Drug Ibuprofen Research Articles

PH-responsive zeolite-A/chitosan nanocarrier for enhanced ibuprofen drug delivery in gastrointestinal systems.

Targeted drug delivery with responsive release is an emerging research area. Along this line, we report herein the fabrication and characterization of zeolite/chitosan (ZA/CS) composite as a pH-responsive drug carrier for ibuprofen. The drug loading and release, along with cytotoxicity, have been examined to assessing the effectiveness of ZA/CS composite as an ibuprofen therapeutic delivery system. The ZA/CS composite demonstrates a drug loading content (DLC) of 1989.13mg/g and an entrapment efficiency content (EEC) of 99.88%, as determined by drug loading. The released ibuprofen demonstrated virtually linear behavior in fluids that simulated the pH values of the gastrointestinal system. The release at pH1.2 reached 55% after 2h. Seven kinetic models were tested to simulate the drug release process. The Ritger-Peppas model was determined to be the most suitable model. The estimated diffusion exponent (n) values were calculated to be 0.863 at pH1.2 and 0.981 at pH7.4, suggesting anomalous or non-Fickian diffusion mechanisms. Importantly, the ZA/CS composite exhibited excellent biocompatibility as demonstrated by a cytotoxicity evaluation using the MTT assay. These unique features render the examined ZA/CS composite a promising candidate for future targeted drug delivery applications.

Ibuprofen reduces inflammation, necroptosis and protects photoreceptors from light-induced retinal degeneration

BackgroundThe retinal degenerative diseases retinitis pigmentosa (RP) and atrophic age- related macular degeneration (AMD) are characterized by vision loss from photoreceptor (PR) degeneration. Unfortunately, current treatments for these diseases are limited at best. Genetic and other preclinical evidence suggest a relationship between retinal degeneration and inflammation. To further explore this relationship, we tested whether Ibuprofen (IBU), an FDA-approved non-steroidal anti-inflammatory drug (NSAID), could promote PR survival and function in a mouse model of light damage (LD)-induced PR degeneration.MethodsLD was induced by exposing mice to 4000 lx of light for 2–4 hours (h). IBU (100 or 200 mg/kg) or vehicle was administered by daily intraperitoneal injection. Retinal structure and function were evaluated by spectral-domain optical coherence tomography (SD-OCT) and electroretinography (ERG). Cell death genes were analyzed at 24 and 72 h after LD using the Mouse Pan-Cell Death Pathway PCR Array (88 genes). The cellular location and protein expression of key necroptosis genes were assessed by immunohistochemistry.ResultsRetinal outer nuclear layer (ONL) thickness in vehicle-injected LD animals was 8.7 ± 0.6% of retinas without LD (p < 0.0001). In IBU 200 mg/kg treated mice, central ONL thickness was 74.9 ± 7.7% of untreated retinas (p < 0.001). A-wave and b-wave ERG amplitudes were significantly preserved in IBU-treated animals. IBU significantly inhibited retinal inflammation. Twenty-four hour after LD, retinal mRNA expression for the inflammatory-factors tumor necrosis factor (Tnf), interleukin-1 beta (Il1B), and C-C motif chemokine ligand 2 (Ccl2) increased by 10-, 17-, and 533-fold, respectively; in IBU-treated animals, the expression levels of these inflammatory factors were not significantly different from no-LD controls. Expression of key necroptosis genes, including Ripk3 and Mlkl, were upregulated in LD vehicle-treated mice, but dramatically reduced to near no LD levels in LD IBU-treated mice. Microglia activation and MLKL protein upregulation were observed primarily in photoreceptors 12 h after LD, as assessed by immunohistochemistry. IBU reduced the upregulation of MLKL protein and microglia migration in the ONL and outer plexiform layer (OPL) of treated retinas.ConclusionsSystemic administration of the anti-inflammatory drug IBU partially protected mouse retinas from light-induced photochemical damage and inhibited both inflammation and the necroptosis cell death pathways. Our results suggest that NSAIDs may provide a promising therapeutic approach for treatment of the human retinal degenerative diseases.

Formulating Single Phasic Silicorhenanite (α- and β-Na2Ca4(PO4)2SiO4) Bioactive Glass Materials Competing with Commercial Crystalline Hydroxyapatite Bone Mineral for Biomedical Applications.

Hydroxyapatite (HAP) is a well-known medically renowned bioactive material known for its excellent biocompatibility and mechanical stability, but it lacks fast bioactivity. The restricted release of ions from hydroxyapatite encourages the search for a faster bioactive material that could replicate other properties of HAP. A new sol-gel-mediated potentially bioactive glass material that could mimic the structure of HAP but can surpass the performance of HAP bioactively has been formulated in this study. Lefebvre et al. suggested that the silicorhenanite phase with the formula Na2Ca4(PO4)2SiO4 is isostructural to hydroxyapatite; however, data in support of this hypothesis are scant. This study succeeds in developing fast apatite-growth-inducing bioactive glass particles similar to the structure of hydroxyapatite. Also, for the first time, the existence and evolution of two forms of silicorhenanite (α- and β-Na2Ca4(PO4)2SiO4) have been unraveled, and their properties have been explored. The effect of calcination temperature on the phase formation of the biomaterial is notified by looking into the result that heat treatment to 900 °C resulted in α-Na2Ca4(PO4)2SiO4 (Sili 900) and 1000 °C yielded β-Na2Ca4(PO4)2SiO4 (Sili 1000). This study conveys a new finding that the hydroxyapatite is isostructural to β-Na2Ca4(PO4)2SiO4 but not to α-Na2Ca4(PO4)2SiO4. Raman spectroscopic analysis proved this structural similarity of Sili 1000 and c-HAP, with relative spectra possessing phosphate bands and the irrelevance of Sili 900 to Sili 1000 and c-HAP. The in vitro MTT assay using NIH 3T3 fibroblasts and in vivo wound healing study confirm the enhanced bioactivity and compatibility of Sili 900 and Sili 1000 compared to c-HAP, favored by the presence of a silica matrix and semicrystallinity. pH analysis proved the rapid ionic leaching out from Sili 900 and Sili 1000 and the faster reactivity of Sili 1000 with the fluid. This rapid burst of ions enhances the clotting ability of the Sili 1000 bioactive material and can be a good ibuprofen drug carrier, which is a potential challenger to hydroxyapatite.

Bilayer TiO2/Mo-BiVO4 Photoelectrocatalysts for Ibuprofen Degradation.

Heterojunction formation between BiVO4 nanomaterials and benchmark semiconductor photocatalysts has been keenly pursued as a promising approach to improve charge transport and charge separation via interfacial electron transfer for the photoelectrocatalytic degradation of recalcitrant pharmaceutical pollutants. In this work, a heterostructured TiO2/Mo-BiVO4 bilayer photoanode was fabricated by the deposition of a mesoporous TiO2 overlayer using the benchmark P25 titania catalyst on top of Mo-doped BiVO4 inverse opal films as the supporting layer, which intrinsically absorbs visible light below 490 nm, while offering improved charge transport. A porous P25/Mo-BiVO4 bilayer structure was produced from the densification of the inverse opal underlayer after post-thermal annealing, which was evaluated on photocurrent generation in aqueous electrolyte and the photoelectrocatalytic degradation of the refractory anti-inflammatory drug ibuprofen under back-side illumination by visible and UV-Vis light. Significantly enhanced photoelectrochemical performance on both photocurrent density and pharmaceutical degradation was achieved for the bilayer structure with respect to the additive effect of the constituent layers, which was related to the improved light harvesting arising from the backscattering by the mesoporous TiO2 layer in combination with the favorable charge transfer at the TiO2/Mo-BiVO4 interface.

Towards targeted cancer therapy: Synthesis, characterization, and biological activity of a new Cu(II)-ibuprofen-2,2'-dipyridylamine metal complex.

This work reports the synthesis of a copper metal complex with the nonsteroidal anti-inflammatory drug (NSAID) ibuprofen, and 2,2'-dipyridylamine employing microwave-assisted synthesis (MWAS). To the best of authors knowledge, this is the first study reporting a NSAID-based complex achieved through MWAS. The coordination compound was characterised by elemental analysis, Fourier transform infrared spectroscopy, thermogravimetry, and ultraviolet-visible spectrophotometry. Additionally, the crystal structure of the copper metal complex was elucidated using single-crystal X-ray diffraction with synchrotron radiation. The compound's interaction with the biomolecules bovine serum albumin (BSA) and calf-thymus DNA (CT-DNA), was assessed through UV-Vis, circular dichroism, and fluorescence spectroscopy. Our findings demonstrate that the metal complex effectively binds to BSA, causing a reduction in its intrinsic fluorescence and α-helical content, and shows a capacity for intercalation between CT-DNA base pairs. Finally, the copper compound exhibited promising in vitro antitumoral activities against human breast cancer cell lines (MCF-7 and MDA-MB-231), as evaluated by MTT (3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide) assay (although a similar cytotoxic effect against a non-tumoral epithelial cancer cell line, MCF-12A, was found), and increased oxidative stress levels as assessed by the TBARS (thiobarbituric acid reactive substances) assay and by evaluating glutathione levels. The results suggest that the metal complex promotes lipid peroxidation by increasing oxidative stress levels, leading to a reduction in viability of the two breast cancer cell lines.

Optimization of a solidified floating organic drop microextraction procedure through an experimental design for the simultaneous determination of four non‐steroidal anti‐inflammatory drugs in river water

AbstractTo simultaneously determine the non‐steroidal anti‐inflammatory drugs ketoprofen, nimesulide, diclofenac and ibuprofen in river water, a simple and cost‐effective solidified floating organic drop microextraction method coupled with high‐performance liquid chromatography was developed. Through multivariate optimization, the variables extracting volume, dispersive volume, sample pH and ionic strength were optimized by a full factorial design 24 and Doehlert matrix. The optimized experimental conditions were 30 μL of extracting solvent (1‐dodecanol), 300 μL of dispersive solvent (acetonitrile) and sample pH of 2. The optimized method showed low limits of detection (0.05 to 0.09 μg L−1), satisfactory recoveries (up to 118%) and enrichment factors ranging from 67 to 197. The optimized method applied in river water samples showed low matrix effects, making it possible to apply this method successfully for the quantification of four NSAIDs in river water samples.

Effect of shockwave therapy on plantar fasciitis in postnatal women: a randomized controlled trial

BackgroundPlantar fasciitis (PF) is a widespread foot issue that can be especially frustrating during pregnancy; it is accompanied by pain in the heel, falling, disability, and reduced quality of life (QoL). This study aimed to explore the efficacy of shockwave therapy (SWT) on PF in postnatal women.Material and methodsForty-four postnatal women with PF were randomly distributed into two groups equal in number. Group (A) was given analgesic drugs (Ibuprofen 200 mg, one tablet/day) and performed plantar fascia-stretching exercises only for 6 weeks, while group (B) followed the same treatment as group (A) plus SWT, twice weekly for 6 weeks. All participating women in both groups were evaluated pre- and post-treatment through the Numeric Pain Rating Scale (NPRS) to evaluate pain intensity levels, the Foot Function Index (FFI) to evaluate foot pain and disability related to PF, and the Six-Minute Walk Test (SMWT) to evaluate the functional exercise capacity and QoL of the affected women.ResultsBoth groups showed significant improvements in all outcomes post-treatment (p = 0.001). Group B demonstrated superior improvements in NPRS (p = 0.001), FFI (p = 0.022), and SMWT (p = 0.001) compared to group A.ConclusionShockwave therapy is a beneficial method for reducing pain intensity, enhancing foot functional level, and improving QoL of postpartum women with plantar fasciitis.

Comparative Evaluation of CyclooxygenaseInhibition Profiles Across Various NSAID Forms and Doses: Implications for Efficacy and Adverse Effects.

Nonsteroidal anti-inflammatory drugs (NSAIDs) are commonly used for pain disorders and exert pharmacological effects by inhibiting cyclooxygenase (COX). Although previous studies have evaluated the COX inhibitory activity and selectivity of NSAIDs, none has compared COX inhibitory concentrations with the plasma concentrations of clinical doses or investigated the efficacy and adverse effects of different dosage forms. Therefore, in this study we evaluated the COX inhibitory activities and inhibition rates of clinical doses of the various NSAID formulations, especially diclofenac sodium. Human blood and the drug (diclofenac sodium, celecoxib, ibuprofen, flurbiprofen, or etodolac) were mixed and incubated, and the supernatant was collected and quantified the COX inhibitory activity of each drug by ELISA. Logistic regression analyses were used to calculate the inhibition rates at maximum plasma drug concentration (Cmax) of clinical doses of marketed formulations. For diclofenac sodium, we also calculated the concentrations at which COX inhibition rates were 50% and 80% (IC50 and IC80). COX-2 inhibition rate at Cmax of clinical doses exceeded 50% except celecoxib 100mg. For diclofenac sodium, the Cmax at the clinical doses of the oral and suppository formulations showed almost complete inhibition of COX-2 and an inhibition rate exceeding IC80 for COX-1. The Cmax at repeated doses of the transdermal formulation showed an inhibition rate above IC80 for COX-2 but below IC80 for COX-1. This result explains why gastrointestinal disorders frequently occur with oral and suppository formulations of diclofenac sodium despite its relatively high COX-2 selectivity. Although the plasma drug concentration of the transdermal formulation is lower than oral and suppository formulations, it has an inhibition rate above IC50 for COX-2, which is required for analgesic efficacy, and has a lower COX-1 inhibition rate than these formulations. The findings explain why the transdermal formulation exerts an analgesic effect despite having a lower Cmax than other diclofenac sodium formulations.

Green synthesis, anti-inflammatory evaluation and molecular docking of novel pyridines via one pot multi-component reaction using ultrasonic irradiation.

In this paper, we present a green application for the synthesis of novel pyridine derivatives 4a-f via one-pot, multicomponent reaction (MCRs) of some aromatic aldehydes 1a-f with malononitrile (2) and N-(4-acetylphenyl)-4-methylbenzenesulfonamide (3) in the presence of ammonium acetate using ultrasonic irradiation (U.S) in an aqueous solvent H2O:EtOH (2:1). The structures of all synthesized pyridines 4a-f were confirmed via elemental analysis and different spectroscopic techniques. This application has many advantages such as avoiding hazardous solvents, excellent yields, inexpensive, simple application, in addition to obtain pure compounds. The anti-inflammatory activity of the newly compounds was examined with the reference drug Ibuprofen. The obtained results showed that most derivatives are promising anti-inflammatory activates. Moreover, compound 4b exhibits the most anti-inflammatory activity with a percentage of inhibition with 51.67% compared with Ibuprofen 53.96%. Furthermore, the newly compounds were studied in their molecular docking simulations against the enzyme Human Cyclooxygenase-2, with Tolfenamic Acid as a reference ligand (PDB ID: 5IKT). Compound 4b demonstrated a robust binding affinity with the target protein 5ikt, evidenced by its binding affinity score of - 11.16 kcal/mol, which is the highest among the studied compounds.

Synthesis of Enantiostructured Triacylglycerols Possessing a Saturated Fatty Acid, a Polyunsaturated Fatty Acid and an Active Drug Intended as Novel Prodrugs.

This report describes the asymmetric synthesis of a focused library of enantiopure structured triacylglycerols (TAGs) comprised of a single saturated fatty acid (C6, C8, C10, C12, C14 or C16), a pure bioactive n-3 polyunsaturated fatty acid (EPA or DHA) and a potent drug (ibuprofen or naproxen) intended as a novel type of prodrug. One of the terminal sn-1 or sn-3 positions of the glycerol backbone is occupied with a saturated fatty, the remaining one with a PUFA, and the drug entity is present in the sn-2 position. This was accomplished by a six-step chemoenzymatic approach starting from enantiopure (R)- and (S)-solketals. The highly regioselective immobilized Candida antarctica lipase (CAL-B) played a crucial role in the regiocontrol of the synthesis. All combinations, a total of 48 such prodrug TAGs, were prepared, isolated and fully characterized, along with 60 acylglycerol intermediates, obtained in very high to excellent yields.

Exploring the enhanced bioactivity and reactivity of novel Fe(III) and Co(II) complexes incorporating sulfadiazine tetradentate ligand: Structural, DFT, molecular docking, and biological applications

This current work presented the synthesis, characterization and bio-evaluation of new Fe(III) (FePSD), and Co(II) (CoPSD) complexes based on N-[4-amino-5-cyano-6-(methylthio)pyridin-2-yl]-3-oxobutanamide in pyridine afford N-(4-amino-5-cyano-6-(methylthio) pyridin-2-yl)-3-oxo-2-([4-(pyrimidin-2-ylsulfamoyl) phenyl]hydrazono) butanamide (PSD). Interestingly, the FePSD and CoPSD complexes exhibit notable stability and solubility in organic solvents, with molar conductivity values of 79.35 Ω−1 cm2 mol−1 for FePSD and 8.89 Ω−1 cm2 mol−1 for CoPSD, indicating a 1:1 electrolytic nature for FePSD and non-electrolytic behavior for CoPSD. FTIR analysis confirmed metal–ligand interactions, as shifts in key bands were observed, while UV–Vis spectra and magnetic moment measurements supported octahedral geometries for both complexes. DFT calculations provided insights into the electronic structure, revealing that CoPSD has higher reactivity and electrophilicity, while FePSD showed moderate reactivity. Thermal and mass spectral analyses further characterized their stoichiometry and stability. The antibacterial and antifungal activities were evaluated against a range of Gram-positive and Gram-negative bacteria and fungal strains. The FePSD and CoPSD complexes demonstrated significantly enhanced antimicrobial efficacy compared to the parent ligand, as evidenced by larger inhibition zones, higher activity indices, and lower minimum inhibition concentrations (MIC). CoPSD exhibited superior antibacterial and antifungal activity compared to FePSD, nearing the effectiveness of standard antibiotics and antifungal drugs. Additionally, the anti-inflammatory potential of these compounds was assessed using the egg albumin denaturation method. Both FePSD and CoPSD showed remarkable inhibition of protein denaturation, surpassing the parent ligand and even outperforming the standard drug Ibuprofen at higher concentrations. The enhancement in biological activity is attributed to the metal chelation effect, which improves cell membrane permeability and reactive oxygen species (ROS) generation. Molecular docking studies further elucidated the binding interactions of PSD, FePSD, and CoPSD with target proteins, revealing stronger hydrophobic interactions and hydrogen bonding in the metal complexes, correlating with their superior biological activity. These findings highlight the potential of FePSD and CoPSD as promising antimicrobial and anti-inflammatory agents.

Comprehensive In Vitro and In Silico Aerodynamic Analysis of High-Dose Ibuprofen- and Mannitol-Containing Dry Powder Inhalers for the Treatment of Cystic Fibrosis.

Background: Cystic fibrosis is a hereditary disease, which causes the accumulation of dense mucus in the lungs accompanied by frequent local inflammation. The non-steroidal anti-inflammatory drug ibuprofen (IBU) and the mucolytic mannitol (MAN) can treat these symptoms. Compared to per os administration, a lower dose of these drugs is sufficient to achieve the desired effect by delivering them in a pulmonary manner. However, it is still a challenge to administer high drug doses to the lungs. We aim to develop two inhaled powder formulations, a single-drug product of MAN and a combined formulation containing IBU and MAN. Methods: MAN was dissolved in an aqueous solution of Poloxamer-188 (POL). In the case of the combined formulation, a suspension was first prepared in a planetary mill via wet milling in POL medium. After the addition of leucine (LEU), the formulations were spray-dried. The prepared DPI samples were analyzed by using laser diffraction, scanning electron microscopy, powder X-ray diffraction, differential scanning calorimetry, density tests, in vitro aerodynamic studies (Andersen Cascade Impactor, Spraytec® device), in vitro dissolution tests in artificial lung fluid, and in silico tests with stochastic lung model. Results: The DPIs showed suitability for inhalation with low-density spherical particles of appropriate size. The LEU-containing systems were characterized by high lung deposition and adequate aerodynamic diameter. The amorphization during the procedures resulted in rapid drug release. Conclusions: We have successfully produced a single-drug formulation and an innovative combination formulation, which could provide complex treatment for patients with cystic fibrosis to improve their quality of life.

Evidence for capture of spin-labeled ibuprofen drug molecules by lipid rafts in model membranes

Lipid rafts are lipid-cholesterol nanostructures thought to exist in cell membranes, which are characterized by higher ordering compared to their surroundings. Ibuprofen and other non-steroidal anti-inflammatory drugs (NSAIDs) have a high affinity for phospholipid membranes and can alter their structure and biological properties. Here we use electron paramagnetic resonance (EPR) in its pulsed electron spin echo (ESE) version to study spin-labeled ibuprofen (ibuprofen-SL) in a raft-mimicking bilayer, which consists of an equimolar mixture of the phospholipids dioleoyl-glycero-phosphocholine (DOPC) and dipalmitoyl-glycero-phosphocholine (DPPC), with cholesterol added in various proportions. ESE decays are sensitive to the presence of low-temperature small-angle orientational motions of molecules − stochastic molecular librations. The data obtained show that in the presence of lipid rafts the temperature dependence of the spin relaxation rate induced by this motion reaches a plateau. This behavior is characteristic of non-cooperative motion of a molecule bound to some structure denser than the rest of the medium. Based on this analogy, the data obtained were interpreted as evidence that ibuprofen-SL molecules are adsorbed on the raft boundaries.

Two birds with one stone: Degradation of pharmaceuticals and elimination of bacteria upon treatment of urban wastewater with a Fenton-like process, based on zero-valent iron at pH 4

ZVI-Fenton, which is the combination of zero-valent iron (metallic Fe) and H2O2 is a relatively cheap advanced oxidation process for the elimination of contaminants from wastewater. Here we experimentally tested the ZVI-Fenton reaction at pH 4 towards two crucial goals in the treatment of secondary (partially treated) urban wastewater: (i) degradation of pharmaceuticals such as anti-inflammatory drugs (ibuprofen) and antibiotics (cefazolin, sulfamethoxazole), and (ii) elimination of a considerable fraction of bacteria through a combination of acidic pH and strongly oxidising conditions. In detail, ZVI-Fenton at pH 4 achieved degradation of both primary contaminants and potentially problematic transformation intermediates. The latter include toxic 4-isobutylacetophenone from ibuprofen and compounds potentially retaining antibiotic properties, namely cefazolin products with an intact β-lactam ring and sulfamethoxazole products retaining the p-amino sulfonic acid moiety. Furthermore, the ZVI-Fenton process significantly lowered the total abundance of bacteria, greatly aiding the final disinfection stage. Overall, both objectives were successfully achieved demonstrating that ZVI-Fenton at pH 4 is an efficient treatment against chemical and microbiological contaminants.

Influence of transition metal (Cu) and rare earth metal (Dy) co-doping on spinel zinc ferrite (Cu0.1Dy0.08Zn0.9Fe1.92O4) for improved photocatalytic degradation of industrial effluents

In the present era, design and development of novel, highly stable, easily and magnetically separable, cost effective, and visible light driven catalytic material for the removal of harmful industrial effluents is of great importance. In this context, facile co-precipitation route was adopted for the synthesis of ZnFe2O4 (ZFO), Cu0.1Zn0.9Fe2O4 (CZFO), Dy0.08ZnFe1.92O4 (DZFO), and Cu0.1Dy0.08Zn0.9Fe1.92O4 (CDZFO) and their fabrication was confirmed by XRD, FTIR, SEM, and UV-Visible spectroscopy. The phase analysis of all designed materials exhibits that there is an increment in the crystallite size of co-doped zinc ferrite (CDZFO) i.e. 11.51 nm as compared to ZFO (10.74 nm), CZFO (10.92 nm), and DZFO (11.41 nm). The optical study shows a significant decrease in bandgap of CDZFO i.e. 1.82 eV as compared to DZFO (1.89 eV), CZFO (2.0 eV), and ZFO (2.14 eV). This decrease in optical bandgap and increase in crystallite size of the CDZFO is due to the quantum confinement effect. The photocatalytic efficiency of pure, doped, and co-doped samples was investigated against organic dye (Congo red), pharmaceutical drug (ibuprofen), and colorless organic compound (benzoic acid). The photocatalytic results reveal that CDZFO showed about ∼90 % degradation of Congo red while ZFO, CZFO, and DZFO showed only 59 %, 70 %, and 79 % respectively. Moreover, CDZFO also showed highest photocatalytic removal efficiency against ibuprofen (88 %) and benzoic acid (74 %) out of all other synthesized materials. The remarkable photodegradation ability of CDZFO for all targeted pollutants could be attributed to the generation of crystal defects in its lattice, its small bandgap, and higher absorption in visible region. Furthermore, the recyclability experiment confirmed the stability and reusability of the prepared sample.

Preparation of Ibuprofen-Loaded Inhalable γCD-MOFs by Freeze-Drying Using the QbD Approach.

Research on cyclodextrin-based metal-organic frameworks (CD-MOFs) is still in its infancy, but their potential for use in drug delivery-expressly in the lung-seems promising. We aimed to use the freeze-drying method to create a novel approach for preparing CD-MOFs. MOFs consisting of γ-cyclodextrin (γCD) and potassium cations (K+) were employed to encapsulate the poorly water-soluble model drug Ibuprofen (IBU) for the treatment of cystic fibrosis (CF). Using the LeanQbD® software (v2022), we designed the experiments based on the Quality by Design (QbD) concept. According to QbD, we identified the three most critical factors, which were the molar ratio of the IBU to the γCD, incubation time, and the percentage of the organic solvent. light-, scanning electron microscope (SEM) and laser diffraction were utilized to observe the morphology and particle size of the samples. In addition, the products were characterized by Differential Scanning Calorimetry (DSC), X-ray Powder Diffraction (XRPD), Fourier Transform Infrared Spectroscopy (FT-IR) and nuclear magnetic resonance spectroscopy (NMR). Based on characterizations, we concluded that a γCD-MOF/IBU complex was also formed using the freeze-drying method. Using formulations with optimal aerodynamic properties, we achieved 38.10 ± 5.06 and 47.18 ± 4.18 Fine Particle Fraction% (FPF%) based on the Andersen Cascade Impactor measurement. With these formulations, we achieved a fast dissolution profile and increased IBU solubility. This research successfully demonstrates the innovative use of freeze-drying to produce γCD-MOFs for inhalable IBU delivery. The method enabled to modify the particle size, which was crucial for successful pulmonary intake, emphasizing the need for further investigation of these formulations as effective delivery systems.

Supercritical carbon dioxide as solvent for manufacturing of ibuprofen loaded gelatine sponges with enhanced performance

Supercritical carbon dioxide was used as the solvent for manufacturing of ibuprofen loaded gelatine sponges with high loading capacity and fast release performance toward healthcare materials in the treatment of postoperative dental pain. The solubility of ibuprofen in supercritical CO2 was first determined at 313 K under different pressure conditions. The micronisation of ibuprofen drugs were successfully adsorbed onto the surface of network pore system of gelatine sponges via supercritical CO₂ processing. The loading capacity of ibuprofen in gelatine sponges obtained by using supercritical CO₂ as the solvent can be up to 19.86 wt%, which was double that of the sample prepared by direct soaking in ethanol. The dissolution of ibuprofen was determined and higher instantaneous dissolution rate was observed for the ibuprofen loaded gelatine sponges synthesized by supercritical CO₂ processing.

Anti-arthritic activity of Trayodashang guggulu, a classical Ayurvedic formulation against complete Freund’s adjuvant-induced rheumatoid arthritis in rats

BackgroundRheumatoid arthritis is a chronic autoimmune disease affecting millions of people across the world. Trayodashang guggulu (TG) is a classical Ayurvedic formulation used for the treating joint diseases since decades in the Indian system of traditional medicine. The aim of the study was to evaluate anti-arthritic activity of TG against complete Freund’s adjuvant-induced arthritis in Wistar rats.MethodsArthritis was induced by single injection of 0.1 ml complete Freund’s adjuvant into the intraplanter surface of left hind paw of Wistar rats. TG was administered orally at the doses of 100, 200, 400 and 800 mg/kg body weight for 14 days. In the preventive dose group, TG was administered at the dose of 100 mg/kg body weight, orally for 28 days. Paw swelling, joint circumference, serum rheumatoid factor, C-reactive protein, serum IL-1β, TNF-α and histopathological parameters were assessed for the evaluation of arthritis. Effects of TG were compared with standard allopathic drug ibuprofen.ResultsTG reversed complete Freund’s adjuvant-induced arthritis in rats when used for 14 and 28 days. Serum rheumatoid factor, C-reactive protein, IL-1β and TNF-α were decreased in rats treated with both standard drug ibuprofen and TG.ConclusionOral administration of TG reduced experimentally induced rheumatoid arthritis in rats by reversing elevated level of serum biochemical markers as well as reducing joint destruction similar to ibuprofen. Results obtained from the study paved the way in exploring more specific mechanisms of action of TG involving in vitro and in silico models.

Analisa mutu tablet ibuprofen generik berlogo dan generik bermerek yang diproduksi industri X di Gresik

Ibuprofen tablets are one of the most widely used antipyretic analgesic drugs for self-medication in pharmacies. According to the Biopharmaceutical Classification System (BCS), Ibuprofen is included in Class II or drugs with low solubility, but high permeability. This study was carried out to determine the physical quality of branded generic and branded generic ibuprofen drugs. This research was carried out by dissolution testing on ibuprofen tablets. The results obtained from the physical quality test met the specified requirements. The dissolution test showed that Q30 had dissolved more than 70%. The conclusion is that the drug meets the requirements and there is no difference between generic drugs with the logo and branded generics.

Amplified pain and complex regional pain syndrome in children: clinical cases and literature review

BACKGROUND: Musculoskeletal pain is a common reason for visiting pediatric clinics. Causes of chronic musculoskeletal pain include various inflammatory or noninflammatory conditions. Amplified pain syndrome refers to a wide range of conditions manifested by chronic pain, the common feature of which is central and/or peripheral sensory amplification of pain. Complex regional pain syndrome is characterized by spontaneously occurring or provoked by irritating stimuli pain of high intensity, disproportionate to the actual injury or other stimulus, and the presence of several concomitant vegetative and motor disorders. CLINICAL CASES: This article presents three clinical cases of pediatric patients with chronic musculoskeletal pain and an analysis of the current literature on chronic pain in children. DISCUSSION: Complex regional pain syndrome is more common in adolescent girls, and conflict or psychological trauma is a common trigger. Symptoms of disproportionate burning pain (causalgia) with trophic changes may indicate complex regional pain syndrome. To date, there are no generally accepted pharmacological treatments recommended for children with complex regional pain syndrome. Nonsteroidal anti-inflammatory drugs (ibuprofen) and paracetamol and their combination are commonly administered in cases wherein symptoms of chronic pain first appear. CONCLUSIONS: Currently, a multidisciplinary approach, including physical, psychological, medical, and invasive methods, appears to be the most adequate treatment method for musculoskeletal pain. The use of analgesics should comply with approved protocols of pain management in pediatric practice.