Catalytic Degradation of Ciprofloxacin in Aqueous Solution by Peroxymonosulfate Activated with a Magnetic CuFe2O4@Biochar Composite.

A magnetic copper ferrite and biochar composite (CuFe2O4@BC) catalyst was prepared by an improved sol-gel calcination method and initially used for the removal of antibiotics ciprofloxacin (CIP) by activated peroxymonosulfate (PMS). Using CuFe2O4@BC as the activator, 97.8% CIP removal efficiency could be achieved in 30 min. After a continuous degradation cycle, CuFe2O4@BC catalyst still exhibited great stability and repeatability and could also be quickly recovered by an external magnetic field. Meanwhile, the CuFe2O4@BC/PMS system presented good stability for metal ion leaching, which was far less than the leaching of metal ions in the CuFe2O4/PMS system. Moreover, the effects of various influencing factors, such as initial solution pH, activator loading, PMS dosage, reaction temperature, humic acid (HA), and the inorganic anions were explored. The quenching experiments and the electron paramagnetic resonance (EPR) analysis manifested that hydroxyl radical (•OH), sulfate radical (SO4•-), superoxide radical (O2•-), and singlet oxygen (1O2) were generated in the CuFe2O4@BC/PMS system, while 1O2 and O2•- are mainly involved in the degradation process. The synergistic effect between CuFe2O4 and BC enhanced the structural stability and electrical conductivity of the material, which promoted the bonding between the catalyst and PMS, resulting in the enhanced catalytic activity of CuFe2O4@BC. This indicates that CuFe2O4@BC activating PMS is a promising remediation technique for CIP-contaminated water.

Ocular Cubosome Drug Delivery System for Timolol Maleate: Preparation, Characterization, Cytotoxicity, Ex Vivo, and In Vivo Evaluation.

Glaucoma is an ocular disease featuring increased intraocular pressure (IOP) and its primary treatment strategy is to lower IOP by medication. Current ocular drug delivery in treating glaucoma is confronting a variety of challenges, such as low corneal permeability and bioavailability due to the unique anatomical structure of the human eye. To tackle these challenges, a cubosome drug delivery system for glaucoma treatment was constructed for timolol maleate (TM) in this study. The TM cubosomes (liquid crystalline nanoparticles) were prepared using glycerol monooleate and poloxamer 407 via high-pressure homogenization. These constructed nanoparticles appeared spherical using transmission electron microscopy and had an average particle size of 142 nm, zeta potential of -6.27 mV, and over 85% encapsulation efficiency. Moreover, using polarized light microscopy and small-angle X-ray scattering (SAXS), it was shown that the TM cubosomes have cubic liquid crystalline D-type (Pn3m) structure, which provides good physicochemical stability and high encapsulation efficiency. Ex vivo corneal permeability experiments showed that the total amount of TM cubosomes penetrated was higher than the commercially available eye drops. In addition, in vivo studies revealed that TM cubosomes reduced the IOP in rabbits from 27.8∼39.7 to 21.4∼32.6 mmHg after 1-week administration and had a longer retention time and better lower-IOP effect than the commercial TM eye drops. Furthermore, neither cytotoxicity nor histological impairment in the rabbit corneas was observed. This study suggests that cubosomes are capable of increasing the corneal permeability and bioavailability of TM and have great potential for ocular disease treatment.

[Preparation and release behaviour of mesoporous silica/ethylcellulose sustained-release mini-matrix].

Hot-melt extrusion was applied to prepare mesoporous silica/ethylcellulose mini-matrix for sustained release, and fenofibrate was used as a model drug, ethylcellulose and xanthan gum were chosen as sustained-release agent and releasing moderator, respectively. This novel matrix obtained the controlled release ability by combining mesoporous silica drug delivery system and hot-melt extrusion technology. And mesoporous silica particle (SBA-15) was chosen as drug carrier to increase the dissolution rate of fenofibrate in this martix. Scanning electron microscope, transmission electron microscope, small angle X-ray powder diffraction and N2 adsorption-desorption were introduced to determine the particle morphology, particle size and pore structure of the synthesized SBA-15. The results showed that SBA-15 had a very high Brunauer-Emmett-Teller specific surface area, a narrow pore size distribution, large pore volume and a ordered two-dimensional hexagonal structure of p6mm symmetry. Differential scanning calorimetry and X-ray powder diffraction results demonstrated that fenofibrate dispersed in an amorphous state inside the pores of the mesoporous silica which contributed to the improvement in the dissolution rate. The drug release of mini-matrices was influenced by ethylcellulose viscosity grades and xanthan gum concentration, which increased with the increasing of xanthan gum concentration and decreasing of ethylcellulose viscosity. Mini-matrix containing 22% xanthan gum exhibited a good sustained release performance, and the drug release behavior followed the first-order kinetics.

Activation of peroxymonosulfate by pyrophosphate for the degradation of AO7 at neutral pH.

In the present study, pyrophosphate (PP) was used to activate peroxymonosulfate (PMS) for acid orange 7 (AO7) removal under neutral pH conditions. The removal rate of AO7 (20 mg/L) was 84% within the reaction time with a rate constant value of 0.0165 min-1 under optimum conditions. Additionally, the effects of the concentrations of PMS and PP in solutions with various pH values and the coexisting inorganic anions on AO7 removal were measured. In addition, the performance of phosphate (P(V)) on PMS activation was compared with that of phosphite (P(III)) species. In contrast to P(III), the concentration of P(V) showed a positive correlation with the efficiency of AO7 decolorization. PMS activation in different types of buffer solutions was also examined, and the results indicated that the decolorization efficiency of AO7 induced by PP addition, and the buffer solution also contributed to PMS self-decomposition. Singlet oxygen (1O2) might be the primary reactive oxygen species (ROS) in the PP/PMS system in which AO7 is decolorized at an initial pH of 7.06, as indicated by quenching experiments and electron spin resonance (ESR) tests. Therefore, PP/PMS systems may be promising technologies for removing organic contaminants, particularly for PP-rich electroplating wastewater.

New cadinane sesquiterpenoids from Mikania micrantha.

Chemical investigation of the aerial parts of Mikania micrantha led to the isolation of eight sesquiterpenoids and ten diterpenoids, including five cadinane sesquiterpenoids (1-5), three bisabolene sesquiterpenoids (6 - 8), nine ent-kaurane diterpenoids (9-17), and an abietane diterpenoid (18). Among them, 1 - 3 are new and feature a rare lactone or furan ring derived from C-6 isopropyl group side chain. Compound 18 was isolated from genus Mikania for the first time, and was also the first example of abietane-type diterpenoids from this plant. Their structures were elucidated on the basis of extensive spectroscopic analyses (1D and 2D NMR, HRESIMS, and ECD). All compounds were examined for their inhibitory effects on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7 macrophage cells, and compound 18 exhibited pronounced inhibition on NO production (IC50 = 11.04 µM), being comparable to the positive control, quercetin (IC50 = 11.15 µM).

Thermo-sensitive gel in glaucoma therapy for enhanced bioavailability: In vitro characterization, in vivo pharmacokinetics and pharmacodynamics study.

AIMS: Glaucoma is a chronic ophthalmic disease, which has become one of the leading causes to progressive and irreversible blindness. Current ophthalmic drug delivery to treat glaucoma is mostly eyedrop, whose rapid elimination on corneal surface can lead to poor bioavailability. The present study was aimed to develop a timolol maleate loaded thermo-sensitive gel (TM-TSG) with improved bioavailability to treat glaucoma. MAIN METHODS: TM-TSG was prepared by homogeneously dispersing 0.3% (w/v) timolol maleate, 24.25% (w/v) poloxamer 407 (P407) and 1.56% (w/v) poloxamer 188 (P188) into phosphate buffer solution (pH = 7.4) and the formulated TM-TSG was characterized. KEY FINDINGS: TM-TSG was stored in liquid form at room temperature (25 °C) and transited to semisolid gel at physiological temperature (32 °C). The rheological property of TM-TSG was in favor of uniform distribution of drug. TM-TSG showed good stability at different conditions including centrifugation, autoclaving and different temperature. In vivo pharmacokinetic studies indicated that TM-TSG could enhance absorption of TM in aqueous humor and improve the ocular bioavailability in comparison of commercial TM eyedrops. In vivo experiment result showed that TM-TSG had greater effect in treating glaucoma than TM eyedrops by sustainably lowering intraocular pressure (IOP) for a week. Moreover, slit lamp test and histopathological analysis demonstrated that TM-TSG had excellent biocompatibility. SIGNIFICANCE: TM-TSG could be a promising ophthalmic delivery system for glaucoma therapy.

Accurate high-throughput identification of parallel G-quadruplex topology by a new tetraaryl-substituted imidazole.

G-quadruplex nucleic acids are four-stranded DNA or RNA secondary structures that are formed in guanine-rich sequences. These structures exhibit extensive structural polymorphism and play a pivotal role in the control of a variety of cellular processes. To date, diverse approaches for high-throughput identification of G-quadruplex structures have been successfully developed, but high-throughput methods for further characterization of their topologies are still lacking. In this study, we report a new tetra-arylimidazole probe psIZCM-1, which was found to display significant and distinctive changes in both the absorption and the fluorescence spectra in the presence of parallel G-quadruplexes but show insignificant changes upon interactions with anti-parallel G-quadruplexes or other non-quadruplex oligonucleotides. In view of this dual-output feature, we used psIZCM-1 to identify the parallel G-quadruplexes from a large set of 314 oligonucleotides (including 300 G-quadruplex-forming oligonucleotides and 14 non-quadruplex oligonucleotides) via a microplate reader and accordingly established a high-throughput method for the characterization of parallel G-quadruplex topologies. The accuracy of this method was greater than 95%, which was much higher than that of the commercial probe NMM. To make the approach more practical, we further combined psIZCM-1 with another G-quadruplex probe IZCM-7 to realize the high-throughput classification of parallel, anti-parallel G-quadruplexes and non-quadruplex structures.