Anti-inflammatory Diclofenac Sodium Research Articles

Anti-Inflammatory And Immunomodulating Activity of the 1(10) Β-Epoxy-5,7α,6β(Н)-Guai-3(4),11(13)-Dien-6,12-Olide

BACKGROUND: The article discusses the results of studies of the anti-inflammatory and immunomodulatory activity of the sesquiterpene lactone 1(10)β-epoxy-5,7α,6β(Н)-guai-3(4),11(13)-diene-6,12-olide (hereinafter referred to as epoxyguaianolide). AIM: The article discusses the results of studies of the anti-inflammatory and immunomodulatory activity of the sesquiterpene lactone 1(10)β-epoxy-5,7α,6β(Н)-guai-3(4),11(13)-diene-6,12-olide. MATERIALS AND METHODS: A non-steroidal anti-inflammatory drug diclofenac sodium at a dose of 25 mg/kg (ampoules, 2 mL each, manufactured by Germany) was used as a reference drug in models of acute aseptic inflammation and cotton ball granuloma. On the model of cyclophosphamide immunosuppression, the immunomodulator levamisole at a dose of 3 mg/kg, was used as a reference drug. The immunomodulating effect of the test samples was studied on outbred adult male rats and outbred mice. We calculated the arithmetic mean, the mean square error of the arithmetic mean, the significance of the difference between the mean Рt according to the student’s t-test (TTEST), and the significance of the difference in Pf variances according to the Fisher f-test. RESULTS: The results of the experiments indicate the presence of a pronounced immunomodulatory activity in epoxyguaianolide. When interacting with cells of the immune system, epoxyguaianolide activated the studied parameters in animals with immunosuppression, whereas in intact animals, it did not affect the above parameters. On the model of cyclophosphamide immunosuppression, it was found that epoxyguaianolide has a pronounced immunomodulatory effect, manifested in an increase in the number of T-lymphocytes and a subpopulation of theophylline-resistant T-lymphocytes, an increase in the number of theophylline-sensitive T- and B-lymphocytes, activation of phagocytosis processes, and increased cell migration. This action of epoxyguaianolide eliminates the minimal possibility of hyperactivation of the immune system, which is an important condition for its use as an immunotropic agent. CONCLUSIONS: The conducted experiments made it possible to recommend epoxyguaianolide for clinical trials as an immunomodulating agent in the treatment of chronic inflammatory diseases accompanied by secondary immunodeficiencies.

Self-healing hydrogel from poly(aspartic acid) and dextran with antibacterial property for burn wound healing

Designing hydrogel dressing with intrinsic antibacterial property to promote skin injury recovery remains a significant challenge. In this research, poly(aspartic hydrazide) with grafted betaine (PAHB) was designed and reacted with oxidized dextran (OD) to fabricate biodegradable PAHB/OD hydrogel and its application as wound dressing was systematically investigated. The PAHB/OD hydrogels exhibited fast gelation, strong tissue adhesion, preferable mechanical properties and biocompatibility. The grafted betaine endowed the hydrogel with antibacterial property and antibacterial rate enhanced through photothermal performance of composited CuS nanoparticles under near infrared (NIR) radiation. The CuS composited PAHB/OD hydrogel (CuS/hydrogel) with microporous morphology was used as burn wound dressing with loaded anti-inflammatory drug diclofenac sodium (DS) in mouse model. The results showed the DS loaded CuS/hydrogel (CuS@DS/hydrogel) promoted the tissue regeneration and suppressed the inflammatory response. The histological analysis and immunohistochemical expression confirmed the CuS@DS/hydrogel promote angiogenesis of the burn wound by regulating the expression of inflammatory cytokines (IL-6 and CD68) and vascular endothelial growth factor (VEGF). Overall, the CuS@DS/hydrogel hydrogel is a promising candidate as wound dressing due to its tissue adhesive, antioxidant, antibacterial and anti-inflammatory activities.

Magnetic Polysaccharide Mesenchymal Stem Cells Exosomes Delivery Microcarriers for Synergistic Therapy of Osteoarthritis.

Osteoarthritis (OA) is a prevalent degenerative disease that afflicts more than 250 million people worldwide, impairing their mobility and quality of life. However, conventional drug therapy is palliative. Exosomes (Exo), although with the potential to fundamentally repair cartilage, face challenges in their efficient enrichment and delivery. In this study, we developed magnetic polysaccharide hydrogel particles as microcarriers for synergistic therapy of OA. The microcarriers were composed of modified natural polysaccharides, hyaluronic acid (HAMA), and chondroitin sulfate (CSMA), and were generated from microfluidic electrospray in combination with a cryogelation process. Magnetic nanoparticles with spiny structures capable of capturing stem cell Exo were encapsulated within the microcarriers together with an anti-inflammatory drug diclofenac sodium (DS). The released DS and Exo from the microcarriers had a synergistic effect in alleviating the OA symptoms and promoting cartilage repair. The in vitro and in vivo results demonstrated the excellent performance of the microcarrier for OA treatment. We believe this work has potential for Exo therapy of OA and other related diseases.

Programmable Electro-Assembly of Collagen: Constructing Porous Janus Films with Customized Dual Signals for Immunomodulation and Tissue Regeneration in Periodontitis Treatment.

Currently available guided bone regeneration (GBR) films lack active immunomodulation and sufficient osteogenic ability- in the treatment of periodontitis, leading to unsatisfactory treatment outcomes. Challenges remain in developing simple, rapid, and programmable manufacturing methods for constructing bioactive GBR films with tailored biofunctional compositions and microstructures. Herein, the controlled electroassembly of collagen under the salt effect is reported, which enables the construction of porous films with precisely tunable porous structures (i.e., porosity and pore size). In particular, bioactive salt species such as the anti-inflammatory drug diclofenac sodium (DS) can induce and customize porous structures while enabling the loading of bioactive salts and their gradual release. Sequential electro-assembly under pre-programmed salt conditions enables the manufacture of a Janus composite film with a dense and DS-containing porous layer capable of multiple functions in periodontitis treatment, which provides mechanical support, guides fibrous tissue growth, and acts as a barrier preventing its penetration into bone defects. The DS-containing porous layer delivers dual bio-signals through its morphology and the released DS, inhibiting inflammation and promoting osteogenesis. Overall, this study demonstrates the potential of electrofabrication as a customized manufacturing platform for the programmable assembly of collagen for tailored functions to adapt to specific needs in regenerative medicine.

Biomimetic chitosan nanoparticles with simultaneous water lubricant and anti-inflammatory

Rheumatoid arthritis (RA) is a chronic inflammatory immune and lubrication dysfunction disease that causes great damage to the joints. Herein, inspired by the unique biochemistry structure and excellent hydration of chondroitin sulfate (CHI) existing in joint system, one kind of novel polysaccharide nanoparticle lubricant, that is chitosan nanoparticles (CS NPs) grafting CHI (CS-CHI), is synthesized by one-step surface chemistry reaction. CHI with negative charges can form hydration layers on the surface of CS NPs, thus improving the lubricity of nanoparticles. Simultaneously, CS-CHI NPs have effective loading and sustained drug release ability for anti-inflammatory drug diclofenac sodium (DS), along with good biocompatibility. Finally, based on a collagen-induced rat RA model, in vitro animals experimental results indicate that the as-synthesized CS-CHI@DS NPs has obvious inhibitory effects on inflammatory factors and can effectively prevent the damaged cartilage from further destruction.

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).

High adsorption of sodium diclofenac on post-synthetic modified zirconium-based metal-organic frameworks: Experimental and theoretical studies

Water pollution by pharmaceuticals is currently a great concern due to their ecological risks. In this study, zirconium-based metal–organic frameworks (UiO-66-(COOH)2) were used for removal of the nonsteroidal anti-inflammatory drug (NSAID) diclofenac sodium (DCF). They have been synthesized using a hydrothermal method. Copper and iron metal ions were incorporated in the framework using post-synthetic modification techniques to produce UiO-66-(COOCu)2 and UiO-66-(COOFe)2. The resulted MOFs were characterized using X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (FT-IR), scanning/transmission electron microscopy, and Brunauer–Emmett–Teller. The effects of the pH, initial concentration, and adsorption time on the adsorption process of diclofenac were studied. The maximum adsorption capacities obtained on UiO-66-(COOH)2, UiO-66-(COOCu)2, and UiO-66-(COOFe)2 were 480.5, 624.3, and 769.1 mg/g, respectively. The adsorption of diclofenac was found to be better fitted with Langmuir isotherm and pseudo-second-order kinetic models. The adsorption mechanism was investigated using XRD, FT-IR, density functional theory and Monte Carlo simulation, in which the latter method was used to calculate the adsorption energies and determine the possible interactions between diclofenac and the adsorbents. UiO-66-(COOH)2, UiO-66-(COOCu)2, and UiO-66-(COOFe)2 exhibited good recyclability for diclofenac removal, which confirms the sustainability of these materials.

Anti-arthritic effect of chicken embryo tissue hydrolyzate against adjuvant arthritis in rats (X-ray microtomographic and histopathological analysis).

Finding new, safe strategies to prevent and control rheumatoid arthritis is an urgent task. Bioactive peptides and peptide‐rich protein hydrolyzate represent a new trend in the development of functional foods and nutraceuticals. The resulting tissue hydrolyzate of the chicken embryo (CETH) has been evaluated for acute toxicity and tested against chronic arthritis induced by Freund's full adjuvant (modified Mycobacterium butyricum) in rats. The antiarthritic effect of CETH was studied on the 28th day of the experiment after 2 weeks of oral administration of CETH at doses of 60 and 120 mg/kg body weight. Arthritis was evaluated on the last day of the experiment on the injected animal paw using X‐ray computerized microtomography and histopathology analysis methods. The CETH effect was compared with the non‐steroidal anti‐inflammatory drug diclofenac sodium (5 mg/kg). Oral administration of CETH was accompanied by effective dose‐dependent correction of morphological changes caused by the adjuvant injection. CETH had relatively high recovery effects in terms of parameters for reducing inflammation, inhibition of osteolysis, reduction in the inflammatory reaction of periarticular tissues, and cartilage degeneration. This study presents for the first time that CETH may be a powerful potential nutraceutical agent or bioactive component in the treatment of rheumatoid arthritis.

3D printable self-healing hyaluronic acid/chitosan polycomplex hydrogels with drug release capability

Multifunctional printable biomaterials are at the base of advanced biomedical applications. Chitosan (CHI) and hyaluronic acid (HA) allow the development of polycomplex hydrogels with tailorable properties, including self-healing and controlled drug release. This work correlates and optimizes the mucoadhesive, swelling, biodegradation, mechanical and rheological properties of HA/CHI polycomplex hydrogels with synthesis parameters such as polysaccharide content and complexation time, according to the interaction forces established between both polyelectrolytes. Related to these dynamic forces, the self-healing ability of the hydrogels was investigated together with the potential of the HA/CHI polycomplex hydrogels for 3D printing. Finally, their capability to modulate and promote controlled release of a variety of drugs (anionic and anti-inflammatory sodium diclofenac and the neutral antibiotic rifampicin) was demonstrated. Thus, the reported tunable properties, self-repair ability, printability and drug release properties, demonstrate the suitability of HA/CHI hydrogels for advanced biomedical applications.

HSA nanoparticles in drug recognition: mechanistic insights with naproxen, diclofenac and methimazole

Protein-based nanoparticles offer a suitable targeted delivery platform to drugs in terms of biocompatibility, biodegradability and abundance in nature. Physicochemical understanding of drug encapsulation by protein nanoparticles and their impact on protein aggregation is essential. In this work, we have examined quantitative aspects of encapsulation of non-steroidal anti-inflammatory drugs naproxen and diclofenac sodium, and anti-thyroid drug methimazole in nanoparticles of human serum albumin (HSA NPs) by using ultrasensitive calorimetry. Thermodynamic signatures accompanying the interactions revealed that the partitioning of all these drugs in HSA NPs is primarily driven via contributions from desolvation of highly hydrated nanoparticles surface. Furthermore, the effect of these nanoparticles on fibrillation of HSA has also been studied. HSA NPs are determined to be ineffective towards inhibition of fibrillation under employed conditions. However, the extent of inhibition by HSA NPs varies depending upon the structural characteristics of the drugs. Such studies help to gain mechanistic aspects on drug loading into protein-based nanoparticles and are expected to provide useful insights into improving existing nano-drug carriers and their efficiency in preventing protein fibrillation. Communicated by Ramaswamy H. Sarma

Thermosensitive Drug Delivery System SBA-15-PEI for Controlled Release of Nonsteroidal Anti-Inflammatory Drug Diclofenac Sodium Salt: A Comparative Study.

Mesoporous SBA-15 silica material was prepared by the sol–gel method and functionalized with thermosensitive polyethylenimine polymers with different molecular weight (g·mol−1): 800 (SBA-15(C)-800), 1300 (SBA-15(C)-1300) and 2000 (SBA-15(C)-2000). The nonsteroidal anti-inflammatory drug (NSAID) diclofenac sodium was selected as a model drug and encapsulated into the pores of prepared supports. Materials were characterized by the combination of infrared spectroscopy (IR), atomic force microscopy (AFM), transmission electron microscopy (TEM), photon cross-correlation spectroscopy (PCCS), nitrogen adsorption/desorption analysis, thermogravimetry (TG), differential scanning calorimetry (DSC) and small-angle X-ray diffraction (SA-XRD) experiments. The drug release from prepared matrixes was realized in two model media differing in pH, namely small intestine environment/simulated body fluid (pH = 7.4) and simulated gastric fluid (pH = 2), and at different temperatures, namely normal body temperature (T = 37 °C) and inflammatory temperature (T = 42 °C). The process of drug loading into the pores of prepared materials from the diclofenac sodium salt solutions with different concentrations and subsequent quantitative determination of released drugs was analyzed by UV-VIS spectroscopy. Analysis of prepared SBA-15 materials modified with polyethylenimines in solution showed a high ability to store large amounts of the drug, up to 230 wt.%. Experimental results showed their high drug release into the solution at pH = 7.4 for both temperatures, which is related to the high solubility of diclofenac sodium in a slightly alkaline environment. At pH = 2, a difference in drug release rate was observed between both temperatures. Indeed, at a higher temperature, the release rates and the amount of released drug were 2–3 times higher than those observed at a lower temperature. Different kinetic models were used to fit the obtained drug release data to determine the drug release rate and its release mechanism. Moreover, the drug release properties of prepared compounds were compared to a commercially available medicament under the same experimental conditions.

A comparative study on antioxidant, anti‐inflammatory, antimicrobial activities and chemical composition of Pyrus ussuriensis cultivars from northeastern China

Pyrus ussuriensis is the most important cultivated pear in the northeastern, cold areas of China. However, studies on the biological activity of Pyrus ussuriensis fruit are rare in the public domain. The present study compared antioxidant, anti-inflammatory, and antimicrobial activities and chemical composition in tissues from the peel and flesh of nine Pyrus ussuriensis cultivars. The chemical composition differed among cultivars and tissue sources. Phenolics were predominant in peel samples, whereas sugars were predominant in flesh samples. Twenty-one phenolic compounds were identified and quantified, including hydroxycinnamic acids, hydroquinones, flavanols, flavonols, flavones, and anthocyanins (only in peel samples). The total phenolic content ranged between 363.0 and 1734.0 mg kg− 1 FW in the peel and from 28.5 to 182.3 mg kg− 1 FW in the flesh. In addition, cultivars with high total phenolic and flavonoid contents had significantly higher antioxidant activities. The in vitro anti-inflammatory study, performed using an egg albumin denaturation assay, demonstrated that both peel and flesh samples had strong activity, which was comparable with that of the standard anti-inflammatory drug diclofenac sodium. The antimicrobial results showed that ‘Jianba’ and ‘Balixiang’ cultivars exhibited strong activity against bacteria strains in the peel and flesh, respectively. The present study provided information for selecting promising Pyrus ussuriensis cultivars with improved health benefits.

Gelatin-based composite hydrogels with biomimetic lubrication and sustained drug release

The occurrence of osteoarthritis is closely related to progressive and irreversible destruction of the articular cartilage, which increases the friction significantly and causes further inflammation of the joint. Thus, a scaffold for articular cartilage defects should be developed via lubrication restoration and drug intervention. In this study, we successfully synthesized gelatin-based composite hydrogels, namely GelMA-PAM-PMPC, with the properties of biomimetic lubrication and sustained drug release by photopolymerization of methacrylic anhydride modified gelatin (GelMA), acrylamide (AM), and 2-methacryloyloxyethyl phosphorylcholine (MPC). Tribological test showed that the composite hydrogels remarkably enhanced lubrication due to the hydration lubrication mechanism, where a tenacious hydration shell was formed around the zwitterionic phosphocholine headgroups. In addition, drug release test indicated that the composite hydrogels efficiently encapsulated an anti-inflammatory drug (diclofenac sodium) and achieved sustained release. Furthermore, the in vitro test revealed that the composite hydrogels were biocompatible, and the mRNA expression of both anabolic and catabolic genes of the articular cartilage was suitably regulated. This indicated that the composite hydrogels could effectively protect chondrocytes from inflammatory cytokine-induced degeneration. In summary, the composite hydrogels that provide biomimetic hydration lubrication and sustained local drug release represent a promising scaffold for cartilage defects in the treatment of osteoarthritis.

Histopathological aspects of co-administration of dexamethasone and diclofenac sodium on male albino rats

Background and objective: Treatment of an animal with dexamethasone will result in sinuses extension, fat accumulation in the liver, and enlargement of hepatocytes. Whereas, non-steroidal anti-inflammatory drugs (diclofenac sodium) administration may lead to degeneration and formation of wide areas in the form of sinusoidal. Hydropic degeneration possibly is seen in the tubular epithelial cells of the kidney tissue. This study aimed to assess the toxic and side effects of dexamethasone and diclofenac sodium on the liver and kidney in rats, whether used separately or together. Methods: A total of 40 male albino rats were divided into four groups of ten in each, including the control group. One set was treated with dexamethasone (1.6 mg/kg/day), the other was treated with diclofenac sodium (30 mg /kg/day), and the last was treated with both drugs together at the same dose without mixture. Both drugs were administered intramuscularly for 30 days. Sections from the liver and kidney were stained by Hematoxeline and Eosin, then examined under a microscope. Results: Histopathological variation in the liver and kidney tissue of the treated animals have revealed that each drug (dexamethasone, diclofenac sodium) showed a significant alteration. Strong changes (+ + +) were observed in kidney tissue include degeneration, inflammatory aggregation, fibrosis, and edema, whereas in liver showed central vein dilatation, necrosis, and kupffer cells hyperplasia. Treating with the two drugs together, less alteration (+) in the tissues was noticed. Conclusion: The effect of both used drugs (dexamethasone and diclofenac sodium) was observed on the liver and kidney tissues of the experimental animals (rats) regardless of being applied separately or the two together. A probable inhibition role of the two drugs on each other have been noticed that lead to call for more detail investigation on this matter in years to come.

UV Spectroscopic Method for Optimization and Determination of Glibenclamide in Bulk, Pharmaceutical Dosage Form and its Application for In Vitro Interaction Studies

A simple, easy and cost-efficient UV spectroscopic method was developed and validated for glibenclamide, the second generation of sulfonylureas, using 0.1 N NaOH as a solvent. The proposed method is linear (R2 > 0.999) with the range 5–25 µg mL−1, accurate (99.60%), precise (inter and intraday variation 0.241 and 0.019%, respectively) and robust (< 1%). The quantification and detection limit were 1.46 and 0.48 μg mL−1, respectively. The validated method was applied for in vitro interaction studies of glibenclamide (GLB) with commonly prescribed quinolones (ciprofloxacin, levofloxacin, moxifloxacin, and gemifloxacin) and nonsteroidal anti-inflammatory drugs (NSAIDs) (diclofenac sodium, ibuprofen, mefenamic acid, and aspirin) using UV spectrophotometer. The in vitro interaction studies were carried out in different artificially prepared physiological buffers at 37 °C for 2 h. Results showed raised level of glibenclamide when interacted with gemifloxacin (pH 7.4), levofloxacin (pH 9), ciprofloxacin (pH 4.5) and with moxifloxacin (pH 4.5, 7.4 and 9). Interaction with NSAIDs results in increased %availability of glibenclamide in the presence of diclofenac sodium, ibuprofen, and mefenamic acid at pH 4.5. The anticipated method can be successfully applied for the routine analysis and also for the interaction of glibenclamide with other drugs.

Ionisable substances chromatography: A new approach for the determination of Ketoprofen, Etoricoxib, and Diclofenac sodium in pharmaceuticals using ion – pair HPLC

An ion-pair HPLC method was developed and validated to analyze three of non-steroidal anti-inflammatory drugs (Ketoprofen, Etoricoxib, and Diclofenac sodium) in their pure and pharmaceuticals based on their ionisable characteristics. Cetyltrimethylammonium bromide (Cetrimide) was used as an ion pair reagent since it had not been used before for this purpose. Chromatographic analysis was accomplished using the C18 (250 × 4.6 mm, 5μm) column. Mobile phase consisted of a mixture of 50% Cetrimide10−3 M and 50% acetonitrile to analyze Ketoprofen and Etoricoxib, whereas for Diclofenac sodium, mobile phase was a mixture of 30% Cetrimide10−3 M and 70% acetonitrile. pH value was adjusted if necessary to 10 with ammonium hydroxide. The flow rate was 1mL/min and detection wavelengths were at 254 nm, 234 nm, and 254 nm for Ketoprofen, Etoricoxib, and Diclofenac sodium; respectively under ambient temperature. Retention times (Rt) were 9.41, 7.34, and 6.66 for Ketoprofen, Etoricoxib, and Diclofenac sodium; respectively. The proposed method was evaluated for linearity, accuracy, precision, and specificity according to ICH guidelines. Ketoprofen, Etoricoxib, and Diclofenac sodium were detected in the following linear ranges: (0.031–0.500mg/mL), (0.007–0.110g/mL), and (0.016–0.250mg/mL); respectively with excellent mean recovery values (98.0–102.0%). RSD% was in an acceptable range (less than 2), proving the precision of the developed method. Specificity was proved in the presence of degradation products. Furthermore, a comparison between the results of this study and the reported HPLC methods indicated that this developed method was better in terms of simplicity, analysis time, and no use of buffers in the mobile phase. In conclusion, the developed method can successfully detect Ketoprofen, Etoricoxib, and Diclofenac sodium quantitatively and qualitatively in their dosage forms without any interference with excipients, making this method valuable, reliable, and practical to be applied in quality control laboratories.

Thermo-Sensitive Dual-Functional Nanospheres with Enhanced Lubrication and Drug Delivery for the Treatment of Osteoarthritis.

Osteoarthritis is a typical degenerative joint disease related to a lubrication deficiency of articular cartilage, which is characterized by increased friction at the joint surface and severe inflammation of the joint capsule. Consequently, therapies combining lubrication restoration and drug intervention are regarded as a promising strategy for the treatment of osteoarthritis. In the present study, thermo-sensitive dual-functional nanospheres, poly[N-isopropylacrylamide-2-methacryloyloxyethyl phosphorylcholine] (PNIPAM-PMPC), are developed through emulsion polymerization. The PNIPAM-PMPC nanospheres could enhance lubrication based on the hydration lubrication mechanism by forming a tenacious hydration layer surrounding the zwitterionic headgroups, and achieve local drug delivery by encapsulating the anti-inflammatory drug diclofenac sodium. The lubrication and drug release tests showed improved lubrication and thermo-sensitive drug release of the nanospheres. The in vitro test using cytokines-treated chondrocytes indicated that the PNIPAM-PMPC nanospheres were biocompatible and upregulated anabolic genes and simultaneously downregulated catabolic genes of the articular cartilage. In summary, the developed PNIPAM-PMPC nanospheres, with the property of enhanced lubrication and local drug delivery, can be an effective nanomedicine for the treatment of osteoarthritis.

Multiple Hydrogen Bonds-Reinforced Hydrogels with High Strength, Shape Memory, and Adsorption Anti-Inflammatory Molecules.

The research on multiple hydrogen bonds (H-bonds) hydrogels have gradually aroused wide interest. In this paper, a multiple H-bonds-reinforced poly(acrylamide-co-2-vinyl-4,6-diamino-2-vinyl-1,3,5-triazine)/tannic acid (P(Am-co-VDT)/TA) hydrogels are prepared. The results suggest that the prepared hydrogel has two types of H-bonds crosslinking regions: A "soft" region of H-bonds between the diaminotriazine (DAT) moieties on the polymer chains and the TA pyrogallol/catechol groups, and a "hard" region of H-bonds forming by DAT moieties with itself. The hard crosslinking region exhibits significantly higher activation energy than the soft region. Such soft and hard dual physically crosslinked networks dramatically enhance the mechanical properties of P(Am-co-VDT)/TA hydrogels in a synergistic manner (tensile strength is 2.34MPa, elongation at break is 410%). Due to the multiple hydrogen bonds, the hydrogel has good pH sensitivity and rapid response to shape memory within a few minutes. In addition, the hydrogels have the capacity of physical adsorption of the anti-inflammatory drug diclofenac sodium and other molecules with a specific spatially arranged chemical composition. These hydrogels with high mechanical strength, excellent shape memory behavior, and capacity of adsorption of anti-inflammatory drug could be attractive candidates for applications in the fields of biomedicine, tissue engineering, and medical materials.

Adult post-tonsillectomy pain management: Opioid versus non-opioid drug comparisons

Objective: The primary purpose of this retrospective study was to determine if a non-steroidal anti-inflammatory drug (diclofenac sodium) plus acetaminophen was as effective as alternative opioid drug regimens, +/- ibuprofen and acetaminophen, for pain management in adults following tonsillectomy. Study design: Retrospective study. Setting: 4 hospitals in Michigan associated with the Detroit Medical Center. Subjects and methods: Medical records of adult tonsillectomy patients (age 18 to 50 Years) were reviewed. The incidences of unscheduled post-operative visits to either the ER or ENT clinic for uncontrolled throat pain and/or postoperative bleeding complications were reviewed.

Synthesis and biological activity evaluation of new thiazolidinone-diclofenac hybrid molecules

A novel series of [2-(2,6-dichlorophenylamino)-phenyl]-acetic acid N`-3-(substituted)-4-thiazolidin-5-ylidenemethyl-hydrazide derivatives has been designed and synthesized. The structures of synthesized compounds were confirmed by their 1H NMR, 13C NMR and LCMS spectroscopic data. Target compounds were screened for their in vitro anticancer activity according to US NCI protocols, in vitro trypanocidal activity toward Trypanosoma brucei brucei (Tbb) and evaluated for anti-inflammatory activity on the carrageenan edema model in rats. Biological screening data led to identification of compounds 3.3 ([2-(2,6-dichloro-phenylamino)-phenyl]-acetic acid N`-(4-oxo-2-thioxo-thiazolidin-5-ylidenemethyl)-hydrazide) and 3.7 ([2-(2,6-dichloro-phenylamino)-phenyl]-acetic acid N`-(4-oxo-2-thioxo-3-(3-trifluoromethylphenyl)thiazolidin-5-ylidenemethyl)-hydrazide) which demonstrated moderate antitumor activity on the non-small-cell lung cancer NCI-H522 and colon cancer HCT-116 cell lines. Several hit compounds (3.2, 3.4) exhibited the promising and significant inhibition growth of the parasites at micromolar concentrations (IC50 values of 4.8 and 7.06 μM, respectively). The synthesized compounds also demonstrated considerable anti-inflammatory effect comparable to the reference non-steroidal anti-inflammatory drugs (NSAIDs) diclofenac sodium or ketorolac tromethamine.