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EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES · 2018 · IF 3.466

The effect of DSPE-PEG2000, cholesterol and drug incorporated in bilayer on the formation of discoidal micelles

Wenli Zhang,Zhiyu Wang,Chenchen Wu,Ya Jin,Xinyue Liu,Zimei Wu,Jianping Liu

In cholesterol/DSPE-PEG 2000 /DPPC systems, nano-disks could evolve between liposomes and spherical micelles in a certain range of PEG-lipids. How cholesterol or drug influences this evolution and what about the properties of discoidal micelles as drug carrier are still not clear. Aiming at this, nanocarriers with different contents of cholesterol and DSPE-PEG 2000 were prepared by thin-film-hydration method. Firstly, the bilayer fluidity of nanocarriers was investigated and proved to decrease with the increase of cholesterol, and the cooperative degree between phospholipids was also related to cholesterol content in an order of 30 > 40 > 15 > 0 mol%. Then three different levels of cholesterol were chosen to study its effect on DSPE-PEG 2000 limit used to form discoidal micelles. For transition from liposomes to disks, the limit of DSPE-PEG 2000 employed is above 0.5 mol% at 0 mol% cholesterol, above 15 mol% at 30 mol% cholesterol and above 5 mol% at 40 mol% cholesterol observed from TEM images, indicating that nanocarriers with 30 mol% cholesterol formed discoidal micelles most difficultly due to the strongest interaction between phospholipids. However, membrane fluidity seems to have little responsibility for the different morphologies. And imatinib (IM) could promote the formation of discoidal micelles, resulting from the interaction between IM and polar headgroups of phospholipid demonstrated by DSC . The relative reduction of entrapment efficiency for three agents with different dissolving properties showed that lipophilic drugs were the most suitable drug that could be loaded into discoidal micelles. In addition, the discoidal micelle formulations tested could readily change to other morphologies after 80 days' storage. In conclusion, both the cholesterol content and IM could affect the formation of discoidal micelles by probably influencing the interaction between phospholipids, also the discoidal structure was not stable enough and only suitable for lipophilic drug loading. We hope this study could help to design the formula and choose the proper drugs that may retain the discoidal morphology.

CAS / MDL: 3326-32-7
研究领域: 药剂学 · 生物物理学
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COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS · 2019 · IF 3.131

Improved hydrolysis of α-tocopherol acetate emulsion and its bioaccessibility in the presence of polysaccharides and PEG2000

Xing-An Luo,Pei Zhao,Hai Zhang,Shu-Yi Feng,Ke-Xian Chen,Zhong-Xiu Chen

Dietary macromolecules are often used for food formulation. Most of the published literature usually focuses on a certain polysaccharide reducing lipid digestion, but the non-specific physical effects such as the excluded volume effect of the surrounding macromolecules, which will possibly enhance the hydrolysis of lipids, is rarely discussed. As the influence of polysaccharides on the gastrointestinal fate of α-tocopherol acetate (VE-A) encapsulated in emulsion have not been conducted so far, in this research, we study the effect of crowded medium created by polysaccharides (Ficoll400) on the hydrolysis of VE-A and its bioaccessibility. The results show that the presence of Ficoll400 increased the bioaccessibility and conversion of VE-A 1.6 times that of a dilute buffer. An enzyme-catalyzed kinetic reaction rate of VE-A hydrolysis is increased up to 3.5 times. Both the improved thermodynamic conversion yields and kinetic rates of the hydrolysis of the VE-A emulsion was further observed in a synthetic macromolecule PEG2000 medium. This research improves our understanding of the crowding effect of macromolecules on VE-A/lipid emulsion digestion.

研究领域: 食品科学 · 营养学 · 生物化学
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Journal of Energy Storage · 2024 · IF 8.9

Preparation and characterization of highly efficient photothermal conversion and storage composites based on Cu2-xS

Min Li,Chao Shen

In order to improve the photothermal conversion performance of a phase change material (PCM) PEG2000, a photothermal conversion material Cu 2-x S was introduced to enhance its light absorbance. The influence of S/Cu stoichiometry and Fe 3+ doping modification ratio on the photoabsorption performance of Cu 2-x S was studied. The composite with photothermal conversion performance was obtained by combining PEG2000. The results show that Cu 2-x S (S2) doped with Fe/Cu stoichiometry ratio of 0.3:1 exhibits the best light absorption performance. Moreover, a small amount of additive of the modified Cu 2-x S (Cu 2-x Fe y S, 1.0 wt%) can greatly increase photothermal conversion and energy storage efficiency. The prepared composite can meet the practical application in the field of solar photothermal conversion.

CAS / MDL: 10125-13-0
研究领域: 材料科学 · 能源科学
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CARBOHYDRATE RESEARCH · 2025 · IF 2.5

Water-stable PEG2000-modified citric acid crosslinked β-CD MOF for efficient removal of tetracycline hydrochloride: synthesis, adsorption behavior, and mechanism

Chunlin Gou,Ziqing Weng,Xiaoshuang Dai,Jianpeng Liu,Ke Mei,Bin Sun,Neng Qiu

To address the ecological and health risks associated with residual tetracycline hydrochloride (TCH) in water, a green-synthesized adsorbent composed of β-cyclodextrin (β-CD), citric acid (CA), and polyethylene glycol (PEG) was developed for the effective removal of TCH from wastewater. The synthetic parameters were optimized, and the resulting PEG-CA-β-CD MOF was characterized by FT-IR, XRD, and SE. TGA analysis indicated an increase in the thermal stability. The maximum adsorption capacity of PEG-CA-β-CD MOF for TCH was 221.6 mg/g at pH = 4. Adsorption kinetics were well-described by the Elovich equation model, while the Freundlich isothermal model accurately described the equilibrium data adsorption Thermodynamic analysis revealed that the adsorption process was endothermic and spontaneous. Furthermore, the adsorbent maintained 84 % of its initial adsorption capacity after four reuse cycles. Analysis using zeta potential, FT-IR, and XPS confirmed that the possible adsorption mechanism of TCH mainly involves electrostatic interactions, hydrogen bonding, and cavity encapsulation. Finally, simulated wastewater experiments showed that PEG-CA-β-CD MOF was able to adsorb TCH efficiently even in the presence of other pollutants. Overall, due to its green synthesis process, low cost, ease of regeneration, and multi-mechanistic adsorption capability, the PEG-CA-β-CD MOF exhibits significant potential for TCH removal in wastewater treatment.

CAS / MDL: 64-75-5
研究领域: 环境科学 · 材料科学 · 化学工程 · 纳米技术 · 污染治理
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Pharmaceutics · 2025 ·Vol. 17 ·期 8 ·950 · IF 5.5

Formulation-Driven Optimization of PEG-Lipid Content in Lipid Nanoparticles for Enhanced mRNA Delivery In Vitro and In Vivo

Wei Liu,Meihui Zhang,Huiyuan Lv,Chuanxu Yang

Background : Lipid nanoparticles (LNPs) represent one of the most effective non-viral vectors for nucleic acid delivery and have demonstrated clinical success in siRNA therapies and mRNA vaccines. While considerable research has focused on optimizing ionizable lipids and helper lipids, the impact of PEGylated lipid content on LNP-mediated mRNA delivery, especially in terms of in vitro transfection efficiency and in vivo performance, remains insufficiently understood. Methods : In this study, LNPs were formulated using a self-synthesized ionizable lipid and varying molar ratios of DMG-PEG2000. Nanoparticles were prepared via nanoprecipitation, and their physicochemical properties, mRNA encapsulation efficiency, cellular uptake, and transfection efficiency were evaluated in HeLa and DC2.4 cells. In vivo delivery efficiency and organ distribution were assessed in mice following intravenous administration. Results : The PEGylated lipid content exerted a significant influence on both the in vitro and in vivo performance of LNPs. A bell-shaped relationship between PEG content and transfection efficiency was observed: 1.5% DMG-PEG2000 yielded optimal mRNA transfection in vitro, while 5% DMG-PEG2000 resulted in the highest transgene expression in vivo. This discrepancy in optimal PEG content may be attributed to the trade-off between cellular uptake and systemic circulation: lower PEG levels enhance cellular internalization, whereas higher PEG levels improve stability and in vivo bioavailability at the expense of cellular entry. Furthermore, varying the PEG-lipid content enabled the partial modulation of organ distribution, offering a formulation-based strategy to influence biodistribution without altering the ionizable lipid structure. Conclusions : This study highlights the critical role of PEGylated lipid content in balancing nanoparticle stability, cellular uptake, and in vivo delivery performance. Our findings provide valuable mechanistic insights and suggest a straightforward formulation-based strategy to optimize LNP/mRNA systems for therapeutic applications.

研究领域: 药学 · 纳米技术 · 基因递送 · 生物医学工程 · RNA治疗
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CHEMICAL ENGINEERING JOURNAL · 2021 · IF 13.273

Super-elastic smart phase change material (SPCM) for thermal energy storage

Haiquan Zhang,Zijing Liu,Junping Mai,Ning Wang,Jie Zhong,Xianmin Mai,Nan Zhang

Super-elastic phase change materials (SPCMs), as brand-novel smart materials, have a wide range of potential applications in stress induction, thermal energy storage and temperature control. Polyacrylamide-based [email protected] _12h SPCMs with an ultimate tensile ratio greater than 500% were synthesized for the first time by a popular molecular self-assembly technology. In-situ polymerized polyacrylamide (PAM) builds a reversible deformable three-dimensional network, while the filled PEG2000 PCMs form hydrogen bonds with its amino group (–NH 2 ). 260% tensile ratio is impossible to cause obvious liquid leakage for the [email protected] form-stable phase change material, even exceeding the melting temperature of the PEG2000 PCM. Reversible PAM–NH 2 ⋯O–PEG hydrogen bond can also reduce the sensitivity of the polyacrylamide-based hydrophobically associated hydrogel (HAH) to air humidity fluctuations. Volumetric deformation ratio of the as-prepared PCM gel is close to zero during water vapour adsorption/desorption, which is much lower than that of the HAH without PEG2000 (20 vol%). Water molecules entering the self-prepared SPCMs are preferentially adsorbed by the PAM 3D architecture, which significantly improves the anti-interference ability of the PEG PCMs. The outstanding comprehensive performance makes the [email protected] SPCMs have great potential in the future.

研究领域: 材料科学 · 热能工程 · 化学工程
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Journal of Materials Chemistry B · 2020 ·Vol. 8 ·期 9 ·1841-1851 · IF 5.344

Improving the anti-inflammatory efficacy of dexamethasone in the treatment of rheumatoid arthritis with polymerized stealth liposomes as a delivery vehicle

Qin Wang,Liming He,Donghao Fan,Wenlang Liang,Jiyu Fang

Rheumatoid arthritis (RA) is an autoimmune disease that causes chronic inflammation of the joints of the body. Although liposomes are a promising drug delivery vehicle, there is still a challenge of using conventional liposomes for the treatment of RA due to their short circulation time and physicochemical instability in blood vessels. Here, we report the formation of polymerized stealth liposomes composed of 1,2-bis(10,12-tricosadiynoyl)-sn-glycero-3-phosphocholine (DC8,9PC) and 1,2-distearoyl-sn-glycero-3-phospho-ethanolamine-poly(ethyleneglycol) (DSPE-PEG2000) with a thin-film hydration method, in which DC8,9PC molecules are cross-linked in the bilayer of the liposomes by UV irradiation and the PEG chains present at the surface of the liposomes provide a stealth layer. We demonstrate that the polymerized stealth liposomes are stable and show long circulation time in blood vessels. They can be internalized by cells without significant toxicity. After being injected into arthritic rats, the polymerized stealth liposomes with loaded dexamethasone (Dex) show long blood circulation time and accumulate preferentially in inflamed joints, consequently suppressing the level of proinflammatory cytokines (TNF-α and IL-1β) in joint tissues, reducing the swelling of inflamed joints and alleviating the progression of RA. We believe that polymerized stealth liposomes can be used as a promising drug delivery vehicle for various therapeutic applications.

研究领域: 药理学 · 药物递送系统 · 风湿病学 · 纳米技术
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POLYMER BULLETIN · 2022 ·Vol. 80 ·期 2 ·1873-1891 · IF 2.843

A flexible method for changing the transition temperature of polyurethane solid–solid phase change materials

Shi Wenshuo,Wei Kun,Fan Yuzhe,Wang Xiaoqing,Shi Jiahao,Wang Sifan,Cheng Peng

Transition temperature is significant in determining applications of phase change materials. In this paper, PEG2000 and PEG4000 were used as soft segments and MDI and 3,3ʹ-Dichloro-4,4ʹ-diaminodiphenylmethane (MOCA) were used as hard segments. Several polyurethane solid–solid phase change materials (PUSSPCMs) were synthesized by adjusting the mass ratio of PEG4000 and PEG2000. Based on the differential scanning calorimeter test, this paper studied the relationship between the mass ratio of PEG2000 and the phase transition temperature. The influence mechanism of phase change temperature was revealed from molecular structure, crystallization properties, and surface morphology. Furthermore, PUSSPCMs were tested for leakage and the thermal stability. The results showed that the synthesized PUSSPCMs had no liquid leakage during the heating process. There was a good linear relationship between the mass ratio of PEG2000 and phase transition temperature. The thermal decomposition onset temperature was above 230 °C.

CAS / MDL: 101-68-8
研究领域: 材料科学 · 化学工程 · 热能存储
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Advanced Science · 2017 ·Vol. 4 ·期 4 ·1600166 · IF 9.034

Thermally Activated Delayed Fluorescence Organic Dots (TADF Odots) for Time-Resolved and Confocal Fluorescence Imaging in Living Cells and In Vivo

Tingting Li,Dongliang Yang,Liuqing Zhai,Suiliang Wang,Baomin Zhao,Nina Fu,Lianhui Wang,Youtian Tao,Wei Huang

The fluorophores with long-lived fluorescent emission are highly desirable for time-resolved fluorescence imaging (TRFI) in monitoring target fluorescence. By embedding the aggregates of a thermally activated delayed fluorescence (TADF) dye, 2,3,5,6-tetracarbazole-4-cyano-pyridine (CPy), in distearoyl-sn-glycero-3-phosphoethanolamine-poly(ethylene glycol) (DSPE-PEG2000) matrix, CPy-based organic dots (CPy-Odots) with a long fluorescence lifetime of 9.3 μs (in water at ambient condition) and high brightness (with an absolute fluorescence quantum efficiency of 38.3%) are fabricated. CPy-Odots are employed in time-resolved and confocal fluorescence imaging in living Hela cells and in vivo. The green emission from the CPy-Odots is readily differentiated from the cellular autofluorescence background because of their stronger emission intensities and longer lifetimes. Unlike other widely studied DSPE-PEG2000 encapsulated Odots which are always distributed in cytoplasm, CPy-Odots are located mainly in plasma membrane. In addition, the application of CPy-Odots as a bright microangiography agent for TRFI in zebrafish is also demonstrated. Much broader application of CPy-Odots is also prospected after further surface functionalization. Given its simplicity, high fluorescence intensity, and wide availability of TADF materials, the method can be extended to develop more excellent TADF Odots for accomplishing the challenges in future bioimaging applications.

CAS / MDL: 109-99-9
研究领域: 生物医学工程 · 生物成像 · 材料科学 · 细胞生物学
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Advanced Healthcare Materials · 2023 · IF 10

Small Ceria Nanoclusters with High ROS Scavenging Activity and Favorable Pharmacokinetic Parameters for the Amelioration of Chronic Kidney Disease

Qianqian Wu,Lu Yang,Ling Zou,Wang Yang,Qingshan Liu,Anwei Zhang,Jiang Cao,Guangyou Shi,Jian He,Xiaochao Yang

The over production of reactive oxygen species (ROS) plays a critical role in the progression of chronic kidney disease (CKD). Organic ROS scavengers currently used for CKD treatment do not satisfy low dosage and high efficiency requirements. Ceria nanomaterials featured with renewable ROS scavenging activity are potential candidates for CKD treatment. Herein, a method for the synthesis of ceria nanoclusters (NCs) featured with small size of ≈1.2 nm is reported. The synthesized NCs are modified by three hydrophilic ligands with different molecular weights, including succinic acid (SA), polyethylene glycol diacid 600 (PEG600), and polyethylene glycol diacid 2000 (PEG2000). The surface modified NCs exhibit excellent ROS scavenging activity due to the high Ce 3+ /Ce 4+ ratio in their crystal structures. Compared with bigger-sized ceria nanoparticles (NPs) (≈45 nm), NCs demonstrate smoother blood concentration-time curve, lower organ accumulation, and faster metabolic rate superiorities. The administration of NCs to CKD mice, especially PEG600 and PEG2000 modified NCs, can effectively inhibit oxidative stress, inflammation, renal fibrosis, and apoptosis in their kidneys. Due to these benefits, the constructed NCs can ameliorate the progression of CKD. These findings suggest that NCs is a potential redox nanomedicine for future clinical treatment of CKD.

CAS / MDL: 25952-53-8
研究领域: 纳米技术 · 药学 · 肾病学 · 生物医学工程
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MOLECULAR PHARMACEUTICS · 2024 · IF 4.5

Self-Delivery Nanomedicines Reverse Thermal Resistance to Enhance Tumor Mild-Temperature Photothermal Therapy

Jinmei Lai,Qunying Shi,Yongqi Xie,Yinyin Zhu,Shiyu Liang,Yi Chen,Jiali Yuan,Lihan Liu

Tumoral thermal defense mechanisms considerably attenuate the therapeutic outcomes of mild-temperature photothermal therapy (PTT). Thus, developing a simple, efficient, and universal therapeutic strategy to sensitize mild-temperature PTT is desirable. Herein, we report self-delivery nanomedicines ACy NPs comprising a near-infrared (NIR) photothermal agent (Cypate), mitochondrial oxidative phosphorylation inhibitor (ATO), and distearoylphosphatidylethanolamine-polyethylene glycol 2000 (DSPE–PEG2000), which have a high drug-loading efficiency that can reverse tumoral thermal resistance, thereby increasing mild-temperature PTT efficacy. ACy NPs achieved targeted tumor accumulation and performed NIR fluorescence imaging capability in vivo to guide tumor PTT for optimized therapeutic outcomes. The released ATO reduced intracellular ATP levels to downregulate multiple heat shock proteins (including HSP70 and HSP90) before PTT, which reversed the thermal resistance of tumor cells, contributing to the excellent results of mild-temperature PTT in vitro and in vivo. Therefore, this study provides a simple, biosafe, advanced, and universal heat shock protein-blocking strategy for tumor PTT.

CAS / MDL: 41532-84-7
研究领域: 纳米技术 · 肿瘤学 · 治疗诊断学 · 生物医学工程
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ACS Applied Materials & Interfaces · 2021 · IF 9.229

pH-Triggered Copper-Free Click Reaction-Mediated Micelle Aggregation for Enhanced Tumor Retention and Elevated Immuno–Chemotherapy against Melanoma

Miao Deng,Rong Guo,Shuya Zang,Jingdong Rao,Mengmeng Li,Xian Tang,Chunyu Xia,Man Li,Zhirong Zhang,Qin He

Natural killer (NK) cell-based immunotherapy presents a promising antitumor strategy and holds potential for combination with chemotherapy. However, the suppressed NK cell activity and poor tumor retention of therapeutics hinder the efficacy. To activate NK cell-based immuno–chemotherapy and enhance the tumor retention, we proposed a pH-responsive self-aggregated nanoparticle for the codelivery of chemotherapeutic doxorubicin (DOX) and the transforming growth factor-β (TGF-β)/Smad3 signaling pathway inhibitor SIS3. Polycaprolactone-poly(ethylene glycol) (PCL-PEG2000) micelles modified with dibenzylcyclooctyne (DBCO) or azido (N3) and coated with acid-cleavable PEG5000 were established. This nanoplatform, namely, M-DN@DOX/SIS3, could remain well dispersed in the neutral systemic circulation, while quickly respond to the acidic tumor microenvironment and intracellular lysosomes, triggering copper-free click reaction-mediated aggregation, leading to the increased tumor accumulation and reduced cellular efflux. In addition, the combination of DOX with SIS3 facilitated by the aggregation strategy resulted in potent inhibition of melanoma tumor growth and significantly increased NK cells, NK cell cytokines, and antitumor T cells in the tumor. Taken together, our study offered a new concept of applying copper-free click chemistry to achieve nanoparticle aggregation and enhance tumor retention, as well as a promising new combined tumor treatment approach of chemotherapy and immunotherapy.

研究领域: 癌症研究 · 纳米技术 · 免疫疗法 · 化疗 · 药学
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