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The presence of pharmaceutical compounds in the environment is a reality that calls for more efficient water treatment technologies. Photocatalysis is a powerful technology available but the high energy costs associated with the use of UV irradiation hinder its large scale implementation. More sustainable and cheaper photocatalytic processes can be achieved by improving the sunlight harvesting and the synthesis of semiconductor/carbon composites has proved to be a promising strategy. Carbamazepine, diclofenac, and sulfamethoxazole were selected as target pharmaceuticals due to their recalcitrant behavior during conventional wastewater treatment and persistence in the environment, as properly reviewed. The literature data on the photocatalytic removal of carbamazepine, diclofenac, and sulfamethoxazole by semiconductor/carbon materials was critically revised to highlight the role of the carbon in the enhanced semiconductor performance under solar irradiation. Generally it was demonstrated that carbon materials induce red-shift absorption and they contribute to more effective charge separation, thus improving the composite photoactivity. Carbon was added as a dopant (C-doping) or as support or doping materials (i.e., nanoporous carbons, carbon nanotubes (CNTs), graphene, and derived materials, carbon quantum dots (CQDs), and biochars) and in the large majority of the cases, TiO2 was the semiconductor tested. The specific role of carbon materials is dependent on their properties but even the more amorphous forms, like nanoporous carbons or biochars, allow to prepare composites with improved properties compared to the bare semiconductor. The self-photocatalytic activity of the carbon materials was also reported and should be further explored. The removal and mineralization rates, as well as degradation pathways and toxicity of the treated solutions were also critically analyzed.

Purpose Individualizing gastric-resistant tablets is associated with major challenges for clinical staff in hospitals and healthcare centres. This work aims to fabricate gastric-resistant 3D printed tablets using dual FDM 3D printing. Methods The gastric-resistant tablets were engineered by employing a range of shell-core designs using polyvinylpyrrolidone (PVP) and methacrylic acid co-polymer for core and shell structures respectively. Filaments for both core and shell were compounded using a twin-screw hot-melt extruder (HME). CAD software was utilized to design a capsule-shaped core with a complementary shell of increasing thicknesses (0.17, 0.35, 0.52, 0.70 or 0.87 mm). The physical form of the drug and its integrity following an FDM 3D printing were assessed using x-ray powder diffractometry (XRPD), thermal analysis and HPLC. Results A shell thickness ≥0.52 mm was deemed necessary in order to achieve sufficient core protection in the acid medium. The technology proved viable for incorporating different drug candidates; theophylline, budesonide and diclofenac sodium. XRPD indicated the presence of theophylline crystals whilst budesonide and diclofenac sodium remained amorphous in the PVP matrix of the filaments and 3D printed tablets. Fabricated tablets demonstrated gastric resistant properties and a pH responsive drug release pattern in both phosphate and bicarbonate buffers. Conclusions Despite its relatively limited resolution, FDM 3D printing proved to be a suitable platform for a single-process fabrication of delayed release tablets. This work reveals the potential of dual FDM 3D printing as a unique platform for personalising delayed release tablets to suit an individual patient’s needs.

Novel formulations and administration routes of established drugs may result in higher maximum concentrations or total exposures and potentially cause previously unrecognized adverse events. This study evaluated the proarrhythmic potential of hydroxypropyl-β-cyclodextrin (HPβCD)-diclofenac, a novel injectable diclofenac formulation solubilized with hydroxypropyl-β-cyclodextrin (HPβCD), on ventricular electrical conduction in preclinical and clinical models. We assessed the effects of diclofenac, HPβCD, and HPβCD-diclofenac on the human delayed rectifier potassium channel (IKr) using human embryonic kidney (HEK) 293 cells transfected with a human ether-à-go-go–related gene (hERG) using whole-cell patch-clamp. In a single-dose, active- and placebo-controlled, 4-period crossover, thorough QT in vivo study, 70 healthy volunteers (mean age, 23.3 years; range, 18–49 years; 55.75% male) received HPβCD-diclofenac at 37.5- and 75-mg doses, inactive vehicle (placebo), and an active control (moxifloxacin). In vitro, diclofenac produced no statistically significant effect on IKr. Significant, non–dose-dependent effects were observed in the presence of HPβCD or HPβCD-diclofenac of similar magnitude across the 300-fold dose range of concentrations tested, suggesting an artifact due to the detergent effect of HPβCD in this in vitro model. In vivo, neither HPβCD-diclofenac dose resulted in QTc prolongation ≥2 ms (≥5 ms is the threshold of clinical concern). No correlation was evident between changes in QTc and plasma concentrations of diclofenac or HPβCD. Confirming study sensitivity, moxifloxacin produced a mean QTc prolongation >10 ms. The findings from the present study suggest that HPβCD-diclofenac does not have a dose-dependent effect in the in vitro hERG assay system and does not produce proarrhythmic QTc prolongation in vivo. ClinicalTrials.gov identifier: NCT01812538.

In this work, a novel nanocomposite containing zeolitic imidazolate framework-67 decorated silica nanoparticles/graphene oxide nanosheets (ZIF-67/SiO 2 NPs/GONs) was synthesized and used for the fabrication of the modified glassy carbon electrode for individual and simultaneous electrodetermination of paracetamol (PAR) and diclofenac (DIC) at trace levels. Structural and morphological characterization of the nanocomposite were carried out using suitable techniques. The modified electrode; ZIF-67/SiO 2 NPs/GONs/GCE, exhibited excellent electrocatalytic activities toward the oxidation of PAR and DIC than the bare GCE, GONs/GCE, SiO 2 NPs/GONs/GCE and ZIF-67/GCE. Through using differential pulse voltammetry, the individual and simultaneous determination of PAR and DIC were conducted by the ZIF-67/SiO 2 NPs/GONs/GCE. Under optimal conditions, it has been observed that the calibration plots for PAR and DIC exhibit linearity within the concentration ranges of 0.5–190 (PAR) and 0.5–200 µM (DIC), with detection limits of 0.29 and 0.132 µM for PAR and DIC, respectively. The ZIF-67/SiO 2 NPs/GONs/GCE shows commendable stability, reproducibility, and repeatability, and the proposed method is evaluated by individual and simultaneous determination of PAR and DIC in real samples with satisfactory results (recovery > 97%).

This study investigated the ability of rhodococci to biodegrade diclofenac (DCF), one of the polycyclic non-steroidal anti-inflammatory drugs (NSAIDs) most frequently detected in the environment. Rhodococcus ruber strain IEGM 346 capable of complete DCF biodegradation (50 µg/L) over 6 days was selected. It is distinguished by the ability to degrade DCF at high (50 mg/L) concentrations unlike other known biodegraders. The DCF decomposition process was accelerated by adding glucose and due to short-term cell adaptation to 5 µg/L DCF. The most typical responses to DCF exposure observed were the changed ζ-potential of bacterial cells; increased cell hydrophobicity and total cell lipid content; multi-cellular conglomerates formed; and the changed surface-to-volume ratio. The obtained findings are considered as mechanisms of rhodococcal adaptation and hence their increased resistance to toxic effects of this pharmaceutical pollutant. The proposed pathways of bacterial DCF metabolisation were described. The data confirming the C-N bond cleavage and aromatic ring opening in the DCF structure were obtained.

The present experimental study reports the performance of tea waste (TW) derived adsorbent for the adsorption of sodium diclofenac (SD) from aqueous solution (SD concentration = 10–50 mg/L). The waste-derived activated carbon was prepared by chemical activation process of raw waste using H 2 SO 4 , KOH, ZnCl 2 , and K 2 CO 3 as activating agents (TW: activating agent = 1:1 by weight). Subsequently, the oven-dried material was carbonized at 600-°C temperature for 2 h. The synthesized adsorbents were porous and their Brunauer-Emmett-Teller (BET) surface area was ranged 115–865 m 2 /g. Among all synthesized adsorbents, the adsorbent activated by ZnCl 2 exhibited the highest adsorption capacity (= 62 mg/g), though it was much lower compared to 91 mg/g obtained with commercial activated carbon (CAC) (SD concentration = 30 mg/L, adsorbent dose = 300 mg/L and initial wastewater pH = 6.47). SD equilibrium data could be described by Langmuir isotherm adequately, while pseudo-second-order rate model showed better fit to the time based adsorption data. Low activation energy of the adsorption process suggests the reaction to be temperature independent. Thermodynamic parameters showed the spontaneous and endothermic nature of adsorption process conducted in the presence of waste derived adsorbent.

Bacterial nanocellulose (BNC) membranes have enormous potential as systems for topical drug delivery due to their intrinsic biocompatibility and three-dimensional nanoporous structure, which can house all kinds of active pharmaceutical ingredients (APIs). Thus, the present study investigated the long-term storage stability of BNC membranes loaded with both hydrophilic and lipophilic APIs, namely, caffeine, lidocaine, ibuprofen and diclofenac. The storage stability was evaluated under accelerated testing conditions at different temperatures and relative humidity (RH), i.e., 75% RH/40 °C, 60% RH/25 °C and 0% RH/40 °C. All systems were quite stable under these storage conditions with no significant structural and morphological changes or variations in the drug release profile. The only difference observed was in the moisture-uptake, which increased with RH due to the hydrophilic nature of BNC. Furthermore, the caffeine-loaded BNC membrane was selected for in vivo cutaneous compatibility studies, where patches were applied in the volar forearm of twenty volunteers for 24 h. The cutaneous responses were assessed by non-invasive measurements and the tests revealed good compatibility for caffeine-loaded BNC membranes. These results highlight the good storage stability of the API-loaded BNC membranes and their cutaneous compatibility, which confirms the real potential of these dermal delivery systems.

Osteoarthritis (OA) remains one of the common degenerative joint diseases and a major cause of pain and disability in older adult individuals. Oral administration of non-steroidal anti-inflammatory drugs (NSAIDs) (such as diclofenac, DIC) or intra-articular injected gluco-corticosteroids (such as dexamethasone, DEX) were the conventional treatment strategies for OA to reduce joint pain. Current limitations for both drugs including severe adverse effects with risks of toxicity were noted. The aim of the present study was to generate a novel OA treatment formulation hyaluronic acid (HA)-Liposomal (Lipo)-DIC/DEX to combat joint pain. The formulation was prepared by constructing DIC with DEX-loaded nanostructured lipid carriers Lipo-DIC/DEX mixed with hyaluronic acid (HA) for prolonged OA application. The prepared Lipo-DIC/DEX nanoparticles revealed the size as 103.6 ± 0.3 nm on average, zeta potential as −22.3 ± 4.6 mV, the entrapment efficiency of 90.5 ± 5.6%, and the DIC and DEX content was 22.5 ± 4.1 and 2.5 ± 0.6%, respectively. Evidence indicated that HA-Lipo-DIC/DEX could reach the effective working concentration in 4 h and sustained the drug-releasing time for at least 168 h. No significant toxicities but increased cell numbers were observed when HA-Lipo-DIC/DEX co-cultured with articular chondrocytes cells. Using live-animal In vivo imaging system (IVIS), intra-articular injection of each HA-Lipo-DIC/DEX sufficed to reduce knee joint inflammation in OA mice over a time span of four weeks. Single-dose injection could reduce the inflammation volume down to 77.5 ± 5.1% from initial over that time span. Our results provided the novel drug-releasing formulation with safety and efficiency which could be a promising system for osteoarthritis pain control.

A novel Schiff base ligand, (E)-2-(2-((2,6-dichlorophenyl)amino)phenyl)-N’-(2-hydroxynaphthalen-1-yl)methylene)acetohydrazide, was synthesized and complexed with Cu(II), Ni(II), Co(II), Gd(III), La(III), and Ag(I) ions. The resulting metal complexes were characterized using FTIR, UV–Vis, 1H NMR, ESR, XRD, thermal analysis, and magnetic susceptibility measurements. Spectroscopic and magnetic data confirmed octahedral geometries for Co(II), Ni(II), and Cu(II), square antiprismatic and tricapped trigonal prismatic geometries for Gd(III) and La(III), respectively, and a tetrahedral geometry for Ag(I). The anti-inflammatory activity was evaluated using ELISA-based COX-1/COX-2 inhibition assays. The HDN ligand exhibited potent COX-2 inhibition (IC₅₀ = 0.06 µM) with a selectivity index (SI) of 174.5, outperforming diclofenac sodium (SI = 4.52) and indomethacin (SI = 1.25), and approaching rofecoxib (SI = 725). The Cu(II) and Gd(III) complexes showed strong cytotoxicity in MTT assays against MCF-7 (IC₅₀ = 0.65 and 0.80 µM) and HepG-2 (IC₅₀ = 1.00 and 2.47 µM) cell lines, significantly surpassing the HDN ligand and standard drugs such as 5-fluorouracil (IC₅₀ = 3.95 µM, MCF-7) and cisplatin (IC₅₀ = 15.24 µM, MCF-7). In silico studies including molecular docking and ADME profiling supported the experimental findings. The HDN ligand and Cu(II) complex exhibited strong binding affinities to COX-2 (− 22.87 kcal/mol), HepG-2 (− 32.56 and − 31.76 kcal/mol), and MCF-7 (− 25.29 and − 20.20 kcal/mol) receptors. SwissADME and BOILED-Egg models predicted high gastrointestinal absorption for the HDN ligand and favorable pharmacokinetic profiles for the metal complexes. The present results provide a preclinical proof-of-concept for diclofenac-derived Schiff base metal complexes as dual anti-inflammatory and anticancer agents. However, their therapeutic potential remains to be validated through stability, mechanistic, and in vivo investigations.

Approximately 3000 pharmaceutical compounds and personal care products (PPCPs) are utilized and discharged into the wastewater at low levels, and they are rarely removed or treated in wastewater treatment facilities. The present study focused on the potential ability of Penicillium aurantiogriseum 2AJS to degrade pharmaceutical and personal care products of different classes of drugs: antipyretic and analgesic drugs (paracetamol, diclofenac, and ibuprofen) and hormones (estrogen, progesterone, and testosterone). Various ligninolytic extracellular enzymatic studies were also studied. A phytotoxicity assay was performed using the Lemna minor species procured from the Vellore Institute of Technology, Vellore. The results revealed degradation of pharmaceutical and personal care products to 95.27% (paracetamol), 94.37% (diclofenac), 89.29% (ibuprofen), 94.16% (progesterone), 91.10% (estrogen), and 82.12% (testosterone). GC–MS and NMR analyses aided in proposing the degradation pathway of all six pharmaceutical compounds. Degradation kinetics showed a first-order model for all the degradation studies with R 2 values ranging between 0.89 and 0.95. A toxicological assay using Lemna minor showed very less toxicity of degraded compounds with a toxicity index ranging between 1.2 and 1.5 compared to the parent compounds. Hence, strain 2AJS can be used in in situ bioremediation of wastewater treatment processes.