Pharmacology Research & Perspectives
·
2022
·Vol. 10
·期 1
·e00928
·
IF 2.963
Siyuan Cao,Min Zhang,Minyan Yuan,Dan Yang,Mei Zhao,Shuo Zhang,Pengjiao Wang,Rongping Zhang,Xiuli Gao
The bioavailability of drugs is often related to intestinal metabolism and transport mechanisms. In previous studies, pharmaceutical excipients were recognized as inert substances in clinical safety evaluations. However, a large number of studies have shown that pharmaceutical excipients regulate the metabolism and transport of drugs in the body and improve the bioavailability. The pharmaceutical excipient polyethylene glycol 400 (PEG400) as a good solubilizer and surfactant has the potential to improve the bioavailability of drugs. The combined action of UDP-glucuronosyltransferases (UGTs) and efflux transport proteins is responsible for the intestinal disposition and poor bioavailability of baicalein. Our aim is to study the effect of PEG400 on the absorption of baicalein on the Caco-2 monolayer, and confirm the interaction of PEG400 with UGTs (UGT1A8 and UGT1A9) and efflux transports. We initially found that baicalein in the Caco-2 monolayer would be metabolized into glucuronide conjugates BG and B6G under the action of UGT1A8 and UGT1A9 on the endoplasmic reticulum membrane, and then mainly excreted to different sides by acting of MRP and BCRP. The addition of PEG400 significantly accelerated the metabolism of B in Caco-2 cells and increased the penetration of BG and B6G. Furthermore, PEG400 also significantly decreased the efflux ratio of BG and B6G, which was the evidence of the interaction with the efflux transporters. In the in vitro intestinal microsome regeneration system, low concentration PEG400 decreased the K m value of UGT1A8 and UGT1A9 (key enzymes that mediate the production of BG and B6G); high concentration PEG400 enhanced the V max value of UGT1A8 and UGT1A9. In conclusion, our results determined that PEG400 interacted with some UGTs and efflux transporters, which were the main factors affecting the absorption of baicalein.
研究领域:
药学
·
药理学
·
药物代谢
·
药物递送系统
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Polymers
·
2025
·Vol. 17
·期 3
·387
·
IF 4.9
Rong Sun,Liangliang Li,Jiangjie Zhou,Yongfeng Zhang,Haiya Sun,Datong Zhang,Qi Wu
Zein exhibits excellent biodegradability, thermal stability, UV resistance, and water barrier properties, making it a promising candidate for food packaging applications. However, pure zein films suffer from brittleness and poor mechanical strength, which limit their practical use. In this study, a unique bilayer packaging film (ZP/P-C) was developed using a layer-by-layer solution casting technique, where hydrophobic zein was coated onto a polyvinyl alcohol and chitosan composite layer (P-C). Incorporating PEG400 into the zein layer improved the interfacial compatibility of the bilayer film, increasing its uniformity and toughness. The resulting bilayer films demonstrated enhanced mechanical properties, flexibility, and water vapor barrier performance. Specifically, the ZP7.5/P-C bilayer film showed an elongation at break of 68.74% and a modulus of elasticity of 187.19 MPa. It had a water vapor permeability of 6.60 × 10−11g·m·m−2·s−1·Pa−1and provided near-complete UV protection within the 200–350 nm range. Furthermore, an intelligent detection bilayer film was created by integrating anthocyanin extract into the zein layer. Adding anthocyanin improved the film’s antioxidant properties and allowed it to respond colorimetrically to total volatile basic nitrogen. The bilayer film ZPBA1.0/P-C displayed an excellent antioxidant activity (45.8%) and remarkable color change (ΔE = 20.2) in response to ammonia, effectively indicating shrimp spoilage in 48 h (ΔE > 10). This investigation spotlights the potential of zein-based bilayer films in active and intelligent food packaging, offering innovative strategies to improve food safety and extend the shelf life of perishable goods.
研究领域:
食品科学
·
材料科学
·
包装工程
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产品关联
DOI
PubMed
高影响因子
RSC Advances
·
2016
·Vol. 6
·期 59
·54377-54381
·
IF 3.289
Dingyi Wang,Shengmei Guo,Rongxing Zhang,Sen Lin,Zhaohua Yan
An efficient procedure for the formation of C–S bonds via C–H functionalization was developed for the synthesis of aryl sulfides in good to excellent yields using TBAI–HBr system promoted direct sulfenylation of various compounds, such as phenols, pyrazolones, indoles and related heteroarenes. Low cost and widely available arylsulfonyl chlorides were used as the sulfur source to provide various sulfur-containing compounds. The characteristic of the present protocol is convenient, green, highly efficient with a wide-application and short reaction time.
研究领域:
有机化学
·
合成化学
✓ 已验证
DOI
高影响因子
Acta Pharmaceutica Sinica B
·
2026
·
IF 14.6
Yutong Sun,Shuze Xian,Zhe Wang,Jinlan Zhang
Pharmaceutical excipient polyethylene glycol 400 (PEG400) is widely used in injections, nanotherapeutics, and drug delivery systems, yet its metabolic characteristics, pathways, and risks remain unclear. In this study, a novel analytical strategy based on ultra-high-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UHPLC–Q-TOF/MS) was developed to comprehensively profile parent PEGs and metabolites. After PEG400 administration, 98 PEG metabolites of seven types were identified in rats. PEG undergoes two metabolic pathways: oxidative reactions, which generate PEG carboxylic acid, PEG aldehyde, and PEG formate ester; and conjugation reactions, which form three types of metabolites. Pharmacokinetics of parent PEGs and metabolites showed that the half-life of parent PEGs is molecular weight-dependent, and the most abundant metabolite, PEG–COOH, is rapidly formed. PEG and its metabolites were widely distributed in tissues, including kidneys, liver, and immune organs, and primarily excreted via the kidneys. Notably, this study first elucidated that PEG400 is oxidized via dual pathways of CYP enzymes and alcohol dehydrogenase/aldehyde dehydrogenase, indicating potential risks of excipient–drug interactions and disulfiram-like reactions. PEG acid metabolites can exacerbate nephrotoxicity in zebrafish and rats with acute kidney injury. These findings highlight unrecognized metabolic risks of PEG400 and raise safety concerns regarding its formulation development and clinical application.
✓ 已验证
DOI
高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
·
2024
·Vol. 26
·期 1
·72
·
IF 4.9
Chaoji Li,Min Zhang,Yanni Zhao,Dan Yang,Mei Zhao,Leyuan Shang,Xiaodong Sun,Shuo Zhang,Pengjiao Wang,Xiuli Gao
Mycophenolic acid (MPA) is a commonly used immunosuppressant. In the human body, MPA is metabolized into mycophenolic acid 7-O-glucuronide (MPAG) and mycophenolic acid acyl-glucuronide (AcMPAG) mainly through liver glucuronidation, which involves UDP-glucuronosyltransferase (UGTs) and transfer proteins. Research has indicated that the pharmaceutical excipient PEG400 can impact drug processes in the body, potentially affecting the pharmacokinetics of MPA. Due to the narrow therapeutic window of MPA, combination therapy is often used, and PEG400 is widely used in pharmaceutical preparations. Therefore, investigating the pharmacokinetic influence of PEG400 on MPA could offer valuable insights for optimizing MPA’s clinical use. In this study, we examined the impact of a single oral dose of PEG400 on the blood levels of MPA in rats through pharmacokinetic analysis. We also investigated the distribution of MPA in various tissues using mass spectrometry imaging. We explored the potential mechanism by which PEG400 affects the metabolism of MPA using hepatic and intestinal microsomes and the Caco-2 cellular transporter model. Our findings reveal that the overall plasma concentrations of MPA were elevated in rats following the co-administration of PEG400, with the AUC0-tof MPA and its metabolite MPAG increasing by 45.53% and 29.44%, respectively. Mass spectrometry imaging showed increased MPA content in tissues after PEG400 administration, with significant differences in the metabolites observed across different tissues. Microsomal and transport experiments showed that PEG400 accelerated the metabolism of MPA, promoted the uptake of MPA, and inhibited efflux. In conclusion, PEG400 alters the in vivo metabolism of MPA, potentially through the modulation of metabolic enzymes and transport.
研究领域:
药理学
·
免疫抑制剂
·
药物代谢
·
药用辅料
·
体内和体外研究
✓ 已验证
产品关联
DOI
PubMed
高影响因子
RSC Advances
·
2023
·Vol. 13
·期 17
·11728-11732
·
IF 3.9
Yanqiang Tong,Weihua Zou,Delin Sun,Zhangheng Wang
Thermochromic wood is an important research direction for wood modification in recent years, and a red poplar-based thermochromic composite (R-PTC) had been prepared in our previous study by compositing a mixture of phase change reagents (tetradecyl ester: C28H56O2 and methyl red: C15H15N3O2) and full poplar wood. In order to improve the heating storage ability of R-PTC and encapsulating phase change reagents to prevent leakage, a new R-PTC composite (PS-R-PTC) was prepared by encapsulated R-PTC with polyethylene glycol 400 (PEG400)–SiO2 in this work. Compared to the original R-PTC samples, the cell walls of PS-R-PTC were not significantly changed by the SiO2 film and we also found that PS-R-PTC with PEG400 (90%)–silica solutions (10%) mixture had better heat storage performance and PS-R-PTC (90%) has better enthalpy change value (R-PTC: 43.01 J g−1; PS-R-PTC (90%): 71.82 J g−1). The PS-R-PTC can show the function of thermal energy storage, which is used in wooden buildings and can be a feasible insulating material for reducing thermal energy losses and hence reducing energy usage. In PS-R-PTC, SiO2 combines with the –OH of the R-PTC and the –OH of PEG400 (HO(CH2CH2O)nH), and these –OH lose hydrogen ions too.
研究领域:
材料科学
·
林业工程
·
能源技术
✓ 已验证
DOI
PubMed
高影响因子
CHEMICAL ENGINEERING SCIENCE
·
2021
·
IF 4.311
Qiao Chen,Yuanhui Ji,Kai Ge
In this work, the influence of polymeric excipients (PEG6000, PEG400, PVPK25, and HPMCE3) on thermodynamic phase behavior of active pharmaceutical ingredients (API) (mesalazine and allopurinol) and its aqueous solution was systematically investigated through experimental measurement and thermodynamic modeling. The API/excipients formulations were prepared by ball milling, and the phase behavior was measured by differential scanning calorimetry (DSC). The results showed that the solubility of API/solvent systems were all increased with higher temperature. Meanwhile, it was found that all four excipients can solubilize mesalazine and allopurinol effectively and the solubilization performance of PVPK25 and HPMCE3 were preferable to PEG. Furthermore, the thermodynamic phase behavior of API in the excipients/water ternary system was predicted by the Perturbed-Chain Statistical Associating Fluid Theory (PC-SAFT), demonstrating good accordance with the experimental results with low average relative deviations (ARDs). This work was expected to provide theoretical guidance for the screening of pharmaceutical formulation excipients.
研究领域:
药剂学
·
热力学
·
材料科学
·
化学工程
✓ 已验证
产品关联
DOI
高影响因子
POLYMER
·
2025
·
IF 4.5
Lishuang Yang,Ruili Li,Jinke Wang,Yujie Gao,Meiyi Wang,Huashan Wang
A photosensitive polyurethane prepolymer with alternating soft and hard segments was synthesized using polyethylene glycol (PEG400) and hexamethylene diisocyanate (HDI). At the same time, hydroxyethyl methacrylate (HEMA) was employed as a chain terminator to introduce acrylate functionalities. The successful formation of urethane linkages was confirmed by Fourier-transform infrared (FTIR) spectroscopy and nuclear magnetic resonance (NMR) spectroscopy. At a soft-to-hard segment molar ratio of 1:1.5, the resulting photopolymerized elastomer exhibited optimal mechanical performance, achieving a tensile strength of 7.8 MPa and an elongation at break of 275%. Furthermore, photopolymerization with lauryl methacrylate (LMA) imparted the material with excellent flexibility. The incorporation of silane-coupling-agent-modified nano-SiO 2 as a reinforcing filler further improved the mechanical strength of the composite. By surface-loading an ionically conductive hydrogel, the material was employed to fabricate a tensile sensor via vat photopolymerization 3D printing, demonstrating its potential in flexible sensing applications.
研究领域:
材料科学
·
高分子化学
·
增材制造
·
传感器
·
纳米复合材料
·
力学性能
·
光聚合
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）