Drug Diclofenac Sodium Research Articles

PHYTOCHEMICAL AND PHARMACOLOGICAL INVESTIGATIONS OF TINOSPORA CORDIFOLIA

The crude ethanol extract of the stem of Tinospora cordifolia (Family Menispermaceae) was evaluated for its antioxidant and analgesic activities. The antioxidant property of the ethanol extract of T. cordifolia was assessed by 1, 1-diphenyl –2- picryl hydrazyl (DPPH) free radical scavenging assay. The extract showed potential antioxidant activity (IC50 about 52.80 µg/ml), which was comparable to standard drug ascorbic acid (IC50 about 4.12 µg ml-1). The ethanolic extract of T. cordifolia also exhibited statistically significant (p<0.001) writhing inhibition in aceitic acid induced white albino mice (Swiss-webstar strain). It produced 40% inhibition of writhing at the dose of 500 mg kg-1 body weight while the standard drug (diclofenac sodium) inhibition was found to 45.22 % at a dose of 25 mg kg-1 body weight. The results tend to suggest that the crude ethanolic extract of T. cordifolia might possess antioxidant and analgesic activities.

Transplantation of adipose-derived mesenchymal stem cells ameliorates acute hepatic injury caused by nonsteroidal anti-inflammatory drug diclofenac sodium in female rats

BackgroundAlthough the beneficial role of adipose-derived mesenchymal stem cells (AD-MSCs) in acute liver injury has been addressed by numerous studies employing different liver injury inducers, the role of rat AD-MSCs (rAD-MSCs) in diclofenac sodium (DIC) – induced acute liver injury has not yet been clarified. ObjectiveThis study aimed to investigate whether rat adipose- rAD-MSCs injected intraperitoneal could restore the DIC-induced hepatoxicity. MethodsHepatotoxicity was induced by DIC in a dose-based manner, after which intraperitoneal injection of rAD-MSCs was performed. ResultsHere, the transplanted cells migrated to the injured liver, and this was evidenced by detecting the specific SRY in the liver samples. After administering DIC, a significant decrease in body weight, survival rate, serum proteins, antioxidants, anti-apoptotic gene expression, and certain growth factors, whereas hepatic-specific markers, pro-inflammatory mediators, and oxidative, pro-apoptotic, and ER-stress markers were elevated. These adverse effects were significantly recovered after engraftment with rAD-MSCs. This was evidenced by enhanced survival and body weight, improved globulin and albumin values, increased expression of SOD, GPx, BCL-2, VEGF, and FGF-basic expression, and decreased serum ALT, AST, ALP, and total bilirubin. rAD-MSCs also reduced liver cell damage by suppressing the expression of MDA, IL-1B, IL-6, BAX, JNK, GRP78/BiP, CHOP, XBP-1, and cleaved caspase 3/7. Degenerative hepatic changes and multifocal areas of fatty change within liver cells were observed in DIC-received groups. These changes were improved with the transplantation of rAD-MSCs. ConclusionsWe could conclude that targeted AD-MSCs could be applied to reduce hepatic toxicity caused by NSAIDs (DIC).

Design of g‐C3N4/BaBiO3 Heterojunction Nanocomposites for Photodegradation of an Organic Dye and Diclofenac Sodium under Visible Light via Interfacial Charge Transfer

AbstractA novel series of the heterojunctions g‐CN/BBO(x) of g‐C3N4 (g‐CN) nanosheets decorated with spherical particles of BaBiO3 (BBO) were designed to enhance photocatalysis through interfacial charge transfer. The synthesized g‐CN/BBO(x) nanocomposites were characterized by various techniques such as XRD, FTIR, TEM, and SEM. Rhodamine B (RhB) dye and diclofenac sodium drug were taken as the model pollutants for the degradation under visible light. BBO facilitates the photocatalytic reaction after accepting electrons from the g‐CN. The g‐CN/BBO(30%) nanocomposite exhibits the best photocatalytic activity, which is 6.5 and 5 times higher than BBO and g‐CN, respectively. The enrichment in photodegradation is attributed to the combined effects of improved dye adsorption, visible light absorption, mobility of photogenerated carriers, and facial separation of electrons and holes (e−, h+) as supported by electrochemical impedance spectroscopy (EIS). This study provides new insight into the engineering, design, and stability of the g‐CN/BBO(x) heterojunction nanocomposite, as well as on its application and plausible mechanism for removal of harmful and detrimental pollutants such as RhB dye and diclofenac sodium drug under visible light.

ASSESSMENT OF PHYTOCHEMICAL AND PHARMACOLOGICAL ACTIVITIES OF THE ETHANOLIC EXTRACTS OF Hygrophila spinosa

Ethanolic extract of Hygrophila spinosa plant was prepared and tested for its phytochemical and pharmacological investigation. The extract showed the presence of steroid, alkaloid, reducing sugar, tannin,flavonoids, saponin and glycoside. The extract significantly and dose dependently inhibited the acetic acid induced writhing in mice (58.8%, P<0.001 and 25% at the dose of 500 and 250 mg/kg body weight respectively) and it is comparable to the activity of the standard analgesic drug diclofenac sodium (72.5%, P<0.001 at the dose of 25 mg/kg body weight). The extract of H. spinosa offered about 1.20 hr and 1.8 hr (P<0.001) of the mean latent period for diarrhoeal episode at the doses of 250 and 500 mg/kg body weight which is comparable to the standard antidiarrhoeal drug loperamide. The results tend to suggest that the plant possess analgesic and antidiarrhoeal activities or active constituent(s) responsible for the mentioned activities and thus supported its traditional uses.

PHYTOCHEMICAL AND BIOLOGICAL INVESTIGATION OF SEEDS OF Hyptis suaveolens

The crude ethanolic extract of the seeds of Hyptis suaveolens was evaluated for its analgesic,antidiarrhoeal and cytotoxic activities. The extract significantly and dose dependently inhibited the acetic acid induced writhing in mice (69.7%, P < 0.001 and 60.6%, P < 0.001 for 500 and 250 mg/kg body weight,respectively), comparable to the standard drug diclofenac sodium. The extract also decreased the frequency of defecation and increased mean latent period significantly (P< 0.05) at the doses of 250 and 500 mg/kg body weight respectively compared with the control group. Moreover, it displayed considerable general toxicity towards brine shrimps. The LC50 value of the extract was 80 µg/ml which was comparable to that of standard drug chloramphenicol (43 µg/ml). All the results tend to justify the traditional uses of the seeds of Hyptis suaveolens.

PHYTOCHEMICAL AND PHARMACOLOGICAL SCREENING OF Enhydra fluctuans Lour.

The study was aimed to evaluate pharmacological activities of the leaves of Enhydra fluctuans Lour. (Family-Asteraceae). The interesting reported pharmacological activities, coupled with the use of the plant in traditional medicine qualify E. fluctuans Lour. for possible analgesic, antidiarrhoeal and antioxidant activities. These activities were investigated on animal model like Swiss albino mice. Phytochemical analysis using standard screening methods indicated the presence of alkaloids, tannins, steroids, gums, glycosides, saponins and flavonoids in the ethanolic plant extract. The ethanolic extract obtained by cold extraction method, showed anti oxidant activity of IC50 = 197 µgm/ml in DPPH assay while that of the standard ascorbic acid was observed to be IC50 = 18 µgm/ml. In Folin-Ciocalteau assay total phenolic content was found to be 157 mg GAE/100 gm of dry powder. This extract when applied at 250 and 500 mg/kg exhibits significant inhibition of writhing reflex 25.43% (p< 0.02) and 40.67 % (p< 0.05) respectively while with that of the standard drug diclofenac sodium inhibition was observed to be 68.82% (p<0.001) at a dose of 25 mg/kg body weight. In castor oil induced method the extract produced 23.81 and 47.62 % (p<0.02 and p<0.01) inhibition of diarrhoea at the doses of 250 mg/kg and 500 mg/kg body weight, respectively while standard loperamide showed 85.72 % (p<0.001) inhibition at a dose of 3 mg/kg body weight.

A Solid–Liquid Composite Lubricating “Nano‐Snowboard” for Long‐Acting Treatment of Osteoarthritis

AbstractOsteoarthritis is a chronic inflammatory disease characterized by cartilage degeneration. Anti‐inflammatory therapy has limited effects, and effective reduction of cartilage wear through lubrication is essential. In vivo stability and lubricity of commercial lubricants are insufficient, leading to failure of lubricating treatment and progression of osteoarthritis. To address these issues, new therapeutic methods combining anti‐inflammation and stable high‐performance lubrication are developed. Inspired by the sliding mechanism of snowboards, a “nano‐snowboard” by modifying molybdenum disulfide (MoS2) with a biomimetic phospholipid polymer poly (dopamine methacrylamide‐co‐2‐methacryloyloxyethyl phosphorylcholine) (PDMPC) and loading anti‐inflammatory drug diclofenac sodium (DS), namely MoS2‐PDMPC‐DS, has been synthesized. MoS2 with a 2D layered structure and photothermal properties, serves as solid lubricant and drug carrier. Meanwhile, the modification of PDMPC on the surface of MOS2 avoids the oxidative denaturation of MoS2 in a physiological environment, forming solid–liquid composite lubrication and improving the lubricity and stability of MoS2 in the joint cavity. In vitro and in vivo experiments show that MoS2‐PDMPC‐DS can stay in the joint cavity for more than one week and exert long‐lasting lubrication and anti‐inflammatory effects to treat osteoarthritis effectively. This solid–liquid composite lubricating nano‐snowboard provides a new idea for synergistic anti‐inflammatory and lubricating treatment of osteoarthritis.

Syntheses, Molecular Docking and Biological Evaluation of 2-(2- hydrazinyl)thiazoles as Potential Antioxidant, Anti-Inflammatory and Significant Anticancer Agents.

Recently, researchers have worked on the development of new methods for the synthesis of bioactive heterocycles using polyethylene glycol as a green solvent. In this context, we report the synthesized 2-(2-hydrazinyl) thiazoles for their in vitro antioxidant, in vitro anti-inflammatory and in vitro anti-cancer activities. The objective of the study was to develop novel antioxidant, anti-inflammatory and anti-cancer drugs. At the outset, the condensation of substituted acetophenones 1, thiosemicarbazide 2, and α-haloketones 3 was carried out using PEG-400 (20 mL) in the presence of 5 mol% glacial acetic acid to afford thiosemicarbazones intermediate. Furthermore, these thiosemicarbazones were reacted with α-haloketones 3 to obtain appropriate 2-(2-hydrazinyl) thiazoles. The synthesized compounds were in vitro tested for their antioxidant, anti-inflammatory, and anti-cancer activity. In vitro evaluation report showed that nearly all molecules possessed potential antioxidant activity against 2,2-Diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO), superoxide radical (SOR) and hydrogen peroxide (H2O2) radical scavenging activity. Most 2-(2-hydrazinyl) thiazoles derivatives have shown potential anti-inflammatory activity as compared to diclofenac sodium as a reference standard. 2-(2-Hydrazinyl) thiazoles derivatives showed significant anticancer activity for human leukemia cell line K-562 compared to adriamycin as a reference standard. All tested compounds showed potential 2,2-Diphenyl-1-picrylhydrazyl (DPPH) and nitric oxide (NO) radical scavenging activity. Among the tested series, 4b, 4d and 4e exhibited good hydrogen peroxide and 4b, 4e, 4f and 4g showed excellent superoxide radical scavenging activity. In addition, the 4b, 4e and 4g compounds revealed potent in vitro anti-inflammatory activity against standard diclofenac sodium drug. 2-(2-Hydrazinyl) thiazole derivatives, such as 4c and 4d, showed significant anticancer activity against human leukemia cell line K-562. Thus, these molecules provide an interesting template for the design and development of new antioxidant, anti-inflammatory, and anti-cancer agents.

Design, Synthesis and Bioevaluation of Highly Functionalized 1,2,3-Triazole-Guanidine Conjugates as Anti-Inflammatory and Antioxidant Agents

In search of new biologically potent molecules a small focused library of new guanidine-1,2,3-triazole hybrid derivatives were synthesized via Organocatalytic enolate- mediated azide-carbonyl [3 + 2] cycloaddition yielding a highly functionalized triazole core structure. The synthesis of all the derivatives were confirmed by spectral analysis 1H NMR, 13C NMR and MS. The new guanidine-1,2,3-triazole conjugates were found to exhibit promising anti-inflammatory and antioxidant activity. The anti-inflammatory activity screened by membrane stabilization method summarizes the four potential conjugates 5c, 5f, 5h and 5g to be potent in comparison with standard drug Diclofenac sodium (DFS). The conjugates were also assessed for antioxidant potential by DPPH method. Among all the synthesized compounds, the compounds 5d, 5f, 5g and 5h exhibited potent antioxidant activity. Molecular docking study was performed to gain insight into the putative binding mode and binding strength of these compounds with the target enzyme Cyclo-oxygenase (COX-2) enzyme. The in vitro and in silico studies together with simpler designing and synthesis strategy via Organocatalytic enolate- mediated azide-carbonyl [3 + 2] cycloaddition followed by a two-component reaction with guanidine in basic conditions rationalize guanidine-1,2,3-triazole hybrid derivatives as easily assessable novel therapeutic agents.

Evaluation of In Vitro Antiprotease Activity of Selected Traditional Medicinal Herbs in Dentistry and Its In Silico PASS Prediction.

Background Dental/oral diseases are one of the significant public health problems globally. Herbal medicines for managing oral diseases are considered an effective alternative to synthetic compounds due to their lower side effect. Azadirachta indica, Terminalia chebula, Camellia sinensis, and Piper nigrum are used to control and prevent oral inflammations in dentistry. In this study, we have evaluated the protease inhibition activity of these plant extracts, and further, the binding mode of the active ingredient of these plants with trypsin was studied using molecular docking. Methods In this study, protease inhibition activity was carried out using aqueous extracts of the plant parts such as Azadirachta indica (neem) twig, Terminalia chebula (Haritaki) fruit, Camellia sinensis (green tea) powder, and Piper nigrum (kali miri) seed. Next, to explore the binding mode of active ingredients azadirachtin, chebuligenic acid, catechin, and piperine with trypsin, we employed a molecular docking study using AutoDock4.2. Results The results revealed that the Azadirachta indica plant extract showed an IC50 value of 96.19 μg mL−1, Camellia sinensis IC50 value of 188.50 μg mL−1, Piper nigrum IC50 value of 371.20 μg mL−1, and Terminalia chebula IC50 value of 639.48 μg mL−1, when compared with standard drug diclofenac sodium, had IC50 value 93.00 μg mL−1. Further, the docking result reveals that all the main active ingredients of these plants have significant binding affinity and prefer the same binding pocket of trypsin. Conclusion Hence, our results show the importance of traditional plants Azadirachta indica, Terminalia chebula, green tea, and Piper nigrum to control oral disease conditions. As they show significant protease inhibition activity, hence, the active ingredient could act as a potential anti-inflammatory agent and further help to prevent or control oral disease conditions such as gingivitis and periodontitis.

NOVEL ECOFRIENDLY TECHNIQUE FOR SPECTROPHOTOMETRIC ANALYSIS OF DICLOFENAC SODIUM TABLETS USING MELTED N, N- DIMETHYLUREA AS SOLID SOLVENT

Commonly used organic solvents for spectrophotometric analysis of water insoluble drugs include alcohol, chloroform, benzene, methylene chloride, dimethyl formamide, acetonitrile, toluene, acetone and hexane. The main drawbacks of organic solvents are high value, toxicity and pollution. Hence, it is essential to replace the organic solvents by other eco-friendly alternative sources. Hydrotropic solubilization technique is the best approach to increase the water solubility of poorly water-soluble drugs and overcome the problems related with organic solvents. The present investigation is an attempt to show application of hydrotropic technique using aqueous solutions of N, N-dimethylurea as a hydrotropic agent for extraction of a poorly water soluble drug, diclofenac sodium, from its tablet formulation. The present research work also provides an ecofriendly method to estimate spectrophotometrically the diclofenac sodium drug in tablet formulations without help of an organic solvent. Proposed spectrophotometric method was found to be novel, accurate, economic, ecofriendly and free from toxicity of organic solvent.

Comparative study of two versatile multi-analyte chromatographic methods for determination of diacerein together with four non-steroidal anti-inflammatory drugs: Greenness appraisal using Analytical Eco-Scale and AGREE metrics

According to green analytical chemistry (GAC) principles, multi-analyte methods are usually more preferred than methods determining one analyte at a time (principle 8) as they allow saving resources (time, reagents and money) (principle 9) and permit the reduction of generated waste (principle 7) as well as reduction of needed samples (principle 2). The present work herein, describes for the first time the development, validation and comparison of novel green versatile multi-analyte HPLC-DAD and HPTLC methods for the quantitative estimation of five drugs (diacerein, aceclofenac, diclofenac sodium, celecoxib and meloxicam) within a single run in a short analysis time. For HPLC-DAD, separation was performed through using Zorbax SB C18 (4.6 × 250 mm, 5 μm particle size) with the mobile phase composed of 0.05 M phosphate buffer pH 3.0 and acetonitrile (42:58, v/v) at a flow rate of 1 mL/min. The chromatograms were extracted at 258, 276 and 355 nm. In HPTLC procedure, precoated TLC silica gel aluminum plates 60 F254 were used with a mobile phase consisting of mixture of (chloroform: methanol: acetic acid, 92:8:0.25, v/v/v). The developed plates were scanned densitometrically at 258, 280 and 360 nm. Validation of the proposed methods was performed following the ICH guidelines for linearity, ranges, precision, accuracy, robustness, detection and quantification limits. Good linearities were confirmed by the high values of correlation coefficients (r > 0.9992). Appraisal of the greenness of the developed methods and comparison with different reported chromatographic methods was performed using the analytical Eco-scale (AES) approach and the novel Analytical GREEnness (AGREE) metric.

SCREENING FOR ANALGESIC AND ANTI INFLAMMATORY ACTIVITIES OF ETHANOLIC EXTRACT OF JUSTICIA GENDARUSSA BURM LEAVES

Ethanol extract of the leaves of Justicia gendarussa Burm was subjected to analgesic and anti-inflammatory activities in animal models. Albino Wistar rats and mice were the experimental animals respectively. Different CNS depressant paradigms like analgesic (determined via Eddy's hot plate approach and acetic acid writhing approach) and antiinflammatory activity (determined via carrageenan induced paw edema using plethysmometer in albino rats) were carried out, following the intra-peritoneal administration of ethanol extract of formulation Justicia gendarussa Burm leaves (EEJG) at the dose level of 250mg/kg and 500mg/kg. The analgesic and anti-inflammatory activities of ethanol extracts of EEJG showed significant results (P andlt. The maximum analgesic activity was observed at 120 min at the dose of 500mg/kg (i.p.) and analgesic and anti-inflammatory activity was compared with standard drug Diclofenac sodium (5 mg/kg). Ethanol extract of Justicia gendarussa Burm leaves has shown significant analgesic and anti-inflammatory activities at the dose of 500mg/kg and was comparable with corresponding standard drugs. The activity was attributed to the presence of phytoconstituents in the tested extract.

Adsorption of Sodium Diclofenac in Functionalized Palygoskite Clays.

The effects of acid and organo-functionalizations on the surface of Brazilian palygorskite clay was investigated, evaluating its potential in the adsorptive capacity of the drug sodium diclofenac present in wastewaters. The modifications on the clay structure were investigated by X-ray diffraction, X-ray fluorescence, thermogravimetric, differential thermal analysis, Fourier transform infrared spectroscopy, surface area by N2 adsorption (77.5 K) and Zeta potential. The experimental design was carried out to find the best conditions for the adsorption tests, in which concentration, mass and pH were significant. In the kinetic study, the pseudo-second-order model better described the adsorption process for acid and organo-functionalized samples. Such results indicate that the adsorption behavior probably occurs due to the phenomenon of chemisorption. Regarding the adsorption isotherms, the Langmuir model was the one that best adjusted both the experimental data of acid and the organo-functionalized samples, whose maximum adsorption capacity were 179.88 and 253.34 mg/g, respectively. This model also indicates that the sodium diclofenac is adsorbed to monolayers homogeneously through chemisorption. In general, the studied clays proved to be suitable adsorbents for the removal of sodium diclofenac.

GC-MS Analysis and Various In Vitro and In Vivo Pharmacological Potential of Habenaria plantaginea Lindl.

Background. The current study aims to give a scientific origin for employing Habenaria plantaginea Lindl. as a potential candidate against nociception, inflammation, and pyrexia. The pharmacological studies were performed on crude extract and subfractions. In the gas chromatography-mass spectroscopy analysis, a total of 21 compounds were identified. The plant samples were displayed for in vitro anti-inflammatory potentials. The observed IC50 for chloroform against cyclooxygenase-2 and 5-lipoxygenase enzymes was 33.81 and 26.74 μg/mL, respectively. The in vivo activities were prerequisites with the acute toxicity studies. In carrageenan-induced inflammation, the chloroform fraction exhibited 46.15% inhibition similar to that of standard drug diclofenac sodium 47.15%. Likewise, in the acetic acid-induced writhing test, the ethyl acetate fraction displayed 71.42% activity, which was dose-dependent as that of standard drug. In Brewer's yeast-induced antipyretic activity, a significant decrease in rectal volume was observed after 30, 60, and 90 minutes. Moreover, the results of this study indicated that the chloroform and ethyl acetate fractions inhibited nociception, inflammation, and pyrexia dose dependently. Likewise, mechanistic insights indicated that naloxone antagonized the antinociceptive effect of chloroform and ethyl acetate fractions, thereby signifying the involvement of opioidergic mechanisms respectively. These results suggest that these molecules present in this plant have synergistically beneficial potential for the cure and management of analgesia, inflammation, and pyrexia.

Comparative Drug Release Investigations for Diclofenac Sodium Drug (DS) by Chitosan-Based Grafted and Crosslinked Copolymers.

The hydrogels responding to pH synthesized by graft copolymerization only and then concurrent grafting and crosslinking of monomer N-isopropyl acrylamide (NIPAAM) and binary comonomers acrylamide, acrylic acid and acrylonitrile (AAm, AA and AN) onto chitosan support were explored for the percent upload and release study for anti-inflammatory diclofenac sodium drug (DS), w.r.t. time and pH. Diclofenac sodium DS was seized in polymeric matrices by the equilibration process. The crosslinked-graft copolymers showed the highest percent uptake than graft copolymers (without crosslinker) and chitosan itself. The sustainable release of the loaded drug was studied with respect to time at pH 2.2, 7.0, 7.4 and 9.4. Among graft copolymers (without crosslinking), Chit-g-polymer (NIPAAM-co-AA) and Chit-g-polymer (NIPAAM-co-AN) exhibited worthy results for sustainable drug deliverance, whereas Crosslink-Chit-g-polymer (NIPAAM-co-AA) and Crosslink-Chit-g-polymer (NIPAAM-co-AAm) presented the best results for controlled/sustained release of diclofenac sodium DS with 93.86 % and 96.30 % percent release, respectively, in 6 h contact time. Therefore, the grafted and the crosslinked graft copolymers of the chitosan showed excellent delivery devices for the DS with sustainable/prolonged release in response to pH. Drug release kinetics was studied using Fick’s law. The kinetic study revealed that polymeric matrices showed the value of n as n > 1.0, hence drug release took place by non-Fickian diffusion. Hence, the present novel findings showed the multidirectional drug release rate. The morphological changes due to interwoven network structure of the crosslinked are evident by the Scanning electron microscopy (SEM) analysis.

Medicated Supportive Braces: A Synergy of Treatments for Joint Pain Relief

Background and objectives: The present study unveils a simple but innovative combina-tion of existing treatments of three different domains with unique logical aspects. Joint pain is the major cause of disability, especially for older adults. Currently, two widely practiced treatment op-tions are combined to produce simultaneous treatments that overcome the drawbacks of individual treatment and improve patient compliance. Moreover, a third treatment option of cooling and coun-terirritant material (Menthol) for pain relief was also explored successfully as a substitute treatment. Method: In the present study, we formulated and optimized an adhesive topical patch of the model drug diclofenac sodium, a widely used medicine for pain relief and menthol, a cooling and counter-irritant substance to aid pain relief. Combinations of two polymers, PVP-K30 and PVA, selected by trial batches, were further optimized by applying a 3x2 full factorial design. Two factors, X1 (PVP-K30) and X2 (PVA), were optimized using three responses, R1 (Q2), R2 (Q4), and R3 (Q12). De-rived mathematical models for responses were validated using checkpoint batches. The final opti-mized batch was derived based on the desirability function. Factorial batches were also evaluated for relevant parameters. Results: Results obtained by checkpoint batches were in line with the experimental results with 5% relative error, revealing that the derived models were valid for the design. The final optimized batch obtained by the desirability function followed all set criteria. Medicated patch prepared by opti-mized formulation was incorporated into the knee brace using an in-house patch holder mechanism. Conclutions: Combined treatment offers better patient compliance for the patient and the healthcare provider, which can be extended to other pain-relieving supportive treatments like elbow braces, waist brace, back support belt, cervical brace, etc.

High surface area and supermicroporous activated carbon from capsicum (Capsicum annuum L.) industrial processing pulp via single-step KOH-catalyzed pyrolysis: Production optimization, characterization and its some water pollutants removal and supercapacitor performance

In this study, we aimed to convert capsicum (Capsicum annuum L.) industrial processing pulp (CP) into low-cost and high-quality activated carbon (AC) under optimal production conditions through single-step KOH-catalyzed pyrolysis. Optimal production conditions were determined by investigating the effects on some textural characteristics of the produced ACs by changing the process variables such as mixing ratio (KOH/CP, w/w), pyrolysis temperature, and pyrolysis duration, respectively. The AC (CPAC) with the BET (Brunauer-Emmett-Teller) highest surface area (1564 m2/g), pore-volume (0.623 cm3/g), and average pore size (1.8 nm) was produced under conditions with a mixing ratio of 1.5, a pyrolysis temperature of 700 °C, and a duration of 1 h. It was characterized by nitrogen adsorption/desorption, Scanning Electron Microscopy (SEM)/Energy Dispersive X-Ray (EDX), X-ray Diffraction (XRD), Raman Microscopy and Fourier Transform Infrared Spectroscopy (FT-IR) techniques. In addition, the adsorption ability was determined by examining the removal performance of water pollutants such as methylene blue (MB) and methanol yellow (MY) dyes, 2,4-dichlorophenoxyacetic acid herbicide (2,4-D), diclofenac sodium drug (DCF), copper(II) ion (Cu(II)), and nitrate (NO3−), which were chosen because they are frequently detected in industrial wastewater, and found to be 294.1, 370.4, 384.6, 294.1, 212.8 and 59.5 mg/g, respectively. The supercapacitor performance of the electrodes developed from CPAC was tested as the coin size cell. The gravimetric capacitances of the electrodes were calculated as 198 F/g at the current densities of 0.5 A/g. The results of this study reveal that CPAC can be used as an alternative to commercial carbon as a clean and ecologically compatible low-cost (~$1.75 per kg) adsorbent that can improve water quality, and promising electrode material for low-cost and high-performance carbon-based supercapacitors.

GC-MS Characterization, In Vitro Antioxidant, Anti-inflammatory and Potential Antidermatophytic Activity of Citrullus lanatus Seed Oil

Background: Dermatophytes are well-known fungus having the capability to invade kerat-inized tissues of nails, skin, and hair, of humans and other animals, causing dermatophytosis. Citrullus lanatus (watermelon) seed is a rich source of vitamin E, essential fatty acids, and minerals, bearing var-ious health benefits. Despite the presence of many useful components, the oil is not much explored. Accordingly, the study was planned to investigate the fatty acid profiling, in vitro antioxidant, anti-inflammatory, and potential antidermatophytic activity of Citrullus lanatus seed oil against dermato-phytic strains. Methods: The C. lanatus oil was extracted from seeds, and fatty acid profiling was characterized by GC-MS. Further, the oil was subjected to DPPH scavenging activity, and the anti-inflammatory activity was evaluated from Bovine serum albumin assay. The antidermatophytic screening against Microsporum canis, Trichophyton rubrum, and Trichophyton mentagrophytes was carried out by agar well diffusion, broth microdilution assay, and growth kinetics assay. Results: The C. lanatus seed oil exhibited good antioxidant activity close to ascorbic acid, i.e., IC50- 52.22 μg/ml, 35.72 μg/ml, respectively, and the oil exhibited moderate anti-inflammatory ac-tivity (315.2 μg/ml) as that of the standard drug diclofenac sodium (174.3μg/ml). The fatty acid profiling indicates the presence of eight main compounds, out of which ç-tocopherol, butylated hy-droxytoluene, and hexadecanoic acid are predominantly present. The C. lanatus seed oil showed promising activity against T. rubrum with a lower minimum inhibitory concentration value with re-spect to positive controls, Fluconazole and Ketoconazole. The oil also had a strong effect on time-dependent kinetic inhibition against T. rubrum. This was the first report of C. lanatus seed oil against any dermatophyte. Conclusion: In conclusion, the study supports the exploitation of C. lanatus seed oil and its main compounds as a source of natural antioxidants, anti-inflammatory, and as a novel agent against dermatophytes for curing superficial fungal infections in the near future.

Distribution of Drug Substances in Solid Lipid Microparticles (SLM)-Methods of Analysis and Interpretation.

The incorporation of drug substances into the matrix of solid lipid microparticles (SLM) is critical to providing effects such as prolonged release, taste masking, and protection of the labile API. Currently, a commonly used method of characterizing multi-compartment lipid systems, such as SLM, is to determine entrapment efficiency (EE) and drug loading (DL) parameters, but this is not sufficient for understanding the localization of API either in the core or on the surface of the microspheres. The main objective of the research was to study the distribution of API in an aqueous dispersion of SLM in order to distinguish between the API incorporated in the lipid matrix and localized in the superficial region (interphase) and to refer the obtained results to the EE and DL parameters. SLM dispersions (10–30% of the lipid) with four model drug substances, i.e., cyclosporine, clotrimazole, diclofenac sodium and hydrocortisone, were prepared and investigated. In the first stage, the experiments were designed to optimize the method of extracting the API fraction localized on the SLM surface by shaking the dispersions with methanol. The fraction dissolved in the aqueous phase was obtained by ultrafiltration of SLM dispersions. Total drug content and the concentration in the separated phases were determined by the HPLC method. The obtained results were compared with the EE and DL parameters. Selected SLM dispersions were tested both before and after thermal sterilization. Short-term shaking of SLM dispersion with methanol does not damage the lipid matrix and allows the API fraction localized on the SLM surface to be extracted, the result of which was the determination of API distribution between lipid matrix, interphase and aqueous phase. It was found that the majority of API represented by EE value was localized on the surface of SLM. Only for cyclosporine was the incorporation of drug molecules in the lipid core very effective (up to 48%), while for other drug substances only 1–21% was found in the lipid core of SLM. A clear influence of the sterilization process on the distribution of API within the microparticles was found. The presented studies showed that the characterization of multi-compartment SLM dispersions solely on the basis of EE and DL values, is insufficient. The proposed new distribution test method enables the localization of API to be demonstrated within the microspheres, with the quantitative characteristics of the drug fraction incorporated in the lipid matrix and the fraction associated with the surface of the lipid matrix. The proposed new method allows the influence of the sterilization process on the changes in the API distribution within the lipospheres to be evaluated. Such characteristics provide new opportunities for the development and use of this dosage form as a carrier providing prolonged release and other aforementioned advantages.