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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2018 · IF 3.862

Therapeutic efficacy of lipid emulsions of docetaxel-linoleic acid conjugate in breast cancer

Tao Zhang,Meng Li,Ruyi Yang,Dong Zhang,Jibin Guan,Jiang Yu,Bin Yang,Huicong Zhang,Shenwu Zhang,Dan Liu,Yongjun Wang

Docetaxel (DTX) solution is among the most widely-used parenteral formulations used in advanced breast cancer therapy. However, severe side effects have been observed due to the use of ethanol and polysorbate 80 . Herein, a novel DTX-based prodrug , docetaxel-linoleic acid conjugate (DTX-LA) was successfully synthesized. The high lipid solubility of DTX and DTX-LA resulted in a tendency for them to become entrapped in the oil core of the emulsions. As anticipated, nano-sized, sterically stabilized oil-in-water lipid emulsions (LMs) of DTX-LA LMs and DTX LMs were successfully constructed. Unlike DTX solution, LMs exhibited high colloidal stability and sustained-release behavior, having a narrow size distribution that was ∼220  nm in diameter. Compared with DTX LMs, DTX-LA LMs had a greater drug-loading capacity. Although the cytotoxicity of DTX-LA LMs was reduced in comparison with DTX solution, the pharmacokinetic study demonstrated increased bioavailability (p < 0.001) and half-life (p < 0.01). Finally, DTX-LA LMs displayed significant antitumor efficacy with reduced side effects in a 4T1 breast cancer xenograft model. Thus, the novel lipid emulsion-based docetaxel prodrug delivery system may be a promising strategy for improving intravenous administration for breast cancer treatment.

研究领域: 药学 · 肿瘤学
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CHEMOSPHERE · 2022 · IF 8.943

Demulsification of amphiphilic gemini ionic liquids and its demulsification mechanism

Fan Ye,Liwei Shen,Shi Liu,Huanyu Liu,Xinyuan Zhang,Zejun Zhang,Ying Yang,Xuening Feng,Yuqi Tang,Dong Xiang,Yuanzhu Mi,Xuemin Yan

This work aims to prepare two new amphiphilic and interfacial active gemini ionic liquids to treat crude oil and investigates its demulsification mechanism. Tetraethylene glycol was pretreated with thionyl chloride and used as a linker to connect succinimide or phthalimide , and then reacted with dodecyl benzene sulphonic acid to obtain the corresponding amphiphilic and interfacial active gemini ionic liquid STA or PTA, respectively. 1 H nuclear magnetic resonance spectroscopy ( 1 HNMR) and Fourier-transform infrared spectroscopy (FTIR) was used to determine the chemical structures. The demulsification tests showed the demulsification efficiency with 150 mg/L of STA or PTA at 60 °C for 30 min was 99.89% and 99.79%, respectively. Furthermore, the demulsification mechanism of STA and PTA were studied and the prominent demulsification ability of STA and PTA were attributed to the better interfacial activity and amphipathy which could destroy the asphaltenes interfacial film. These results showed that STA and PTA had excellent demulsification efficiency, which promised application in petroleum industry .

研究领域: 石油化学 · 界面化学
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BIOMEDICAL CHROMATOGRAPHY · 2024 ·Vol. 39 ·期 1 ·e6055 · IF 1.8

Development of a UPLC-MS/MS Method for Bioanalysis of Ethoxysanguinarine and Its Application in Pharmacokinetic Study of Ethoxysanguinarine Nanoemulsion

Jianhui Luo,Songshen Chen,WenYang Song,Yongtong Huang,Song Gao,Jiu Wang

Ethoxysanguinarine (ETSG), a benzophenanthridine alkaloid, exhibits diverse biological activities, including antibacterial, antifungal, anti-inflammatory, antioxidant, and anti-tumor effects. Despite these properties, limited research exists on ETSG in vivo pharmacokinetics due to its poor solubility and low bioavailability. In this study, we developed a rapid and specific UPLC-MS/MS method for ETSG bioanalysis. Sample preparation involved one-step protein precipitation using methanol and phellodendrine as an internal standard (IS). The Waters HSS T3 column (2.1 * 50 mm, 1.8 μM) employed a gradient elution with mobile phases A (2 mmol/L ammonium formate aqueous solution-formic acid [99.8:0.2, v/v]) and B (methanol-formic acid [99.8:0.2, v/v]). Mass analysis via Waters Q-mass spectrometer utilized positive scan mode and multiple reaction monitoring. ETSG and IS were detected at m/z 332.0 → 274.0 and 342.0 → 177.0, respectively, within 7.0 min. The method demonstrated excellent precision, accuracy, recovery, and stability, with a linear calibration curve (1.1–560 ng/mL) and strong correlation coefficient (0.9984). Successful pharmacokinetic evaluation in Sprague–Dawley rats included intravenous ETSG administration and intragastric ETSG nanoemulsion/suspension. This method enables steroidal saponin analysis from ETSG in biological samples.

CAS / MDL: 67-68-5 25322-68-3
研究领域: 药物分析 · 生物化学 · 药理学
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Expert Opinion on Drug Delivery · 2020 · IF 4.838

Oral co-delivery nanoemulsion of 5-fluorouracil and curcumin for synergistic effects against liver cancer

Pu Guo,Chao Pi,Shijie Zhao,Shaozhi Fu,Hongru Yang,Xiaoli Zheng,Xiaomei Zhang,Ling Zhao,Yumeng Wei

Background A novel nanoemulsion (CU/FU-LN) was developed as an oral 5-fluorouracil and curcumin co-delivery system for synergistic efficacy against liver cancer.Methods MTT assay, confocal laser scanning microscope, and H&E staining were utilized to establish the efficacy and safety of CU/FU-LN.Results The AUC(0-t) of CU/FU-LN was 8.85-fold and 8.59-fold greater than those of CU and FU, respectively. The IC50 of CU/FU-LN was 4.6-fold and 4.9-fold lower than those of FU and CU in HepG2 cells, respectively. In vivo anti-tumor trials, the tumor inhibition rate was significantly elevated by CU/FU-LN (49.29%), compared 24.84% and 4.72% for FU and CU, respectively. Ki-67 immunohistochemical analysis revealed that CU/FU-LN had an obvious anti-proliferation effect. The IC50 of CU/FU-LN in L02 cells was 1.51-fold and 2.60-fold higher than those of CU and FU, respectively. Certain vital organs in the mice of the CU/FU-LN group showed markedly fewer lesions than those of the CU, FU, and CU+FU groups. The CU/FU-LN treatment caused no significant change in mouse body weight relative to the control group (P > 0.05). Conclusions We successfully prepared a promising co-delivery platform for the synergistic treatment of liver cancer and it has a comparatively enhanced efficacy and mitigated toxicity.

研究领域: 药剂学 · 肿瘤学 · 生物医学工程
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ENERGY & FUELS · 2020 · IF 3.421

Application of Novel Amphiphilic Janus-SiO2 Nanoparticles for an Efficient Demulsification of Crude Oil/Water Emulsions

Han Jia,Jiajun Dai,Pan Huang,Yugui Han,Qiuxia Wang,Juan He,Jinyong Song,Xin Wei,Hui Yan,Dexin Liu

It is greatly desired to develop a high-efficiency demulsifier for the treatment of O/W emulsions in the production fluids of the petroleum industry. In this study, the amphiphilic Janus-SiO2 nanoparticles (Janus-C18) was synthesized and used as a demulsifier for surfactant-stabilized O/W emulsions. The successful preparation of Janus-C18 was verified by transmission electron microscopy (TEM), Fourier transform infrared spectroscopy (FT-IR), thermogravimetric analysis (TGA), and contact angle measurements. Then, Janus-C18’s demulsification efficiency was systematically evaluated by the bottle test. Various silica nanoparticles and emulsifier were employed in the control experiments. Based on the Janus-C18’s demulsification performance in different conditions and the ζ-potential measurement, the possible demulsification mechanism of Janus-C18 was proposed. Furthermore, Janus-C18 exhibited excellent performance in separating oil from crude oil/water emulsions at a relatively low concentration (150 mg/L), with the oil removal rate exceeding 99%.

研究领域: 化学工程 · 材料科学 · 石油工程
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JOURNAL OF DISPERSION SCIENCE AND TECHNOLOGY · 2023 · IF 2.2

The demulsification of oily wastewater by a hyperbranched polymer grafted SiO2

Yu Zhang,Jiazhe Kuang,Bin Li,Yuanzhu Mi,Ying Yang,Xuening Feng

In this work, a PAMAM@SiO2 demulsifier was synthesized by the reaction of a hyperbranched poly (amido amine) (PAMAM) and KH570 modified SiO2. The structure, morphology and composition of PAMAM@SiO2 were characterized by FT-IR, SEM and EDS. The effect of the concentration of PAMAM@SiO2, salinity and temperature on the demulsification performance was systematically studied. The results showed that the transmittance of aqueous phase after demulsification could reach as high as 92.1% at optimal conditions, and corresponding oil removal rate was 99.53%. Interfacial activity, three-phase contact angle, self-assembly of interfacial film and dynamic interfacial tension were investigated to explore the demulsification mechanism. Also, the aggregation process of oil droplets in emulsion was observed with a microscope. It indicates that the PAMAM@SiO2 demulsifier has a potential application in the treatment process of oily wastewater.

研究领域: 材料科学 · 环境科学
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SEPARATION SCIENCE AND TECHNOLOGY · 2024 · IF 2.3

Comparative study on the performance and properties of polyether and polyacrylate crude oil demulsifier

Sisi Yuan,Xiujun Wang,Yongjun Wang,Ming Duan,Yan Xiong,Shenwen Fang

Polyacrylate crude oil demulsifier is one of the hot topics in the research and development of demulsifier at present, there is a lack of systematic comparative study on performance and properties of polyether and polyacrylate crude oil demulsifier. In this paper, the demulsification performance and microscopic demulsification process of the two demulsifiers, namely polyacrylate P(MA-DBC) and polyether P199–59 are discussed. The demulsification performance of polyether P199–59 was superior to that of polyacrylate P(MA-DBC). The study of the microscopic process of demulsification established that for P199–59, the diffusion rate was faster, the saturated adsorption capacity was higher, the ability to destroy the oil-water interface film was stronger and the probability of water droplets collision coalescence was higher; therefore, it can achieve faster dehydration speed and higher dehydration rate than that of P(MA-DBC). The results of this comparative study are meaningful for improving the demulsification performance of polyacrylate demulsifier.

CAS / MDL: 1338-39-2
研究领域: 化学工程 · 石油工程
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JOURNAL OF HAZARDOUS MATERIALS · 2024 · IF 12.2

Synthesis and demulsification performance of a novel low-temperature demulsifier based on trimethyl citrate

Liwei Shen,Guosheng Ai,Hanguang Liu,Lianggen Zhu,Lu Lai,Xuemin Yan,Weichu Yu,Yuanzhu Mi

A significant amount of water-in-oil (W/O) emulsion is generated during petroleum extraction. However, the current commercial demulsifiers are expensive to produce and requires high demulsification temperatures, leading to increased energy and economic consumption. To enhance the efficiency of demulsifiers and reduce the cost of demulsifying W/O emulsions, we have successfully developed a novel demulsifier named TCED through a straightforward two-step process. This demulsifier features trimethyl citrate as the hydrophilic core grafted with three hydrophobic chains. Its structure was characterized using EA, FT-IR and 1 H NMR spectroscopy , and the demulsification performance was comprehensively evaluated. At a low demulsification temperature of 40 °C, TCED demonstrated a remarkable demulsification efficiency (DE) of 99.06% and 98.74% in emulsions containing water contents of 70% (E70) and 50% (E50), respectively. Especially, a DE of 100% could be obtained in both E70 and E50 emulsions at a concentration of 600 mg/L. Moreover, TCED displayed a high DE even at high salinity levels of 50,000 mg/L and across a wide pH range of 2–10. Additionally, the phase interface was consistently clear after demulsification. To investigate the demulsification mechanism of TCED, various adsorption kinetics experiments were conducted, including measurements of interfacial tension (IFT), surface tension (SFT), interfacial competitive adsorption, and stability of interfacial film. The results obtained from the experiments indicated that TCED possessed remarkable diffusion and replacement capabilities within the emulsions. As a result, it effectively disrupted the original interfacial active substances, such as asphaltenes aggregates found in crude oil. TCED exhibits a high DE at low concentration and temperature. This characteristic highlights its significant potential for low-temperature demulsification applications in the petroleum industry.

CAS / MDL: 1587-20-8
研究领域: 石油化学 · 表面化学
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JOURNAL OF CONTROLLED RELEASE · 2024 · IF 10.5

Lipiodol emulsion as a dual chemoradiation-sensitizer for pancreatic cancer treatment

Shuang Zhu,Chenglu Gu,Long Gao,Shuanglong Du,Duiping Feng,Zhanjun Gu

Pancreatic ductal adenocarcinoma (PDAC) has a low survival rate and limited treatment options. Concurrent chemoradiotherapy is considered beneficial to improve tumor control, but the low drug bioavailability at tumor site and the low radiation tolerance of surrounding healthy organs greatly limits its effectiveness. Lipiodol, a natural drug carrier used in clinical transarterial chemoembolization, has shown potential as a radiosensitizer due to its high Z element iodine composition. Thus, this study aims to repurpose lipiodol as a sensitizer to simultaneously enhance chemo- and radiotherapy for PDAC. To this end, a stable lipiodol emulsion (IOE) loaded with gemcitabine is designed using clinically approved surfactants. At in vivo level, IOE demonstrates better radiotherapeutic effect than existing nanoradiosensitizers and enhanced drug bioavailability over free drug, leading to significant tumor inhibition and improved survival rates under concurrent chemo-radiotherapy. This may due to the sustained drug release, homogenous spatial distribution, and long-term retention ability of IOE in solid PDAC tumor. Furthermore, to better understand the functioning mechanism of drug-loaded IOE, in vitro study is conducted to reveal the ROS- and DNA damage-related therapeutic pathways. Lastly, a comprehensive toxicity assessment also proves the good biocompatibility and safety of as-prepared IOE. This study offers a clinically feasible sensitizer for simultaneous chemoradiotherapy and holds potential for other types of cancer treatment in clinics.

研究领域: 肿瘤学 · 放射治疗学 · 药剂学
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CHEMICAL ENGINEERING JOURNAL · 2016 · IF 5.31

An innovative method to introduce magnetism into demulsifier

Shenwen Fang,Bin Chen,Ting Chen,Ming Duan,Yan Xiong,Peng Shi

In this work, a novel magnetic demulsifier was synthesized by a facile way within one step. The propyleneoxide-ethyleneoxide block polyether , one of the most frequently used demulsifier in petroleum industry , was endowed with the magnetism by reacting with iron (III) acetylacetonate. The as-prepared magnetic demulsifier was characterized by transmission electron microscopy (TEM), superconducting quantum interference device (SQUID), Fourier transform infrared spectroscopy (FTIR) and X-ray photoelectron spectroscopy (XPS). The magnetic demulsifier showed excellent demulsification performance for water in crude oil emulsion. The demulsification process was revealed by using confocal microscope. Besides, the used magnetic demulsifier could be readily recycled by magnetic separation and solvent washing, and it presented excellent demulsification performance within 3 cycles. The findings in this work might provide a facile approach to prepare varieties of magnetic demulsifiers.

CAS / MDL: 14024-18-1
研究领域: 化学工程 · 材料科学
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Journal of Cleaner Production · 2021 · IF 9.297

Coalescence and separation of surfactant-stabilized water-in-oil emulsion via membrane coalescer functionalized by demulsifier

Peng Shi,Rui Zhang,Wanfen Pu,Rui Liu,Shenwen Fang

The coalescence and separation of surfactant stabilized water-in-oil emulsion was an important process in the chemical industry but the conventional thermo-chemical demulsification had high energy and reagent consumption. The studies on demulsification at room temperature via porous materials usually involved the emulsion with low water content (<1%). This study demonstrated the coalescence of W/O emulsion with 50% water content via filtration by a demulsifier-grafted polyether sulfone (PES) microfiltration membrane. The material worked as coalescer and it divided the emulsion into layered oil and water with high purity after filtration. The obtained material was analyzed by attenuated total reflectance infrared spectroscopy (ATR-FTIR) and X ray photoelectron spectroscopy (XPS) to prove the existence of demulsifier. When the demulsifier loading was 0.8 wt% of the solvent, the initiator loading was 0.8 wt% of the demulsifier, and the polymerization grafting was carried out at 50  ° C for 5 h, the demulsification efficiency could reach 97.9%. The separation efficiency of the oil from water and the water from oil could get up to 99.5% simultaneously.

研究领域: 化学工程 · 材料科学
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JOURNAL OF MOLECULAR LIQUIDS · 2024 · IF 5.3

Synthesis of a low-temperature demulsifier with dual-hydrophobic chains through a simple low-temperature process

Jie Ma,Tao Wang,Wei Hou,Zhenhua Wu,Suling Bao,Dan Wu,Wentao Ma,Yu Zhang

The extraction of crude oil generates a significant volume of stable emulsions that can lead to various adverse effects in industrial extraction processes. Therefore, emulsion demulsification is a crucial step. In this paper, PGDA, a low-temperature W/O demulsifier with double hydrophobic chains, was synthesized from poly(ethylene glycol) diacrylate by a simple low-temperature process. The structure of PGDA was analyzed by FTIR and 1 H NMR, and the demulsification performance was evaluated by a bottle-testing method. The results demonstrated that PGDA, at a concentration of 500 mg/L, achieved a demulsification efficiency of 100 % under low-temperature conditions (45 °C) over a 5-hour period. Furthermore, it also showed good demulsifying performance in wide pH range (6–10) and high salinity (100,000 mg/L). In addition, the possible mechanism of demulsification of PGDA was investigated by zeta potential, interfacial tension, and three-phase contact angle, etc. PGDA showed strong competitive adsorption ability with asphaltenes at the interface. PGDA has the ability to navigate rapidly to the oil–water boundary and displace the native surfactants there, thus destabilizing the emulsion and thus promoting the separation of oil and water. PGDA by virtue of the simple synthesis process, low demulsification temperature and high efficiency are of practical application.

CAS / MDL: 26570-48-9
研究领域: 化学工程 · 石油工程
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