Diclofenac Research Articles

TRABECULECTOMY IN CLOSED ANGLE UVEITIS GLAUCOMA A CASE REPORT

Introduction : Glaucoma uveitis is caused by increased outflow resistance, which distorts the balance between water production and outflow. Trabeculectomy is better than LPI in controlling IOP in glaucoma uveitis
 Case Illustration : Male patient aged 45 years, came to the Eye Polyclinic at Serui Hospital with complaints of very painful right eye since 2 weeks ago, the patient also complained of being unable to see at all, red eyes, headache, stiff neck, nausea and vomiting. Ophthalmological examination reveal right eye vision no light perception (NLP), palpebral edema, spasm, conjunctival hyperemia, corneal edema, shallow anterior chamber angle, iris-corneal contact, negative pupillary reflex, total pupillary block, negative fundus reflex, schiotz IOP 81 mmHg.
 Discussion : The patient diagnosed as right eye acute glaucoma and treated with acetazolamide, timolol maleate eye drops, potassium aspar tablets, prednisolone acetate drops, diclofenac sodium drops in the right eye, paracetamol tablets, re-evaluate in 2 hours. The patient chose to be referred to a hospital in Surabaya. The patient came back with the same complaint and was treated the same as before, right eye surgery trabeculectomy + peripheral iridectomy with releaseable suture flap limbal base with controlled IOP results, releaseable suture sutures were removed in 2 weeks. Trabeculectomy of the uveitic eye is generally less successful because of accelerated wound healing by the postoperative fibrinous and cellular response. Antimetabolites such as 5FU and Mitomycin C are used to enhance the success of trabeculectomy in uveitis eyes (5FU, MMC). 95% success (IOP less than 21 mm Hg with 1 or no treatment) was achieved with MMC augmented trabeculectomy.
 Conclusion : Increased IOP due to pupillary block causes acute glaucoma with signs of high IOP, middilated pupils, decreased pupillary reflexes, and irregular shape, corneal epithelial edema, episcleral and conjunctival vascular congestion, shallow anterior chamber, small number of flares and cells.

TRABECULECTOMY IN CLOSED ANGLE UVEITIS GLAUCOMA A CASE REPORT

Introduction : Glaucoma uveitis is caused by increased outflow resistance, which distorts the balance between water production and outflow. Trabeculectomy is better than LPI in controlling IOP in glaucoma uveitis
 Case Illustration : Male patient aged 45 years, came to the Eye Polyclinic at Serui Hospital with complaints of very painful right eye since 2 weeks ago, the patient also complained of being unable to see at all, red eyes, headache, stiff neck, nausea and vomiting. Ophthalmological examination reveal right eye vision no light perception (NLP), palpebral edema, spasm, conjunctival hyperemia, corneal edema, shallow anterior chamber angle, iris-corneal contact, negative pupillary reflex, total pupillary block, negative fundus reflex, schiotz IOP 81 mmHg.
 Discussion : The patient diagnosed as right eye acute glaucoma and treated with acetazolamide, timolol maleate eye drops, potassium aspar tablets, prednisolone acetate drops, diclofenac sodium drops in the right eye, paracetamol tablets, re-evaluate in 2 hours. The patient chose to be referred to a hospital in Surabaya. The patient came back with the same complaint and was treated the same as before, right eye surgery trabeculectomy + peripheral iridectomy with releaseable suture flap limbal base with controlled IOP results, releaseable suture sutures were removed in 2 weeks. Trabeculectomy of the uveitic eye is generally less successful because of accelerated wound healing by the postoperative fibrinous and cellular response. Antimetabolites such as 5FU and Mitomycin C are used to enhance the success of trabeculectomy in uveitis eyes (5FU, MMC). 95% success (IOP less than 21 mm Hg with 1 or no treatment) was achieved with MMC augmented trabeculectomy.
 Conclusion : Increased IOP due to pupillary block causes acute glaucoma with signs of high IOP, middilated pupils, decreased pupillary reflexes, and irregular shape, corneal epithelial edema, episcleral and conjunctival vascular congestion, shallow anterior chamber, small number of flares and cells.

Utilization of Suji Leaves Extract (Pleomele Angustifolia N.E Brown) in Inhibiting Carrageenan-Induced Inflammation on Rats

Suji leaf (Pleomele angustifolia N.E. Brown) has long been used as an ingredient for traditional medicines. This study seeks to evaluate the anti-inflammatory activity of suji leaf extract in terms of its ability to reduce oedema in the hind paws of rats. Six groups were treated: negative control, positive control given diclofenac sodium as anti-inflammatory medication, two groups of suji leaf extract powder (SEP) with doses of 300 and 800 mg/kg, acetone extract of suji leaf (AES), and a group of acetone extract of SEP (EA-SEP) at a dose of 500 mg/kg with oral administration. Injections of 1% carrageenan suspension into the right hind paw of rats induced inflammation. The results demonstrated that SEP administered at a dose of 800 mg/kg has an inflammatory capacity (80.56%), AES (56.94%), and AE-SEP (75.7%). Chlorophyll, total phenol, and antioxidant capacity in SEP (9.0809 mg /g sample; 3.7354 mg GAE/g sample; 3.04 mg AAE/g sample), AES (4.6471 mg /g sample; 0.9994 mg GAE/g sample; 3.26 mg AAE/g sample), and AE-SEP (6.4912 mg /g sample; 2.1703 mg GAE/g sample; 2.55 mg AAE/g sample). According to qualitative test results, Suji extract contains bioactive compounds of the flavonoid group, saponins, steroids, and triterpenoids. It is believed that phenolic compounds function as anti-inflammatory agents.

Guava seed activated carbon loaded calcium alginate aerogel for the adsorption of diclofenac sodium: Characterization, isotherm, kinetics, and optimization via Box-Behnken design

This study aimed to develop a novel adsorbent designed for the removal of diclofenac sodium (DS) from water. The synthesized adsorbent, a composite sponge known as guava seeds activated carbon loaded calcium alginate (GSAC@CA aerogel), was created through the combination of powdered activated carbon derived from guava seeds and loaded onto a calcium alginate hydrogel. Characterization through SEM, XRD, FT-IR, BET, and XPS revealed a confirmed surface area of 738.82 m2/g. The investigation delved into assessing the influence of pH, initial DS concentration, and adsorbent dose on the adsorption of DS. Isotherm studies on adsorption suggested that a Langmuir model provided a good fit, indicating a monolayer adsorption process. Kinetic studies revealed a well-fitted pseudo-second-order model, shedding light on the dynamics of the reaction. The chemisorption nature was elucidated by the Dubinin-Radushkevich model, demonstrating an adsorption energy of 22.6 kJ/mol. These results affirm the potential of the GSAC@CA aerogel composite sponge as an efficient adsorbent for removing diclofenac sodium from water. Examination of the impact of temperature on the adsorption process revealed an endothermic behavior, indicating an increase in temperature. The positive change in entropy suggested the spontaneous nature of the reaction. Remarkably, the GSAC@CA aerogel composite sponge exhibited strong adsorption capabilities, achieving a maximum adsorption capacity of 489.97 mg/g. Across five consecutive cycles, the composite consistently demonstrated high-level adsorption, maintaining a removal efficiency of 87.77 %. The adsorption mechanism of diclofenac sodium (DS) on the GSAC@CA aerogel composite sponge was determined to encompass various processes, such as hydrogen bonding, π-π interactions, ion exchange, and electrostatic pore filling. Additionally, the adsorbent demonstrated successful regeneration over three cycles when applied to a real-world sample. The incorporation of the Box-Behnken design (BBD) introduced a strategic aspect to enhance adsorption outcomes, offering valuable insights for optimizing the adsorption process in practical applications.

Effects of Diclofenac Etalhyaluronate (SI-613/ONO-5704) on Cartilage Degeneration in Arthritic Rats and Inflammatory Cytokine-Stimulated Human Chondrocytes.

Cartilage degeneration is a key feature of osteoarthritis (OA) and rheumatoid arthritis and is thought to negatively impact patients' quality of life. Diclofenac etalhyaluronate (DEH, SI-613/ONO-5704) is a hyaluronic acid (HA) derivative chemically bound to diclofenac (DF) that has been reported to improve OA symptoms; however, its effect on cartilage degeneration remains unknown. In the present study, we investigated the chondroprotective effect of DEH in rats with collagen-induced arthritis and interleukin-1β-stimulated human chondrocytes. Rats with collagen-induced arthritis were administered DEH and HA intra-articularly, and DF orally. Knee joint swelling, histological scores of articular cartilage, and inflammatory (Il1b) and catabolic (Mmp3 and Mmp13) gene expression in the synovial tissue and cartilage were evaluated. In vitro direct effects of DEH on matrix metalloproteinase (MMP)-3 and MMP-13 expression were examined in interleukin-1β-stimulated human chondrocytes. In a rat model of collagen-induced arthritis, a single intra-articular dose of DEH inhibited knee joint inflammation and cartilage degeneration. Daily oral administration of DF had similar effects. Conversely, HA administered as a single intra-articular dose had no effect. Only DEH inhibited Mmp3 gene expression in the cartilage, whereas DEH and DF inhibited Mmp3 and Mmp13 mRNA expression in the synovial tissue. In interleukin-1β-stimulated human chondrocytes, DEH and HA inhibited MMP-3 and MMP-13 production, whereas DF had no effect. In this study, we demonstrated the chondroprotective effect of DEH in rats with collagen-induced arthritis and in interleukin-1β-stimulated human chondrocytes. Thus, DEH may suppress cartilage degeneration in patients with musculoskeletal diseases, such as OA.

Physiological responses on the reproductive, metabolism and stress endpoints of Astyanax lacustris females (Teleostei: Characiformes) after diclofenac and ibuprofen exposure

Diclofenac (DCF) and ibuprofen (IBU) are pharmaceutical compounds frequently detected in aquatic compartments worldwide. Several hazard effects including developmental abnormalities and redox balance impairment have been elucidated in aquatic species, but multiple endocrine evaluations are scarce. Therefore, the present study aimed to assess the disruptive physiological effects and toxicity of DCF and IBU isolated and combined, using females of the native freshwater teleost Astyanax lacustris. In regards to NSAIDs bioavailability, the results showed absence of degradation of IBU and DCF after 7 days of exposure. IBU LC50 for A. lacustris was 137 mgL−1 and females exposed to IBU isolated increased thyroxine (T4) concentration at 24 h and decreased after 96 h; DCF exposure decreased triiodothyronine (T3) concentration at 96 h. Circulating levels of 17β-estradiol (E2), cortisol (F) and testosterone (T) were not affected by any treatment. HPG and HPI axis genes fshβ, pomc and vtg were upregulated after 24 h of IBU exposure, and dio2 was downregulated in DCF fish exposed group after 96 h compared to the mixture. Protein concentration was reduced in muscle and increased in the liver by DCF and mixtures exposures at 24 h; while liver lipids were increased in the mixture groups after 96 h. The study point out the capacity of NSAIDs to affect endocrine endpoints in A. lacustris females and induce changes in energetic substrate content after acute exposure to isolated and mixed NSAIDs treatments. Lastly, the present investigation brings new insights into the toxicity and endocrine disruptive activity of NSAIDs in Latin America teleost species and the aquatic environment.

Steroids and/or Non-Steroidal Anti-Inflammatory Drugs as Postoperative Treatment after Trabeculectomy—12-Month Results of a Randomized Controlled Trial

This prospective randomized controlled trial aimed to compare the efficacy and safety of topical preservative-free diclofenac (DICLO) to dexamethasone (DEX) eyedrops, and their combination (DEX+DICLO) after trabeculectomy. Sixty-nine patients with medically uncontrolled glaucoma were randomized to receive topical postoperative treatment with DICLO (n = 23), DEX (n = 23), or a combination of DEX and DICLO (n = 23). The primary outcome was the intraocular pressure (IOP) 12 months postoperatively. Secondary outcomes included surgical success, failure, visual field, and visual acuity from baseline to 12 months postoperatively. IOP reached the lowest point one day after trabeculectomy. At 12 months, IOP was 10.0 mmHg (95% CI, 8.4–11.6 mmHg) for DICLO, 10.9 mmHg (95% CI, 9.4–12.3 mmHg) for DEX, and 11.2 mmHg (95% CI, 9.1–13.3 mmHg) for DEX+DICLO. There were no significant differences in IOP, surgical success, failure, visual field, or visual acuity between the DICLO, DEX, or DEX+DICLO groups. We found that topical diclofenac was not statistically different from topical dexamethasone in controlling IOP 12 months after trabeculectomy. Combining diclofenac and dexamethasone offered no added IOP control compared to dexamethasone alone.

Anti-Arthritic, Anti-Inflammatory, Thrombolytic, Membrane Stabilizing, Antifungal and Cytotoxic Activity of Polyscias scutellaria Leaf Extract: An In-vitro Analysis

The objective of this investigations was to evaluate in Vitro anti-arthritic, anti-inflammatory, thrombolytic, membrane stabilizing, antifungal and cytotoxic activities from the methanolic leaf extract of Polyscias scutellaria. Primary evaluation of methanolic extract of Polyscias scutellaria leaf (MEPSL) was performed via phytochemical screening. Presence of Alkaloids, flavonoids, saponins, glycosides, carbohydrates and reducing sugars were observed by phytochemical screening, among other secondary compounds. Using in vitro methods of protein denaturation, the anti-arthritic and anti-inflammatory properties of MEPSL was investigated. The results showed that the extracts significantly slowed down arthritis and inflammation with the percent inhibition of 94.59% and 86.33% at the conc. of 1000 µg/mL compared to the standard diclofenac sodium (98.19%) and acetyle salicylic acid (98.56%) at same concentration respectively. The thrombolytic activity of the extracts was additionally examined by clotlysis method, and the results showed that the ability to break up blood clots increased with the amount of extract used with the value of 97.32% which is very significant compared to the standard streptokinase which showed clotlysis of 91.304%. MEPSL was also showed action that stabilized membranes by using heat induced hemolysis method, which could be helpful in treating conditions like bleeding and swelling with the percent of protection value of 58.87% when compared to standard diclofenac sodium with the percent of protection value 73.63%. Antifungal action was also seen, which shows that it could be used to treat diseases caused by fungi with the zone of inhibition 7-36 mm varying on the type of fungi. Lastly, in vitro method was used to investigate the extracts' damaging effect on Artemia salina by using shrimp lethality assay. The results showed significant cytotoxicity with the LC50 value of 1.057 µg/mL compared to the standard vincristine sulphate (LC50 value of 0.608 µg/mL). To sum up, it is clear that the phytochemical found in this plant can be used for wide range of drug discovery field due to its potent pharmacological actions.

Zingiber officinale Root Capsule Extract Synergistically Enhance the Anti-Inflammatory Effects of Diclofenac Sodium in Experimental Acute Inflammation.

The present study aimed to evaluate the anti-inflammatory effects of ginger (Zingiber officinale) root capsule extract (GRCE) in doses of 100 mg/kg b.w. (body weight) and 200 mg/kg b.w. alone and in combination with a low dose (5 mg/kg b.w.) of diclofenac sodium (D) on carrageenan-induced acute inflammation (AI). The association of GRCE in a dose of 200 mg/kg b.w. with D offered the highest inhibition percentage for edema, reaching the maximum level of inhibition (95%) after 24 h. The association of GRCE in a dose of 200 mg/kg b.w. with D showed the ability to reduce tissue inflammatory changes when compared to D alone, while GRCE alone did not exhibit such properties. The association of both doses of GRCE with D showed significantly lower plasma and tissue levels of pro-inflammatory cytokines such as tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), and interleukin-1β (IL-1β) by up to 55% (p ≤ 0.0317), with the best results obtained by the group who received GRCE in the higher dose. These associations reduced the serum and tissue levels of prostaglandin-endoperoxide synthase 2 (COX-2) by up to 71% (p ≤ 0.0371). In conclusion, the association of GRCE with a low dose of D could be an appropriate combination to decrease the dose used to reduce serum and tissue levels of inflammatory molecules, edema, and histological changes in acute inflammation. Further research will be necessary to achieve clinical evaluation.

Comparison between Diclofenac Sodium and Ketorolac in the Management of Post-Appendectomy Pain

Aim: To compare the Diclofenac Sodium and ketorolac in the management of post-appendectomy pain. Study design: Single blinded analytical comparative trial Place and duration of study: Tertiary Care Hospital, Lahore from 01-03-2022 to 30-11-2022. Methodology: One hundred and twenty three patients within 8-48 years who were suffering from acute appendicitis and required appendectomy were randomly selected. They were randomly divided into two groups. One was Diclofenac sodium group which had 61 cases in it and was selected to receive Diclofenac Sodium post-surgery. The other group having 62 patients was ketorolac group receiving ketorolac for pain relief. The patients received the pain killer post 30 and then 60 minutes after their surgery. The comparative results and efficacy of each pain killer was analyzed and assessed through faces pain scale. Results: The mean age of the patients was 20.5±5.5 in diclofenac sodium and 21.3±6.1 in Ketorolac group. There were 75.4% males in former group while 62.9% in later group. The mean value of BMI was within normal range in both groups. The pain score recorded highest number of cases in Diclofenac Sodium and ketorolac group at score 02 within 30 minutes after surgery while the pain score significantly dropped in ketorolac group in 60 minutes to score 00 while it persisted highest in score 02 among patients given Diclofenac Sodium. Conclusion: Intravenous ketorolac has advanced analgesic effect than Diclofenac Sodium with a substantial low risk involved in cases of appendectomy. Key Words: Appendicitis, NSAIDS, Ketorolac, Diclofenac, Management.

Long-term dietary exposure to the non-steroidal anti-inflammatory drugs diclofenac and ibuprofen can affect the physiology of common carp (Cyprinus carpio) on multiple levels, even at “environmentally relevant” concentrations

The aim of the study was to evaluate the effects of emerging environmental contaminants, the non-steroidal anti-inflammatory drugs (NSAIDs) diclofenac (DCF) and ibuprofen (IBP), on physiological functions in juvenile common carp (Cyprinus carpio). Fish were exposed for 6 weeks, and for the first time, NSAIDs were administered through diet. Either substance was tested at two concentrations, 20 or 2000 μg/kg, resulting in four different treatments (DCF 20, DCF 2000, IBP 20, IBP 2000). The effects on haematological and biochemical profiles, the biomarkers of oxidative stress, and endocrine disruption were studied, and changes in RNA transcription were also monitored to obtain a comprehensive picture of toxicity. Fish exposure to high concentrations of NSAIDs (DCF 2000, IBP 2000) elicited numerous statistically significant changes (p < 0.05) in the endpoints investigated, with DCF being almost always more efficient than IBP. Compared to control fish, a decrease in total leukocyte count attributed to relative lymphopenia was observed. Plasma concentrations of total proteins, ammonia, and thyroxine, and enzyme activities of alanine aminotransferase (ALT), aspartate aminotransferase, and alkaline phosphatase (ALP) were significantly elevated in either group, as were the activities of certain hepatic antioxidant enzymes (superoxide dismutase, glutathione-S-transferase) in the DCF 2000 group. The transcriptomic profile of selected genes in the tissues of exposed fish was affected as well. Significant changes in plasma total proteins, ammonia, ALT, and ALP, as well as in the transcription of genes related to thyroid function and the antioxidant defense of the organism, were found even in fish exposed to the lower DCF concentration (DCF 20). As it was chosen to match DCF concentrations commonly detected in aquatic invertebrates (i.e., the potential feed source of fish), it can be considered “environmentally relevant”. Future research is necessary to shed more light on the dietary NSAID toxicity to fish.

Functionalization of Arabinoxylan in Chitosan Based Blends by Periodate Oxidation for Drug Release Study

AbstractThis article presents the isolation of arabinoxylan (AX) from Plantago ovata seed husk and its oxidation using periodate to create oxidized‐AX (OAX) with distinct functionalities. Utilizing the solution casting method, biocompatible blends of arabinoxylan/chitosan (AX/CS) are prepared at various weight ratios, and their properties are assessed. Fourier transform infrared spectroscopy (FT‐IR), x‐ray diffraction (XRD), and thermogravimetric analysis (TGA) are employed to gauge compatibility and thermal traits of AX and OAX with CS. Solubility tests reveal partial and limited solubility of AX and OAX in distilled water, respectively. OAX displays favorable compressibility and flow rate through Carr's index, Hausner's ratio, and angle of repose analyses. FT‐IR data confirm intermolecular hydrogen bonding between CS′s −NH2− group and OAX′s carbonyl group, with XRD showing low crystallinity. Diclofenac sodium (DC) is loaded as a model drug into AX/CS and OAX/CS blends for release studies in pH 6.8 phosphate buffer. Results exhibit OAX/CS blends with sustained drug release, surpassing AX/CS blends. Among ratios tested, the OAX/CS (1 : 2) blend emerges as a superior excipient, demonstrating enhanced in‐vitro release potential, highlighting oxidized blends′ promise in sustained drug delivery systems.

Discovery of new thymol-3,4-disubstituted thiazole hybrids as dual COX-2/5-LOX inhibitors with in vivo proof

New thymol–3,4-disubstitutedthiazole hybrids were synthesised as dual COX-2/5-LOX inhibitors. Compounds 6b, 6d, 6e, and 6f displayed in vitro inhibitory activity against COX-2 (IC50= 0.037, 0.042, 0.046, and 0.039 µM) nearly equal to celecoxib (IC50= 0.045 µM). 6b, 6d, and 6f showed SI (379, 341, and 374, respectively) higher than that of celecoxib (327). 6a–l elicited in vitro 5-LOX inhibitory activity higher than quercetin. 6a–f, 6i–l, 7a, and 7c possessed in vivo inhibition of formalin induced paw edoema higher than celecoxib. 6a, 6b, 6f, 6h–l, and 7b showed gastrointestinal safety profile as celecoxib and diclofenac sodium in the population of fasted rats. Induced fit docking and molecular dynamics simulation predicted good fitting of 6b and 6f without changing the packing and globularity of the apo protein. In conclusion, 6b and 6f achieved the target goal as multitarget inhibitors of inflammation.

Graphite/carbon-doped TiO2 nanocomposite synthesized by ultrasound for the degradation of diclofenac.

Graphite/C-doped TiO2 nanocomposite was synthesized at room temperature using a simple, impressive, and indirect sonication (20kHz) by the cup horn system. Tetrabutyltitanate as the precursor of titanium and graphite (G) as the carbon source was used in the preparation of nanocomposite as a photocatalyst. The molar ratio of G/TiO2 as a key parameter was investigated in the synthesis of G/C-doped TiO2. The obtained materials were widely characterized using XRD, SEM, TEM, FTIR, XPS, and UV-Vis diffuse reflectance techniques. The UV-Vis diffuse reflectance spectroscopy results showed that the edge of light absorption of nanocomposite was distinctly red-shifted to the visible area via carbon doping. The XPS outcomes acknowledged the existence of the C, Ti, and O in the photocatalyst. The composite showed an enhancement in the dissociation efficiency of photoinduced charge carriers through the doping process. The photocatalytic activity of the synthesized nanocomposite was checked with diclofenac (DCF) as a pharmaceutical contaminant. The results displayed that G/C-doped TiO2 represented better photocatalytic performance for DCF than TiO2. This was due to the excellent crystallization, intense absorption of visible light, and the impressive separation of photoinduced charge carriers. Various active species such as •OH, •O2¯, h+, and H2O2 play a role in the degradation of DFC. Therefore, different scavengers were used and the role of each one in degradation was investigated. According to the obtained results, •O2¯ radical showed a major role in the photocatalytic process. This work not only proposes a deep insight into the photosensitization-like mechanism by using G-based materials but also develops new photocatalysts for the removal of emerging organic pollutants from waters using sunlight as available cheap energy.

Natural Silicates Encapsulated Enzymes as Green Biocatalysts for Degradation of Pharmaceuticals.

Biocatalytic degradation with the use of enzymes has gained great attention in the past few years due to its advantages of high efficiency and environmental friendliness. Novel, cost-effective, and green nanoadsorbents were produced in this study, using natural silicates as an enzyme host matrix for core-shell immobilization technique. With the natural silicate as a core and silica layer as a shell, it was possible to encapsulate two different enzymes: horseradish peroxidase (HRP) and laccase, for removal and degradation of three pharmaceuticals: diclofenac (DFC), carbamazepine (CBZ), and paracetamol (PC). The biocatalysts demonstrated high oxidation rates for the selected pollutants. In particular HRP immobilized fly ash and perlite degraded DFC and PC completely during 3 days of interaction and also showed high degradation rates for CBZ. Immobilized laccase was successful in PC degradation, where up to 70-80% degradation of the compounds with aromatic rings was reported by NMR measurements for a high drug concentration of 10 μg/mL. The immobilization method played a significant role in this process by providing stability and protection for the enzymes over 3 weeks. Furthermore, the enzymes acted differently in the three chosen supports due to their complex chemical composition, which could have an effect on the overall enzyme activity.

In vitro assessment on anti-inflammatory and anti-lipidemic properties of selected plant species

Preliminary assessment for anti-inflammatory and anti-lipidemic properties was done with different solvent extracts derived from Urtica urens and Polygonum chinense leaves through in vitro experimentation. To evaluate anti-inflammatory properties, the stability of human red blood cells membranes and the denaturation activity of proteins were assessed. For anti-lipidemic effects, an assay was conducted to measure the inhibition of HMG-CoA reductase. The results of membrane stabilization showed IC50 values of 480.96 ± 0.02 and 319.41 ± 0.19 µg/mL for ethyl acetate extract of U. urens and P. chinense, respectively. The standard drug Diclofenac sodium exhibited IC50 value of 240.37 ± 0.04 µg/mL. For protein denaturation, IC50 values were determined as 221.75 ± 0.2 and 315.76 ± 0.19 µg/mL for U. urens and P. chinense, respectively. The IC50 value of the standard drug was calculated as 126.7 ± 0.34. The IC50 values towards HMG-CoA reductase inhibition were subsequently determined as 29.84 ± 0.35 µg/mL for U. urens and 24.34 ± 0.04 µg/mL for P. chinense against the standard drug Diclofenac sodium (7.52 ± 0.43 µg/mL). GC-MS chromatograms revealed the presence of bioactive compounds in ethyl acetate extract of P. chinense leaves. This work is substantiation for the traditional therapeutic utilization of these extracts.

Simultaneous determination of dantrolene with ibuprofen and diclofenac in plasma by HPLC-DAD: Application to comparative pharmacokinetic study

AbstractMuscle relaxants and pain killers with their different types are widely used as combination approach for treatment of pain associated with several muscle spasm conditions. A sensitive and simple HPLC-UV detection method was developed in this work for simultaneous assay of Dantrolene (DNT) and co-administrated: Ibuprofen (IBU) and Diclofenac (DIC). After simple protein precipitation, separation was achieved using C18 column (150 × 4.6 mm) with a mobile phase of acidified water with orthophosphoric acid (pH = 3.5) and acetonitrile using gradient elution with a flow rate of 1 mL/min. The DAD was adjusted at 380, 219, 280 and 240 nm to measure DNT, IBU, DIC, and dexamethasone (internal standard), respectively. Linearity was demonstrated over the range from 0.1 to 3 μg/mL, 1 to 40 μg/mL, and 0.1 to 2 μg/mL for DNT, IBU, and DIC, respectively. The validated method was applied successfully to compare the effect of co-administration of IBU or DIC on the pharmacokinetic profile of DNT.

Breast milk concentrations of acetaminophen and diclofenac - unexpectedly high mammary transfer of the general-purpose drug acetaminophen

BackgroundBreastfeeding is considered to be the most effective way of ensuring the health and survival of newborns. However, mammary transfer of drugs administered to mothers to breastfeeding infants remains a pressing concern. Acetaminophen and diclofenac sodium are widely prescribed analgesics for postpartum pain relief, but there have been few recent reports on the mammary transfer of these drugs, despite advances in analytic techniques.MethodsWe conducted a study on 20 postpartum mothers from August 2019–March 2020. Blood and milk samples from participants were analyzed using liquid chromatography-electrospray ionization tandem mass spectrometry within 24 hours after oral administration of acetaminophen and diclofenac sodium. The area under the concentration-time curve (AUC) was calculated from the concentration curve obtained by a naive pooled-data approach.ResultsFor acetaminophen, AUC was 36,053 ng/mL.h and 37,768 ng/mL.h in plasma and breast milk, respectively, with a milk-to-plasma drug concentration ratio of 1.048. For diclofenac, the AUC was 0.227 ng/mL.h and 0.021 ng/mL.h, in plasma and breast milk, respectively, with a milk-to-plasma drug concentration ratio of 0.093.ConclusionsWhile diclofenac sodium showed low mammary transfer, acetaminophen showed a relatively high milk-to-plasma drug concentration ratio. Given recent studies suggesting potential connections between acetaminophen use during pregnancy and risks to developmental prognosis in children, we believe that adequate information regarding the fact that acetaminophen is easily transferred to breast milk should be provided to mothers.

Designing Advanced Drug Delivery Systems: Core-Shell Alginate Particles through Electro-Fluid Dynamic Atomization.

Innovations in drug delivery systems are crucial for enhancing therapeutic efficiency. Our research presents a novel approach based on using electro-fluid dynamic atomization (EFDA) to fabricate core-shell monophasic particles (CSMp) from sodium alginate blends of varying molecular weights. This study explores the morphological characteristics of these particles in relation to material properties and process conditions, highlighting their potential in drug delivery applications. A key aspect of our work is the development of a mathematical model that simulates the release kinetics of small molecules, specifically sodium diclofenac. By assessing the diffusion properties of different molecules and gel formulations through transport and rheological models, we have created a predictive tool for evaluating the efficiency of these particles in drug delivery. Our findings underscore two critical, independent parameters for optimizing drug release: the external shell thickness and the diffusivity ratios within the dual layers. This allows for precise control over the timing and intensity of the release profile. This study advances our understanding of EFDA in the fabrication of CSMp and offers promising avenues for enhancing drug delivery systems by tailoring release profiles through particle characteristic manipulation.

Antiarthritic and Antioxidant Activities of Antrocaryon micraster Seed Extract and Its Fractions.

Rheumatoid arthritis (RA) is an incurable debilitating disease which attacks the joints and impairs quality of life. Antrocaryon micraster is used to treat RA in African traditional medicine. However, its antiarthritic activity has not been pharmacologically studied. This study, therefore, reports the antiarthritic and antioxidant activities of A. micraster seed extract and its fractions. The seed extract (ASE) was produced by Soxhlet extraction and partitioned into petroleum ether (ASEP), ethyl acetate (ASEE), and aqueous (ASEA) fractions. The total polyphenolic content, DPPH antioxidant activity, and in vitro arthritic activity using the protein denaturation assay were evaluated for ASE and its fractions. The arthritic activity of the crude extract (ASE) and its most effective fraction (ASEA), in the in vitro assay, were then evaluated against CFA-induced arthritis in rats. The polyphenolic constituent of ASE was estimated to be 13.00 ± 0.00 mg/100 mg of GAE. ASEA contained the highest quantity of polyphenolic constituents (10.76 ± 0.00 mg/100 mg of GAE) among the fractions of the extract. ASE and ASEA produced profound antioxidant activity (IC50 = 20.17 ± 1.291 and 19.35 ± 0.865, respectively) which were similar to that of ascorbic acid (IC50 = 17.35 ± 0.500) in the DPPH free radical scavenging assay. Furthermore, in vitro antiarthritic activity of ASEA was 13.63 and 5.75 times higher than the antiarthritic activity of the crude extract and diclofenac sodium, respectively. In the CFA-induced arthritis assay, both ASE and ASEA significantly (P < 0.001) inhibited cachexia, paw edema, infiltration of inflammatory cells, pannus formation, and synovium damage. These results indicate that A. micraster seed extract and its fractions possessed significant antiarthritic activity via inhibition of oxidative stress, inflammation, protein denaturation, infiltration of inflammatory cells, and synovium injury due to its constituents such as polyphenols and phytosterols.