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EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES · 2022 · IF 5.112

Effect of polyethylene glycol 400 on the pharmacokinetics and tissue distribution of baicalin by intravenous injection based on the enzyme activity of UGT1A8/1A9

Le-Yuan Shang,Ming-Hao Zhou,Si-Yuan Cao,Min Zhang,Peng-Jiao Wang,Shuo Zhang,Xiao-Xia Meng,Qi-Mei Yang,Xiu-Li Gao

Baicalin (BG) is a bioactive flavonoid extracted from the dried root of the medicinal plant, Scutellaria radix (SR) (dicotyledonous family, Labiatae), and has several biological activities. Polyethylene glycol 400 (PEG400) has been used as a suitable solvent for several traditional Chinese medicines (TCM) and is often used as an excipient for the compound preparation of SR. However, the drug–excipient interactions between BG and PEG400 are still unknown. Herein, we evaluated the effect of a single intravenous PEG400 administration on the BG levels of rats using pharmacokinetic and tissue distribution studies. A liver microsome and recombinant enzyme incubation system were used to further confirm the interaction mechanism between PEG400 and UDP-glucuronosyltransferases (UGTs) (UGT1A8 and UGT1A9). The pharmacokinetic study demonstrated that following the co-intravenous administration of PEG400 and BG, the total clearance (CL z ) of BG in the rat plasma decreased by 101.60% ( p < 0.05), whereas the area under the plasma concentration-time curve (AUC) 0-t and AUC 0-inf increased by 144.59% ( p < 0.05) and 140.05% ( p < 0.05), respectively. Additionally, the tissue distribution study showed that the concentration of BG and baicalein-6-O-β-D-glucuronide (B6G) in the tissues increased, whereas baicalein (B) in the tissues decreased, and the total amount of BG and its metabolites in tissues altered following the intravenous administration of PEG400. We further found that PEG400 induced the UGT1A8 and UGT1A9 enzyme activities by affecting the maximum enzymatic velocity (V max ) and Michaelis–Menten constant (K m ) values of UGT1A8 and UGT1A9. In conclusion, our results demonstrated that PEG400 interaction with UGTs altered the pharmacokinetic behaviors and tissue distribution characteristics of BG and its metabolites in rats.

CAS / MDL: 27061-78-5
✓ 已验证 产品关联 DOI PubMed 高影响因子
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International Journal of Nanomedicine · 2022 · IF 7.033

Poly(ε-Caprolactone)-Methoxypolyethylene Glycol (PCL-MPEG)-Based Micelles for Drug-Delivery: The Effect of PCL Chain Length on Blood Components, Phagocytosis, and Biodistribution.

Zemin Hou,Wencheng Zhou,Xi Guo,Rui Zhong,Ao Wang,Jiehua Li,Ying Cen,Chao You,Hong Tan,Meng Tian

Background The main challenge of polymeric micelles as drug delivery systems is that the actual delivery efficiency is not as high as expected, which is closely related with the interactions with the complex biological environments such as blood components, phagocytosis, and biodistribution. Herein, we expect to understand these concerns for the clinically relevant micelles that composed of methoxypolyethylene glycol (MPEG) with identical chain length And poly(ε-caprolactone) (PCL) with tunable chain length (PCL n -MPEG) (n=20, 30, and 40) wherein doxorubicin was encapsulated as a model drug. Methods The doxorubicin-loaded PCL n -MPEG micelles were prepared by a dialysis method and characterized by dynamic light scattering and transmission electron microscopy. The surface PEG density and chain conformation were investigated by dissipative particle dynamics simulation. The stability of the micelles was detected by nanoparticle tracking analysis. The effects of PCL chain length on the blood components, phagocytosis, and biodistribution were assayed in vitro and in vivo. Results The micelles exhibited spherical morphology with a diameter about 30nm. The PEG chain conformation from "mushroom-like" to "brush-like" was evident. The micelles have no remarkable effect on the red blood cells, blood coagulation, and platelet activation. Interestingly, the protein adsorption was affected and dependent on the chain conformation, with lowest adsorption for PCL 30 -MPEG, which also has the loWest phagocytosis. The stability of the micelles was in the order of PCL 40 -MPEG>PCL 30 -MPEG>PCL 20 -MPEG which was dependent on the PCL chain length. The micelles mainly accumulated in liver, with the order consistent with their stability, indicating that, besides the phagocytosis, the stability of the micelle plays an important role in biodistribution as well. The related mechanisms were proposed and discussed. Conclusion Manipulating the PEG/PCL ratio of the micelle is an effective approach to modulate the protein adsorption, phagocytosis, and biodistribution, which may be a prerequisite for clinical applications.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF CHEMICAL THERMODYNAMICS · 2021 · IF 3.178

Liquid-liquid equilibrium data measurement and thermodynamic modelling for ternary mixtures composed of water, diethylene glycol dimethyl ether and different solvents at 298.2 K

Yueyang Jiang,Song Lin,Houchun Yan,Hongyue Guo,Qingsong Li

Liquid-liquid equilibrium (LLE) data for water + diethylene glycol dimethyl ether + {methyl isobutyl carbinol, methyl isobutyl ketone, methyl isopropyl ketone, methyl tert -butyl ether, n -octanol and 2-ethyl-1-hexanol} was measured at 298.2 K under 101.3 kPa. The effect of separating diethylene glycol dimethyl ether from water is evaluated by the distribution coefficient and the separation coefficient. The Othmer-Tobias and Hand equations were chosen to examine the experimental LLE data. Meanwhile, the data was correlated by the NRTL and UNIQUAC thermodynamic models with AAD % less than 0.55 and RMSD % less than 0.77. The separation performance of six solvents was compared using the σ -profile analysis via the exploration of the intermolecular interaction.

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SENSORS AND ACTUATORS B-CHEMICAL · 2020 · IF 7.1

Polyacrylic acid/polyethylene glycol hybrid antifouling interface for photoelectrochemical immunosensing of MDA-MB-231 cells using BiOBr/FeTPPCl/BiOI co-sensitized composite as matrix

Xin Liu,Dawei Fan,Chenchen Zhang,Xinrong Shao,Hongmin Ma,Yong Zhang,Xueying Wang,Qin Wei,Huangxian Ju

An ultrasensitive photoelectrochemical (PEC) antifouling immunosensor was proposed using BiOBr/FeTPPCl/BiOI as matrix and polyacrylic acid (PAA)/polyethylene glycol (PEG) as hybrid antifouling interface for MDA-MB-231 detection. An indium tin oxide (ITO) electrode was successively modified with bismuth oxybromide (BiOBr) with layered crystal structure, which was sensitized with tetraphenyl iron(Ⅲ) porphyrin chloride (FeTPPCl) to widen the absorption range of visible light, and decorated with bismuth oxyiodide (BiOI) nanosheets to improve the PEC response. The joint action of PAA and PEG could offset the adsorption of non-specific proteins on the immunosensing interface for obtaining good antifouling performance. Based on the specific interaction of sialic acid (SA) on the cytomembrane with 3-aminophenylboronic acid (APBA), and the synergistic antifouling effect of PEG and PAA, a simple PEC immunosensing method was developed for the quantitative determination of MDA-MB-231 cells. This proposed antifouling PEC immunosensor exhibited a wide linear range (1 × 10 2 ∼ 1 × 10 6 cells·mL -1 ) and a low detection limit (30 cells·mL -1 ). The development of antibody-free immunosensors may improve the application for the diagnosis of human breast cancer.

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Catalysis Science & Technology · 2020 ·Vol. 10 ·期 15 ·5149-5162 · IF 5.721

Efficient synthesis of methanol and ethylene glycol via the hydrogenation of CO2-derived ethylene carbonate on Cu/SiO2 catalysts with balanced Cu+–Cu0 sites

Tongyang Song,Wei Chen,Yuanyuan Qi,Jiqing Lu,Peng Wu,Xiaohong Li

Achieving high catalytic performance with Cu-based catalysts is crucial for the hydrogenation of CO2-derived ethylene carbonate (EC) to simultaneously yield methanol (MeOH) and ethylene glycol (EG). Although Cu-based catalysts are widely studied for the target reaction, there are still some issues to be clarified. In this study, we prepared a 29.1 wt% Cu/SiO2-MHT catalyst by a modified hydrothermal method and successfully applied it to the hydrogenation of EC. In comparison with its three analogues having similar Cu loading and comparable Cu particle size but prepared by different methods, we found that the catalytic performance of the Cu/SiO2 catalysts, including the activity and the selectivity to MeOH, could be tuned by adjusting the Cu+/(Cu0 + Cu+) ratio via different preparation methods. As a result, the Cu/SiO2-MHT catalyst furnished 89% MeOH yield and 37.6 h−1 turnover frequency. To our best knowledge, these values are one of the highest among all heterogeneous Cu catalysts up to now. The results reveal that a cooperative effect exists between Cu0 and Cu+. When the Cu0 species are sufficient to activate H2, a more favorable formation of MeOH can be achieved with more Cu+ species and greater Cu+ surface areas. Furthermore, a greater amount of Lewis acid on the Cu/SiO2-MHT catalyst is also beneficial for MeOH formation.

CAS / MDL: 12125-02-9
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Analytical Methods · 2019 ·Vol. 11 ·期 48 ·6176-6183 · IF 2.378

1H NMR determination of 1,3-dicyclohexylurea, glutaric acid and triethylamine in medical four-arm poly(ethylene glycol)-N-hydroxysuccinimide-glutarate for better quality control

Fei-Fei Li,Hui-Xiang Liu,Yan-Li Zhang,Shu-Qi Wang

Absorbable vascular sealing medical glue, which belongs to Class III medical devices, is a special new material for preventing the leakage of cerebrospinal fluid. Medical four-arm poly(ethylene glycol)-N-hydroxysuccinimide-glutarate (4-arm-PEG-SG) with a molecular weight of 20 000 is the main component of the absorbable medical glue. According to its quality standard, the quality control of residues 1,3-dicyclohexylurea (DCU), glutaric acid (GA) and triethylamine (TEA) is required. A rapid analytical method of quantitative 1H nuclear magnetic resonance (1H NMR) for the determination of residues DCU, GA and TEA in medical 4-arm-PEG-SG was established in the present study. The peaks at δ 1.56 (4H, m), δ 2.71 (4H, t, J = 6.7 Hz), and δ 2.42 (6H, q, J = 7.2 Hz) were selected for quantifying DCU, GA and TEA, respectively, with deuterated pyridine as the solvent and tetramethylsilane as the internal standard. The 1H NMR assay was validated by several experimental parameters including specificity, linearity, accuracy, precision, robustness, limit of detection (LOD), limit of quantification (LOQ) and stability. The average recoveries obtained were in the range of 99.48–102.02% for all three residues. Compared with the HPLC and GC approaches, the proposed 1H NMR method proved to be a powerful tool for quantification due to its unique advantages of simplicity, rapidity and high robustness, especially not requiring standard compounds for calibration curve preparation.

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Journal of Energy Storage · 2023 · IF 9.4

Synthesis of highly thermal conductive carbon nanotubes on cellulose nanofiber film-loaded polyethylene glycol phase change material with flame retardancy by layered double hydroxide

Qian Cao,Hongyuan Ding,Jianghui Xie,Dengji Xu,Yanjun Chen,Li Guo,Changcheng Liu,Que Huang

The nitrogen-doped carbon nanotubes (CNTs) were obtained by using methyl orange as a soft template and high temperature treatment, on which the layered double hydroxide (LDH) was grown in situ by hydrothermal method , and finally mixed with the phase change materials (PCM) by vacuum filtration to obtain a series of novel composite films with great flame retardancy and thermal conductivity . The use of cellulose nanofiber (CNF), polyvinylpyrrolidone (PVP) and polyethylene glycol (PEG) as PCM increased the film-forming properties, and the CNTs could improve the thermal conductivity of composites, while reducing the agglomeration of LDH nanolayers and improving the flame retardancy of the composite films. The results showed that the LDH grown on the nanotubes had a typical hexagonal lamellar structure , and its uniform distribution was the fundamental reason for the flame retardancy of the films which was verified by defined combustion experiments, the shortest self-extinguishing time and the least unburned area were achieved at a mass ratio of 7.14 % of LDH material. The melt and crystallization enthalpies of the thermally conductive flame-retardant films were 74.65 J/g −1 and 74.82 J/g −1 , and the thermal conductivity of the material was increased to 0.04129 W/(m·K) after the use of 2.5 % thermally conductive filler . It can reduce the temperature of LED by up to 5.9 °C during the LED opening process and up to 5.2 °C during the LED closing process.

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Polymer Chemistry · 2016 ·Vol. 7 ·期 13 ·2372-2380 · IF 5.687

Room temperature synthesis of poly(poly(ethylene glycol) methyl ether methacrylate)-based diblock copolymer nano-objects via Photoinitiated Polymerization-Induced Self-Assembly (Photo-PISA)

Jianbo Tan,Yuhao Bai,Xuechao Zhang,Li Zhang

The photoinitiated polymerization-induced self-assembly (photo-PISA) of 2-hydroxypropyl methacrylate (HPMA) is conducted in water by using poly(poly(ethylene glycol) methyl ether methacrylate) (PPEGMA) based macro-RAFT agents. Polymerizations were carried out at room temperature via exposure to visible light irradiation, and quantitative monomer conversions (>99%) were achieved within 30 min of visible light irradiation. A remarkably diverse set of complex morphologies (spheres, worms, and vesicles) have been prepared by aqueous photo-PISA under mild conditions (water medium, room temperature, and visible light). The morphology of nano-objects can be tuned by changing the reaction parameters (e.g. degree of polymerization, solids concentration), and two detailed phase diagrams were constructed. The polymerization can be activated or deactivated by a simple “ON/OFF” switch of the light source. A thermo-responsive behavior of PPEGMA14-PHPMA200 nanoparticles prepared at 15% w/w was investigated by changing the temperature from 25 °C to 4 °C.

CAS / MDL: 27813-02-1
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ADVANCED MATERIALS · 2023 · IF 29.4

Photothermal and Photocatalytic Glycol Chitosan and Polydopamine-Grafted Oxygen Vacancy Bismuth Oxyiodide (BiO1-xI) Nanoparticles for the Diagnosis and Targeted Therapy of Diabetic Wounds

Jianglong Kong,Sihan Ma,Runxuan Chu,Jiawen Liu,Hongrui Yu,Meiru Mao,Xiaohan Ge,Yuting Sun,Yi Wang

Treatment of diabetic wounds is a significant clinical challenge due to the massive infections caused by bacteria. In this study, multifunctional glycol chitosan and polydopamine-coated BiO 1-x I (GPBO) nanoparticles (NPs) with near-infrared (NIR) photothermal and photocatalytic abilities are prepared. When infection occurs, the local microenvironment becomes acidic, and the pH-switchable GPBO can target the bacteria of the wound site. The NIR-assisted GPBO treatment exhibits anti-bacterial effects with fast response, high efficiency, and long duration to Escherichia coli, Pseudomonas aeruginosa , and Staphylococcus aureus . GPBO achieves excellent photothermal imaging and CT imaging of the mouse subcutaneous abscess model. With the assistance of NIR irradiation, the GPBO promotes the healing of the diabetic wound model with the effects of anti-bacteria, anti-inflammation, the M2 polarization promotion of macrophages, and angiogenesis. This is the first-time report of nano-sized BiO 1-x I. The synthesis and selected application for the imaging and targeted therapy of diabetic wounds are presented. This study offers an example of the NP-assisted precise diagnosis and therapy of bacterial infection diseases.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF MATERIALS SCIENCE · 2018 ·Vol. 53 ·期 9 ·6433-6449 · IF 2.993

Synthesis of chitosan/poly (ethylene glycol)-modified magnetic nanoparticles for antibiotic delivery and their enhanced anti-biofilm activity in the presence of magnetic field

Wang Xi,Deng Aipeng,Cao Weiwei,Li Qiang,Wang Lina,Zhou Jie,Hu Bingcheng,Xing Xiaodong

Biocompatible Fe 3 O 4 /chitosan (CS)/poly (ethylene glycol) (PEG)/gentamicin (Gent) magnetic nanoparticles, namely Fe 3 O 4 @PEG-Gent NPs, have been successfully developed for antibiotic delivery. In which, PEG dicarboxylic acid was used to modify Fe 3 O 4 NPs for good dispersity as well as offer sufficient carboxyl groups as binding sites. And then the free Gent was facilely loaded onto Fe 3 O 4 NPs so as to achieve powerful antibacterial activity via electrostatic interactions. Under acidic condition, the CS and PEG of Fe 3 O 4 @PEG-Gent were protonated to introduce the positive charge to NPs surface, thus facilitating the contact with negatively charged bacterial cell membrane. What is more, the stretches of CS chains triggered by acidic pH may prevent the antimicrobial efficiency of Gent from weakening. Compared with the free antibiotic, these nanocomposites presented better antimicrobial efficacy against gram-positive bacteria S. aureus under acidic condition. Intriguingly, the confocal laser scanning macroscopy imaging suggested that the anti-biofilm efficacy of nanocomposites was significantly enhanced in the presence of an external magnetic field. Due to the superparamagnetic performance of Fe 3 O 4 NPs, these nanocomposites were allowed deeper penetration into a mature biofilm of S. aureus by magnetic field, leading to an effective Gent delivery for eradication of biofilm. The ingenious fabrication of the antibiotic delivery system not only efficiently improved the effectiveness and bioavailability of Gent at acidic media, but also provided an innovative platform to treat bacterial biofilms-associated infection by applying extra environmental factors such as magnetic field.

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RSC Advances · 2015 ·Vol. 5 ·期 26 ·20227-20233 · IF 3.84

Poly(γ-glutamic acid) induced homogeneous mineralization of the poly(ethylene glycol)-co-2-hydroxyethyl methacrylate cryogel for potential application in bone tissue engineering

Chuntao Liu,Xin Liu,Changyun Quan,Xiaoqiong Li,Chaozhu Chen,Hua Kang,Weikang Hu,Qing Jiang,Chao Zhang

Methacrylated poly(γ-glutamic acid) (mPGA) was introduced to the spongy poly(ethylene glycol)-co-2-hydroxyethyl methacrylate (PEG-HEMA) cryogels. A suitable amount (<0.1% w/v) of poly(γ-glutamic acid) (γ-PGA) in cryogels was found to promote homogeneous mineralization, while higher concentration of γ-PGA inhibited the mineralization. The deposited minerals mainly consisted of hydroxyapatite, carbonated apatite, and calcium phosphate, and were independent on the concentration of γ-PGA. The mineralized cryogels can support adhesion, viability, and migration of rat bone marrow stromal cells (rMSCs). The γ-PGA/HEMA-PEGDA cryogels showed their great potential as promising scaffolding materials in bone tissue engineering.

CAS / MDL: 868-77-9 110-18-9
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Materials Science & Engineering C-Materials for Biological Applications · 2017 · IF 4.164

Y-shaped methoxy poly (ethylene glycol)-block-poly (epsilon-caprolactone)-based micelles for skin delivery of ketoconazole: in vitro study and in vivo evaluation

Peizong Deng,Fangfang Teng,Feilong Zhou,Zhimei Song,Ning Meng,Na Liu,Runliang Feng

Ketoconazole is a hydrophobic broad-spectrum antifungal agent for skin infection therapy. In order to develop topical formulation of ketoconazole for improving its selective skin deposition and water-solubility, ketoconazole-loaded Y-shaped monomethoxy poly(ethylene glycol)-block-poly(ɛ-caprolactone) micelles were prepared through thin-film hydration method with high entrapment efficiency (96.1   ±   0.76%) and small particle (about 58.66   nm). The drug-loaded micelles showed comparative in vitro antimicrobial activity with KET cream. In e x in vivo skin deposition and permeation study, ketoconazole-loaded micelles provided skin accumulation higher than marketed ketoconazole cream without obvious permeation in the whole period. Fluorescence microscopy study and histopathological study demonstrated the copolymeric micelles' penetrating into skin in depth due to its capability of weakening the barrier function of stratum corneum. In vivo skin deposition parameters further confirmed high skin deposition of drug-loaded micelles (AUC (0-t)   =   396.16   μg·h/cm 2 ) over marketed ketoconazole cream (AUC (0-t)   =   250.03   μg·h/cm 2 ). Meanwhile, in vivo pharmacokinetic parameters proved that ketoconazole-loaded micelles reduced ketoconazole's distribution in blood in comparison with the cream (AUC (0-t)   =   93,028.00   μg·h/L vs AUC (0-t)   =   151,714.00   μg·h/L), meaning lower possibility of its systemic unwanted effects in the skin fungal infection treatment. The results suggested that the copolymeric micelles can be adopted for specific delivering ketoconazole into skin for fungal infection cure.

✓ 已验证 DOI PubMed 高影响因子
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