta potential, rheological behavior, and SEM. The tablets prepared with varying concentrations of TSP (2.5 %, 5 %, 7.5 %, and 10 % w/w) and diclofenac sodium (DS) were evaluated and compared with the same concentrations of gum acacia and PVP K-30. The presence of carbohydrates was confirmed by Molisch's test. The FTIR spectra established the compatibility of the drug with excipients. The SEM images revealed asymmetric and elongated particles of TSP powder. The hydration kinetics study showed matrix hydration and water penetration velocity within the range of 0.602-0.753 g/g and 0.112-0.189 cm/g.h, respectively. The tablets showed drug release of >75 % at 45 min. The release-exponent value above 0.89 indicated a super case II drug transport combining matrix erosion and diffusion. Optimum tablet hardness and very low friability, even at 2.5 % binder concentration, suggested the potential application of the novel TSP as a tablet binder in the formulation of the tablets.

3.
Cureus ; 16(8): e66386, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-39246923

RESUMO

Endoscopic cholangiopancreatography (ERCP) is a widely used diagnostic and therapeutic tool for pancreaticobiliary conditions. One of its major complications is pancreatitis. This study aims to understand the incidence of post-ERCP pancreatitis after using rectal diclofenac and Indomethacin as prophylactic measures. We retrieved 2870 articles from the PubMed, ScienceDirect, and Google Scholar databases. Using the Medical Subject Headings (MeSH) strategy in PubMed, we chose research articles published in the last five years. Exclusion criteria included paid full-text articles, abstracts, letters to editors, patients not undergoing ERCP, ages more than 45 years, animal studies, and non-English studies. The 2020 Preferred Reporting Items for Systematic Reviews and Meta-Analysis (PRISMA) criteria were used in the design of our systematic reviews. It was found that the medical world is still debating whether rectal diclofenac and Indomethacin are beneficial in avoiding post-ERCP pancreatitis (PEP). Rectal diclofenac is used. Although its effectiveness is debated due to mixed findings and concerns about certain outcomes, it is also considered beneficial in specific circumstances, such as before ERCP. Studies on rectal Indomethacin also yield contradictory results; while some emphasize the drug's large reduction in PEP incidence, especially in low-risk people, others question its efficacy. We need further studies to clarify the remaining uncertainties.

4.
Int J Biol Macromol ; 278(Pt 3): 134871, 2024 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-39173807

RESUMO

Pharmaceuticals and personal care products and dyes have low biodegradability and high toxicity, seriously threaten the human health and ecological environment. Therefore, seeking effective removal methods has become the focus of research. In this study, silver-based metal-organic framework (Ag-MOF) and chitosan (CS) hybrid adsorbent (Ag-MOF-CS) was synthesized via solvothermal one-pot synthesis to remove diclofenac sodium (DCF) and acid Red 1 (AR1) from water for the first time. The morphology and structure of Ag-MOF-CS were confirmed by various characterizations. The effect on adsorption was investigated by changing the adsorbent dosage, pH and other conditions. The adsorption kinetics, adsorption isotherms and thermodynamics were analyzed. Ag-MOF-CS showed a high adsorption capacity. And the maximum adsorption capacity of Ag-MOF-CS for DCF and AR1 was 351.75 mg/g and 678.83 mg/g, respectively. The adsorbent bound to DCF and AR1 may via electrostatic forces, π-π interactions, hydrogen bonding. Even after four cycles of Ag-MOF-CS, the DCF removal can still be higher than 80 %. The eco-friendly Ag-MOF-CS demonstrated significant potential for utilization in treating wastewater.


Assuntos
Quitosana , Corantes , Diclofenaco , Estruturas Metalorgânicas , Prata , Poluentes Químicos da Água , Purificação da Água , Quitosana/química , Estruturas Metalorgânicas/química , Prata/química , Poluentes Químicos da Água/química , Poluentes Químicos da Água/isolamento & purificação , Adsorção , Cinética , Corantes/química , Corantes/isolamento & purificação , Diclofenaco/química , Purificação da Água/métodos , Concentração de Íons de Hidrogênio , Termodinâmica
5.
Pharmaceuticals (Basel) ; 17(7)2024 Jul 12.
Artigo em Inglês | MEDLINE | ID: mdl-39065784

RESUMO

In recent years, solid dosage forms have gained interest in pediatric therapy because they can provide valuable benefits in terms of dose accuracy and stability. Particularly for orodispersible films (ODFs), the literature evidences increased acceptability and dose flexibility. Among the various available technologies for obtaining ODFs, such as solvent casting, hot-melt extrusion, and ink printing technologies, the solvent-free preparation methods exhibit significant advantages. This study investigated Vacuum Compression Molding (VCM) as a solvent-free manufacturing method for the preparation of flexible-dose pediatric orodispersible films. The experimental approach focused on selecting the appropriate plasticizer and ratios of the active pharmaceutical ingredient, diclofenac sodium, followed by the study of their impacts on the mechanical properties, disintegration time, and drug release profile of the ODFs. Additional investigations were performed to obtain insights regarding the solid-state properties. The ODFs obtained by VCM displayed adequate quality in terms of their critical characteristics. Therefore, this proof-of-concept study shows how VCM could be utilized as a standalone method for the production of small-scale ODFs, enabling the customization of doses to meet the individual needs of pediatric patients.

6.
SLAS Technol ; 29(5): 100170, 2024 Jul 25.
Artigo em Inglês | MEDLINE | ID: mdl-39067817

RESUMO

In this work, an automated dissolution system (dissoBOT) was used for dissolution testing for the first time. Carry-over (CO) of the dissoBOT was determined for paracetamol (PA) and diclofenac sodium (DS), which are active pharmaceutical ingredients (APIs). Initially, partial method validation of the UV-VIS spectrophotometry method for PA and DS determination was performed by defining the limit of detection (LOD), the limit of quantification (LOQ), linear concentration range, accuracy, and precision. The LODs and LOQs were less than 0.01 mg/L for both APIs. The determined linear concentration ranges were from 1.00 mg/L to 30.00 mg/L for PA and from 0.50 mg/L to 3.50 mg/L for DS (the square of the correlation coefficient was greater than 0.9990, and the quality coefficient was less than 1.00 % for both APIs). The accuracy of the method was evaluated by calculating the recovery (Re) of the solutions of standards with known concentrations. The method for both APIs was deemed to be accurate (the average Re for PA and DS were 99.81 % and 101.43 %, respectively). Precision was evaluated by calculating the relative standard deviation (RSD). The method for PA and DS was deemed to be precise, as the RSD value for PA was 0.13 %, and for DS was 0.38 %. The volume (V) of the washing medium in both cleaning cycles performed by the dissoBOT system, as well as the medium dispensing V, were established, where the medium dispensing V was in accordance with the United States Pharmacopeia requirements. The CO of the dissoBOT system, using tap water as the washing medium, was determined to be less than 1.00 % for both APIs. The CO values for one cleaning cycle of the sampling station with a V of 2 mL was in the range of 1.24-1.54 %, for V of 5 mL was in the range of 0.78-0.93 %, and for V of 10 mL was in the range of 0.27-0.36 %. In addition, the CO of the dissoBOT, when employing two cleaning cycles of the sampling station (each V of 10 mL) was reduced (CO <0.20 %). Finally, the dissoBOT was successfully employed for the dissolution PA and DS tables.

7.
ACS Infect Dis ; 10(8): 2860-2869, 2024 Aug 09.
Artigo em Inglês | MEDLINE | ID: mdl-39073350

RESUMO

The continuous rise of multidrug-resistant (MDR) Gram-negative bacteria poses a severe threat to public health worldwide. Colistin(COL), employed as the last-line antibiotic against MDR pathogens, is now at risk due to the emergence of colistin-resistant (COL-R) bacteria, potentially leading to adverse patient outcomes. In this study, synergistic activity was observed when colistin and diclofenac sodium (DS) were combined and used against clinical COL-R strains of Escherichia coli (E. coli), Klebsiella pneumoniae (K. pneumoniae), Acinetobacter baumannii (A. baumannii), and Pseudomonas aeruginosa (P. aeruginosa) both in vitro and in vivo. The checkerboard method and time-killing assay showed that DS, when combined with COL, exhibited enhanced antibacterial activity compared to DS and COL monotherapies. Crystal violet staining and scanning electron microscopy showed that COL-DS inhibited biofilm formation compared with monotherapy. The in vivo experiment showed that the combination of DS and COL reduced bacterial loads in infected mouse thighs. Synergistic activity was observed when COL and DS were use in combination against clinical COL-R strains of E. coli, K. pneumoniae, A. baumannii and P. aeruginosa both in vitro and in vivo. The synergistic antibacterial effect of the COL-DS combination has been confirmed by performing various in vitro and in vivo experiments, which provides a new treatment strategy for infections caused by MDR bacteria.


Assuntos
Antibacterianos , Colistina , Diclofenaco , Sinergismo Farmacológico , Bactérias Gram-Negativas , Testes de Sensibilidade Microbiana , Colistina/farmacologia , Animais , Antibacterianos/farmacologia , Diclofenaco/farmacologia , Camundongos , Bactérias Gram-Negativas/efeitos dos fármacos , Biofilmes/efeitos dos fármacos , Farmacorresistência Bacteriana Múltipla , Acinetobacter baumannii/efeitos dos fármacos , Pseudomonas aeruginosa/efeitos dos fármacos , Infecções por Bactérias Gram-Negativas/tratamento farmacológico , Infecções por Bactérias Gram-Negativas/microbiologia , Klebsiella pneumoniae/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Humanos , Quimioterapia Combinada , Feminino
8.
Int J Toxicol ; 43(5): 491-502, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38901831

RESUMO

These toxicity studies aimed to assess the safety and tolerability of a novel intravenous diclofenac sodium (37.5 mg/mL) formulation containing povidone K12 (80 mg/mL) as the key excipient in Wistar rats. This formulation was tested at doses of 3, 7, and 15 mg/kg/day and was administered daily for 28 days by intravenous route. Toxicokinetic estimation revealed a dose-proportional increase in plasma exposure to diclofenac. The formulation was well tolerated in males; however, mortality was observed in females (2/15) at the highest dose (15 mg/kg/day). Adverse gastrointestinal events related to NSAIDS and a few other treatment-related effects on clinical and anatomic pathology were noted at the 15 mg/kg/day dose, which normalized at the end of the 2-week recovery period. In addition, the excipient povidone K12 was present in a higher amount than the approved Inactive Ingredient Database (IID) limit in the proposed novel formulation. It was qualified through a separate 28-day repeated dose toxicity study by intravenous route in Wistar rats. Povidone K12 was found to be well tolerated and safe up to a dose of 165 mg/kg/day. No treatment-related adverse effects were observed in this study. In conclusion, repeated administration of a novel intravenous formulation containing diclofenac sodium was found to be safe up to the dose of 7 mg/kg/day in female rats and 15 mg/kg/day in male rats.


Assuntos
Anti-Inflamatórios não Esteroides , Diclofenaco , Ratos Wistar , Animais , Diclofenaco/toxicidade , Diclofenaco/farmacocinética , Diclofenaco/administração & dosagem , Masculino , Feminino , Anti-Inflamatórios não Esteroides/toxicidade , Anti-Inflamatórios não Esteroides/administração & dosagem , Anti-Inflamatórios não Esteroides/farmacocinética , Ratos , Excipientes/toxicidade , Excipientes/farmacocinética , Excipientes/química , Povidona/toxicidade , Povidona/química , Povidona/farmacocinética , Administração Intravenosa , Relação Dose-Resposta a Droga , Injeções Intravenosas
9.
Heliyon ; 10(11): e31425, 2024 Jun 15.
Artigo em Inglês | MEDLINE | ID: mdl-38828354

RESUMO

The current work suggests a new, ultrasensitive green functionalized sensor for the determination of anti-inflammatory medication diclofenac sodium (DCF). Alumina (Al2O3) and cerium oxide (CeO2) nanoparticles (NPs) have attracted great interest for their use as outstanding and electroactive nanocomposite in potentiometric and sensory research due to their ultrafunctional potential. The formed nanoparticles have been confirmed using various spectroscopic and microscopic techniques. The fennel extract-mediated Al2O3/CeO2 nanocomposite (Al2O3/CeO2 NCS) modified coated wire membrane sensor developed in this study was used to quantify DCF in bulk and commercial products. Diclofenac sodium was coupled with phosphomolybdic acid (PMA) to generate diclofenac phosphomolybdate (DCF-PM) as an active ion-pair in the existence of polyvinyl chloride (PVC) and o-nitrophenyl octyl ether (o-NPOE). Clear peaks at 270, and 303 nm with band gaps of 4.59 eV and 4.09 eV were measured using UV-vis spectroscopy of Al2O3 and CeO2, respectively. The crystallite sizes of the formed nanoparticles were XRD-determined to be 30.13 ± 8, 17.72 ± 3, and 35.8 ± 0.5 nm for Al2O3, CeO2, and Al2O3/CeO2 NCS, respectively. The developed sensor showed excellent response for the measurement and assay of DCF, with a linearity between 1.0 × 10-9 and 1.0 × 10-2 mol L-1. EmV = (57.76) log [DCF] +622.69 was derived. On the other hand, the typical type DCF-PM presented a potentiometric response range of 1.0 × 10-5-1.0 × 10-2 mol L-1 and a regression equation of EmV = (56.97) log [DCF]+367.16. The functionalized sensor that was proposed was successful in determining DCF in its commercial tablets with percent recovery 99.95 ± 0.3. Method validation has been used to improve the suitability of the suggested potentiometric technique, by studying various parameters with respect to the international council harmonization requirements for analytical methodologies.

10.
ACS Appl Mater Interfaces ; 16(23): 29876-29890, 2024 Jun 12.
Artigo em Inglês | MEDLINE | ID: mdl-38829728

RESUMO

A novel therapeutic approach combining acupuncture and diclofenac sodium (DS) administration was established for the potential treatment for rheumatoid arthritis (RA). DS is a commonly used anti-inflammatory and analgesic drug but has short duration and adverse effects. Acupoints are critical linkages in the meridian system and are potential candidates for drug delivery. Herein, we fabricated a DS-loaded multilayer-modified acupuncture needle (DS-MMAN) and investigated its capacity for inhibiting RA. This DS-MMAN possesses sustained release properties and in vitro anti-inflammatory effects. Experimental results showed that the DS-MMAN with microdoses can enhance analgesia and efficiently relieve joint swelling compared to the oral or intra-articular administration of DS with gram-level doses. Moreover, the combination of acupoint and DS exerts a synergistic improvement in inflammation and joint damage. Cytokine and T cell analyses in the serum indicated that the application of DS-MMAN suppressed the levels of pro-inflammatory factors and increased the levels of anti-inflammatory factors. Furthermore, the acupoint administration via DS-MMAN could decrease the accumulation of DS in the liver and kidneys, which may express better therapeutic efficiency and low toxicity. The present study demonstrated that the acupuncture needle has the potential to build a bridge between acupuncture and medication, which would be a promising alternative to the combination of traditional and modern medicine.


Assuntos
Terapia por Acupuntura , Artrite Reumatoide , Diclofenaco , Agulhas , Diclofenaco/administração & dosagem , Diclofenaco/farmacologia , Diclofenaco/química , Artrite Reumatoide/terapia , Artrite Reumatoide/tratamento farmacológico , Animais , Camundongos , Masculino , Sistemas de Liberação de Medicamentos/instrumentação , Humanos , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/farmacologia , Anti-Inflamatórios não Esteroides/administração & dosagem , Ratos
11.
Arch Microbiol ; 206(7): 289, 2024 Jun 07.
Artigo em Inglês | MEDLINE | ID: mdl-38847838

RESUMO

Staphylococcus epidermidis is an opportunistic pathogen commonly implicated in medical device-related infections. Its propensity to form biofilms not only leads to chronic infections but also exacerbates the issue of antibiotic resistance, necessitating high-dose antimicrobial treatments. In this study, we explored the use of diclofenac sodium, a non-steroidal anti-inflammatory drug, as an anti-biofilm agent against S. epidermidis. In this study, crystal violet staining and confocal laser scanning microscope analysis showed that diclofenac sodium, at subinhibitory concentration (0.4 mM), significantly inhibited biofilm formation in both methicillin-susceptible and methicillin-resistant S. epidermidis isolates. MTT assays demonstrated that 0.4 mM diclofenac sodium reduced the metabolic activity of biofilms by 25.21-49.01% compared to untreated controls. Additionally, the treatment of diclofenac sodium resulted in a significant decrease (56.01-65.67%) in initial bacterial adhesion, a crucial early phase of biofilm development. Notably, diclofenac sodium decreased the production of polysaccharide intercellular adhesin (PIA), a key component of the S. epidermidis biofilm matrix, in a dose-dependent manner. Real-time quantitative PCR analysis revealed that diclofenac sodium treatment downregulated biofilm-associated genes icaA, fnbA, and sigB and upregulated negative regulatory genes icaR and luxS, providing potential mechanistic insights. These findings indicate that diclofenac sodium inhibits S. epidermidis biofilm formation by affecting initial bacterial adhesion and the PIA synthesis. This underscores the potential of diclofenac sodium as a supplementary antimicrobial agent in combating staphylococcal biofilm-associated infections.


Assuntos
Antibacterianos , Biofilmes , Diclofenaco , Staphylococcus epidermidis , Biofilmes/efeitos dos fármacos , Staphylococcus epidermidis/efeitos dos fármacos , Staphylococcus epidermidis/fisiologia , Diclofenaco/farmacologia , Antibacterianos/farmacologia , Testes de Sensibilidade Microbiana , Anti-Inflamatórios não Esteroides/farmacologia , Aderência Bacteriana/efeitos dos fármacos , Humanos , Polissacarídeos Bacterianos/metabolismo , Proteínas de Bactérias/genética , Proteínas de Bactérias/metabolismo , Infecções Estafilocócicas/microbiologia , Infecções Estafilocócicas/tratamento farmacológico , Regulação Bacteriana da Expressão Gênica/efeitos dos fármacos
12.
Int J Phytoremediation ; 26(11): 1847-1853, 2024 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-38794784

RESUMO

This study explored the efficacy of activated carbon derived from rice straw and treated with ZnCl2 (ZnCl2-RS) for the removal of diclofenac sodium (DCF) and paracetamol (PCM) through an adsorption process. The investigation included examining the variations in removal efficiency at different pH levels and ZnCl2-RS doses. The characteristics of the ZnCl2-RS, prepared for the study, were determined through SEM and FTIR analyses, revealing a composition of 49.4% carbon and 8.3% zinc. At pH 5, the adsorption efficiency for DCF and PCM was enhanced, achieving removal rates of 92.2% for DCF and 89.1% for PCM with 0.2 g of ZnCl2-RS. The adsorption of DCF and PCM by ZnCl2-RS followed pseudo-second-order kinetic and adhered to the Langmuir isotherm model. The maximum adsorption capacities were calculated as 26.04 mg/g for DCF and 19.05 mg/g for PCM. In conclusion, the cost-effective production of activated carbon from agricultural waste like rice straw yielded a promising adsorbent material for efficiently removing pharmaceuticals such as diclofenac sodium and paracetamol. This approach not only contributes to waste reduction but also promotes the repurposing of agricultural waste materials.


This study is about the preparation of rice straw, which is produced as agricultural waste, by ZnCl2 activation and the usability of the prepared adsorbent material in the purification of drugs used as analgesics such as diclofenac sodium and paracetamol. Although there are studies on the use of activated carbon produced from rice straw in the removal of pollutants such as dye, studies on drug removal are quite limited.


Assuntos
Acetaminofen , Carvão Vegetal , Cloretos , Diclofenaco , Oryza , Poluentes Químicos da Água , Compostos de Zinco , Oryza/química , Adsorção , Carvão Vegetal/química , Biodegradação Ambiental , Cinética , Concentração de Íons de Hidrogênio
13.
Basic Clin Pharmacol Toxicol ; 135(2): 173-179, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-38803141

RESUMO

INTRODUCTION: To investigate the in vitro effect of diclofenac on tubal smooth muscle as an alternative to hyoscine-N-butyl bromide, which is used for premedication before hysterosalpingography (HSG). MATERIAL AND METHODS: Fallopian tubes were retrieved from seven healthy women after bilateral tubal ligation and in vitro contractility and histological studies were conducted using tissue bath and immunohistochemistry. RESULTS: Diclofenac sodium and hyoscine-N-butyl bromide did not significantly change the basal mean tension; however, they decreased the contractions induced by potassium chloride (KCl). The relaxant effect of diclofenac sodium and hyoscine-N-butyl bromide was not statistically significantly different. The presence of cyclooxygenase (COX)-2 enzyme in the fallopian tube was demonstrated by immunohistochemical studies. CONCLUSIONS: The in vitro relaxant effect of diclofenac sodium on the fallopian tube is similar to hyoscine-N-butyl bromide. Diclofenac may have the potential to be used as an alternative to hyoscine-N-butyl bromide in premedication in HSG.


Assuntos
Brometo de Butilescopolamônio , Ciclo-Oxigenase 2 , Diclofenaco , Tubas Uterinas , Humanos , Diclofenaco/farmacologia , Feminino , Brometo de Butilescopolamônio/farmacologia , Tubas Uterinas/efeitos dos fármacos , Tubas Uterinas/metabolismo , Adulto , Ciclo-Oxigenase 2/metabolismo , Músculo Liso/efeitos dos fármacos , Histerossalpingografia , Técnicas In Vitro , Cloreto de Potássio/farmacologia , Contração Muscular/efeitos dos fármacos , Anti-Inflamatórios não Esteroides/farmacologia
14.
Int J Biol Macromol ; 271(Pt 1): 132606, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38788875

RESUMO

The present investigation was aimed to fabricate and optimize extended-release beads of diclofenac sodium based on an ion-cross-linked matrix of pectin (PTN) and taro (Colocasia esculenta) stolon polysaccharide (TSP) with 23 full factorial design. Total polysaccharide concentration (TPC), polysaccharide ratio (PR), and cross-linker concentration ([CaCl2]) were taken as independent factors with two levels of each. Initially, TSP was extracted, purified, and characterized. Fourier-transform infrared spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC) showed drug-polymer compatibility. The study also revealed the significant positive effect of TSP on drug entrapment efficiency (DEE) and sustaining drug release. The response variables (DEE, cumulative % drug-release at 1, 2, 4, 6, and 10 h, release-constant, time for 50 % and 90 % drug release (T50%, T90%), release-similarity factor (f2), and difference factor (f1) were analyzed, and subsequently, independent fabrication variables were numerically optimized by Design-Expert software (Version-13; Stat-Ease Inc., Minneapolis). The optimized batch exhibited appreciable DEE of 88.5 % (± 2.2) and an extended-release profile with significantly higher T50%, T90%, and release-similarity factor (f2) of 4.7 h, 11.4 h, and 71.6, respectively. Therefore, the study exhibited successful incorporation of the novel TSP as a potential alternative adjunct polysaccharide in the pectin-based ion-cross-linked inter-penetrating polymeric network for extended drug release.


Assuntos
Colocasia , Preparações de Ação Retardada , Diclofenaco , Liberação Controlada de Fármacos , Pectinas , Diclofenaco/química , Pectinas/química , Colocasia/química , Portadores de Fármacos/química , Polissacarídeos/química , Cálcio/química , Microesferas , Espectroscopia de Infravermelho com Transformada de Fourier
15.
Int J Biol Macromol ; 271(Pt 1): 132637, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38795565

RESUMO

Metal-organic frameworks are emerging inorganic-organic hybrid materials that can be self-assembled from metal ions and organic ligands via coordination bonds. These materials possess large specific surface area, tunable pore structure, abundant active center, diversity of functional groups as well as high mechanical and thermal stability which promote their applications in adsorption and catalysis studies. In this study, NH2-MIL-53(Al/Zr) was prepared and embedded into sodium alginate gel spheres (NH2-MIL-53(Al/Zr)-SA) and its adsorption properties towards TC and DCF in solution were investigated. According to XRD and FTIR analysis, the structure of the raw material was not changed after making the gel spheres. The maximum adsorption towards TC (pH =3) and DCF (pH =5) reached 98.5 mg·g-1 and 192 mg·g-1, respectively. The process was consistent with Langmuir and Freundlich, suggesting that there was both monolayer and multilayer adsorption which infers the presence of physical adsorption (intra-particle diffusion) and non-homogeneous chemical adsorption. The thermodynamic parameters showed that the adsorption process was a spontaneous entropy increasing reaction. The regeneration rate of spent NH2-MIL-53(Al/Zr)-SA could still reach 99.1 % after three cycles, indicating good regeneration performance. This study can provide a basis for the application of NH2-MIL-53(Al/Zr)-SA in wastewater treatment.


Assuntos
Alginatos , Diclofenaco , Géis , Estruturas Metalorgânicas , Tetraciclina , Alginatos/química , Adsorção , Diclofenaco/química , Estruturas Metalorgânicas/química , Tetraciclina/química , Géis/química , Poluentes Químicos da Água/química , Termodinâmica , Purificação da Água/métodos , Cinética , Concentração de Íons de Hidrogênio , Zircônio/química
16.
Environ Pollut ; 351: 124077, 2024 Jun 15.
Artigo em Inglês | MEDLINE | ID: mdl-38705447

RESUMO

In this paper, the S-scheme/Schottky heterojunction photocatalyst (CuInS2/Bi/Bi2MoO6, CIS/Bi/BMO) was successfully constructed via a facile in-situ solvothermal method, aimed at enhancing its photocatalytic performance. The results of the study on the photocatalytic degradation of diclofenac sodium (DCF) under simulated solar light irradiation revealed that the as-prepared composite exhibited remarkable catalytic efficiency in comparison to the pristine Bi2MoO6 and CuInS2. The plasmonic bismuth (Bi) was formed during the solvothermal process. Subsequently, CuInS2 and Bi were grown on the surface of Bi2MoO6 leading to forming CIS/BMO S-scheme heterojunction, along with a Schottky junction between Bi and Bi2MoO6. The use of ethylene glycol as a support was the main reason for the significant improvement in photocatalytic efficiency in the degradation of DCF. Moreover, the probable photocatalytic mechanisms for the degradation of DCF had been proposed based on the active species quenching experiments. The eleven degradation products were detected by HPLC-MS, and the degradation reaction pathway of DCF was deduced. Additionally, the CIS/Bi/BMO photocatalyst exhibited a consistently high removal rate after four cycles. This study proposes a new strategy for designing efficient S-scheme/Schottky heterojunction photocatalysts for solar energy conversion.


Assuntos
Bismuto , Cobre , Diclofenaco , Fotólise , Bismuto/química , Diclofenaco/química , Catálise , Cobre/química , Poluentes Químicos da Água/química , Molibdênio/química , Índio/química , Processos Fotoquímicos
17.
Int J Pharm ; 659: 124276, 2024 Jun 25.
Artigo em Inglês | MEDLINE | ID: mdl-38821436

RESUMO

Neuropathic pain is chronic pain caused by a lesion or disease of the somatosensory nervous system. Neuropathic pain, with a high incidence and complex pathogenesis, is one of the most significant areas of clinical medicine and basic research. Currently, prescribed treatments are still unsatisfactory or have limited effectiveness. A medicinal preparation is required that relieves the neuropathic pain and prolongs action time, which has not yet been discovered. In this study, MIL-101 (Fe) was employed as a drug carrier to regulate the release of diclofenac sodium, thereby achieving the effect of analgesia and sustained release. The release curves demonstrated that diclofenac sodium could be continuously released from MIL-101 (Fe) for more than 48 h. There was no toxicity in vitro and in vivo, and the safety of MIL-101 (Fe) was confirmed by hematoxylin and eosin as well as ELISA tests in vivo. The results of behavioral testing, pharmacokinetics, and RNA sequencing analysis showed that MIL-101 (Fe) loaded with diclofenac sodium could enhance the mechanical withdrawal threshold and alleviate cold allodynia induced by Spared Nerve Injury, prolonging the work time by three days. The results indicated that MIL-101 (Fe) exhibited excellent biocompatibility, while the MIL-101 (Fe)-DS demonstrated analgesic and controlled-release properties. These findings provide a scientific foundation for the clinical management of neuropathic pain and the development of a novel formulation.


Assuntos
Diclofenaco , Nanomedicina , Neuralgia , Ratos Sprague-Dawley , Medula Espinal , Transcriptoma , Animais , Diclofenaco/administração & dosagem , Diclofenaco/farmacologia , Neuralgia/tratamento farmacológico , Masculino , Medula Espinal/metabolismo , Medula Espinal/efeitos dos fármacos , Transcriptoma/efeitos dos fármacos , Nanomedicina/métodos , Ratos , Portadores de Fármacos/química , Anti-Inflamatórios não Esteroides/administração & dosagem , Anti-Inflamatórios não Esteroides/farmacologia , Liberação Controlada de Fármacos , Preparações de Ação Retardada , Modelos Animais de Doenças , Hiperalgesia/tratamento farmacológico
18.
Pharmaceutics ; 16(3)2024 Feb 23.
Artigo em Inglês | MEDLINE | ID: mdl-38543207

RESUMO

This study focuses on how to define an Analytical Target Profile (ATP) which is intended for use in practice and on facilitating the selection of in vitro release test (IVRT) technology for diclofenac sodium topical hydrogel and cream. The implementation involves incorporating the new draft guidelines of the International Council for Harmonisation (ICH Q14) and USP (United States Pharmacopeia) Chapter 1220. Four IVRT apparatuses were compared (USP Apparatus II with immersion cell, USP Apparatus IV with semisolid adapter, static vertical diffusion cell, and a new, in-house-developed flow-through diffusion cell) with the help of the ATP. Performance characteristics such as accuracy, precision, cumulative amount released at the end of the IVRT experiment, and robustness were investigated. We found that the best apparatus for developing IVRT quality control (QC) tests in both cases was USP II with an immersion cell. All four different IVRT apparatuses were compared with each other and with the data found in the literature.

19.
Cureus ; 16(2): e55279, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38435225

RESUMO

Diclofenac sodium is a commonly used nonsteroidal anti-inflammatory drug. It is widely used for acute and chronic pain management. Side effects, such as fixed drug eruption, asthmatic attack, and vasospastic angina, are commonly seen after the use of diclofenac sodium. However, anaphylaxis and anaphylactic shock secondary to injection of diclofenac sodium are rare. Our main aim in reporting this adverse event is to alert healthcare professionals to this potentially life-threatening adverse effect of diclofenac sodium and prompt use of adrenaline for treatment.

20.
Int J Biol Macromol ; 265(Pt 1): 130758, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38462106

RESUMO

Diclofenac sodium (DCF) was reported as an important emerging environmental pollutant and its removal from wastewater is very urgent. In this study, different alkyl substituted ionic liquids (1-alkyl -3-vinyl- imidazolium bromide [CnVIm]Br, n = 4, 6, 8, 10, 12) functionalized tragacanth gum (TG-CnBr) are prepared by radiation induced grafting and crosslinking polymerization. The adsorption behaviors of ionic liquids functionalized tragacanth gum for diclofenac sodium from aqueous solutions are examined. The adsorption capacity of TG-CnBr for diclofenac sodium increases with the increasing of alkyl chain length of the imidazolium cation and the hydrophobicity of the hydrogels. The maximum adsorption capacity by TG-C12Br for diclofenac sodium at 30, 40 and 50 °C were 327.87, 310.56 and 283.29 mg/g, respectively. The adsorption of TG-C12Br towards diclofenac sodium was little decreased with NaCl increasing. The removal efficiency was still remained 94.55 % within 5 adsorption-desorption cycles by 1 M HCl. Also, the adsorption mechanism including electrostatic attraction, hydrophobic interaction, hydrogen bonding, and π - π interaction was proposed.


Assuntos
Líquidos Iônicos , Tragacanto , Poluentes Químicos da Água , Diclofenaco/química , Tragacanto/química , Hidrogéis/química , Água , Adsorção , Poluentes Químicos da Água/química
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