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Journal of Materials Chemistry B · 2019 ·Vol. 7 ·期 17 ·2835-2844 · IF 5.047

Accurate intracellular and in vivo temperature sensing based on CuInS2/ZnS QD micelles

Hui Zhang,Youshen Wu,Zhenhai Gan,Yuexuan Yang,Yiming Liu,Peng Tang,Daocheng Wu

Accurate and sensitive temperature sensing is of great importance for studying biological activities in cells and tissues. Due to the complexity of the microenvironments, most of the existing thermometry systems cannot meet the needs of accurate intracellular and in vivo temperature sensing with high-sensitivity and low-toxicity. After investigation, we found that the fluorescence intensity of CuInS2/ZnS quantum dots (QDs) is significantly temperature dependent, and these QDs can be used for intracellular and in vivo temperature sensing after being encapsulated by amphiphilic micelles (QD-micelles). These QD-micelles have a size of approximately 10.1 ± 2.5 nm and an emission band of approximately 650 nm with intense photoluminescence (PL). Meanwhile, its high thermal sensitivity of 2% °C−1 at near-room temperature is insensitive to solution pH, ionic strength, and protein concentration. Even at a concentration of 300 μg mL−1, our QD-micelles do not exert cytotoxic effects on HeLa and PC-3 cells. Similar to being dispersed in water, the QD-micelles continue to exhibit a high thermal sensitivity of 2.0% °C−1 intracellular and 2.1% °C−1 in tumor tissues, and the PL intensity (I) and temperature (T) over the physiological temperature range have a good linear correlation. Therefore, they have considerable potential in biomedical applications.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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INTERNATIONAL IMMUNOPHARMACOLOGY · 2025 · IF 4.7

Dual-targeted hybrid micelles mediated by VCAM-1 suppress synovial angiogenesis in rheumatoid arthritis

Yuanyuan Wang,Ruibo Guo,Baoli Xu,Ming Zou,Liang Kong,Chuan Tang,Runchao Jiang,Wei Wang,Xuan Zhang,Guangyao Lv

Introduction: Rheumatoid arthritis (RA) is an autoimmune disease characterized by persistent synovitis and the formation of pannus, leading to proliferation of synovial tissue and destruction of bone and cartilage. Traditional drug therapy is often limited by the lack of drug targeting and the continuous synovial angiogenesis. Herein, a dual-targeted micelles for macrophages and vascular endothelial cells with excellent anti-inflammatory and anti-angiogenic properties was constructed to effectively treat RA. Methods: We developed vascular cell adhesion molecule-1 (VCAM-1) binding peptide modified polyphyllin I (PPI) loaded micelles (VM-PE@Ms) in which eucommia ulmoides polysaccharide (EUP) was used as the hydrophilic parts of the hybrid micelles. The targeting, ROS scavenging effect, anti-inflammatory activity, and inhibition of angiogenesis of the micelles were assessed in vitro. Collagen-induced arthritis (CIA) rats model was employed to explore targeting, impact on inflammatory cytokine levels, and cartilage protective effect of the micelles in vivo. Results: VM-PE@Ms. exhibited targeting to both activated RAW264.7 cells and human umbilical vein endothelial cells (HUVECs), and strong inhibitory effect of inflammatory cytokine secretion, ROS generation, and angiogenesis. In vivo assays demonstrated that VM-PE@Ms. displayed desirable pharmacodynamics property, which was confirmed by precise inflammatory joint targeting and retention capacity and bone erosion remission effects and was related to suppression of inflammation and synovial angiogenesis. Conclusion: In summary, the proposed dual-targeted hybrid micelles have the potential role for anti-inflammatory and anti-angiogenic therapy of RA.

CAS / MDL: 23491-52-3 57-11-4
研究领域: 纳米医学 · 风湿病学 · 药物递送 · 炎症 · 血管生成
✓ 已验证 产品关联 DOI PubMed 高影响因子
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BIOMATERIALS · 2025 · IF 12.9

mTOR-siRNA-Conjugated and Gboxin-Loaded Micelles for Mitochondrial Dysfunction-Driven Synergistic Glioblastoma Therapy

Zhouchun Chen,Qingshan Yang,Mengyu Fan,Tianran Chai,Yang Liu,Xue Xia,Muhammad Ismail,Meng Zheng

Targeting mitochondrial-mediated energy metabolism has emerged as a promising therapeutic strategy for glioblastoma multiforme (GBM), given its crucial role in sustaining the rapid growth and survival of tumor cells. In this study, we developed a combinatory, non-cationic siRNA-conjugated self-assembled micelle system core-encapsulated with Gboxin (siRNA-micelle@Gboxin) designed to induce severe mitochondrial dysfunction in GBM cells. The mTOR-siRNA component in the micelle silences mTOR expression, downregulates mTORC1 activity, and reduces 4EBP1 phosphorylation, leading to inhibition of mRNA translation and disruption of cellular energy metabolism, ultimately resulting in decreased ATP production. Concurrently, the GBM-specific drug Gboxin inhibits oxidative phosphorylation (OXPHOS), directly inducing mitochondrial dysfunction and exacerbating the energy crisis within glioma cells, synergistically accelerating apoptosis through mitochondrial damage. Notably, this dual-target inhibition of mTORC1 and OXPHOS by siRNA-micelle@Gboxin resulted in a more potent, synergistic anti-tumor effect than targeting either pathway alone. These findings highlighted that the Gboxin-loaded siRNA micelle offers a promising and innovative nanotherapeutic approach for GBM treatment, harnessing the synergistic effects of gene silencing and chemotherapy-based mitochondrial disruption to achieve a powerful therapeutic efficacy.

研究领域: 肿瘤学 · 纳米医学 · 分子生物学 · 癌症代谢 · 基因治疗
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COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS · 2025 · IF 5.4

Effect of Gemini surfactants on self-thickening acids: size and morphological changes in micelles

Peng Li,Lei Wang,Gui-qiang Fei,Hua-qiang Shi,Rong Wang,Jin-hao Gao,Zhi-qiang Dang,Xu-jie Lin,Jia-li Chen,Xiao-juan Lai

The micelle behavior between surfactants and hydrophobic associative polymers solves the problem of temperature resistance of self-thickening acids. Gemini betaine 2C 12 -SGS is synthesized from N-[3-(dimethylamino)propyl] lauramide, sodium 3-chloro-2-hydroxy-propanesulfonate, and 1,4-dibromobutane. When Gemini Betaine 2C 12 -SGS was added to the ADOM acid solution, the residual viscosity of the residual acid solution was 103 and 55.67 mPa·s after shearing for 1   h at 150 °C and 180 °C, respectively, which increased by 41.64 and 32.74 mPa·s, respectively, and increased by 67.86% and 142.78%, respectively, compared with those without surfactant. The interaction between surfactants and self-thickening acids provides theoretical support for their composite system to serve as an acidizing fluid for high-temperature carbonate reservoirs.

CAS / MDL: 3179-80-4
研究领域: 胶体与界面化学 · 石油工程材料 · 高分子物理 · 油田化学 · 流变学
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JOURNAL OF PHOTOPOLYMER SCIENCE AND TECHNOLOGY · 2019 ·Vol. 31 ·期 6 ·739-746 · IF 0.934

Synthesis of Water-Soluble Spiropyran-Modified Poly(acrylic acid) Micelles and Their Optical Behaviors

Rui Xue,Xinghua Zhang,Jintao Tian

In this study, a spiropyran derivative (SPOH) is firstly grafted onto a polymer backbone of a poly(acrylic acid) (PAA) via an esterification process. The synthesized spiropyran-modified poly(acrylic acid) (PAA-SP) polymer is characterized by FTIR and 1H NMR. The synthesized PAA-SP is then dissolved into water to achieve water-soluble micelles. The optical behaviors of PAA-SP micelles are investigated by ultraviolet-visible (UV-Vis) absorption spectra and fluorescence emission spectra under acid/base and light stimuli in aqueous solution. Our experimental results reveal that the as-prepared PAA-SP micelles are water-soluble and show good photochromic and emissive behaviors. Meanwhile, the optical behaviors of the micelles are light-responsive and acid/base-responsive and hence can be tailored via the adjustments of both light and pH value of the solution sample. And our results may be meaningful for practical application of hydrophobic spiropyran derivatives in aquatic environments.

研究领域: 材料科学 · 化学
✓ 已验证 DOI 高影响因子
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CHEMICAL PHYSICS LETTERS · 2022 · IF 2.719

Redox-responsive nano-micelles containing trisulfide bonds to enhance photodynamic efficacy of zinc naphthalocyanine

Xian-hui He,Mao Zhao,Xue-ying Tian,Yu-jun Lu,Shun-yu Yang,Qian-rong Peng,Min Yang,Wen-wen Jiang

A novel amphiphilic polymer with the trisulfide bond was developed. The nano-micelles could be formed through the self-assembling of this polymer with hydrophobic zinc naphthalocyanine, a NIR-absorbing photosensitizer. The micelles showed unique rods, high drug loading, high stability, high sensitivity to GSH, and excellent biosafety. The singlet oxygen production quantum yield of micelles was obviously higher than that of free photosensitizers and micelles containing disulphide bonds in the simulated tumor environment. The phototoxicity of micelles in cancer cells was significant. The redox response drug-loaded micelle was promising to enhance the photodynamic efficacy of zinc naphthalocyanine in cancer cells.

研究领域: 纳米技术 · 药学 · 癌症研究 · 生物医学工程
✓ 已验证 DOI 高影响因子
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MOLECULAR PHARMACEUTICS · 2017 · IF 4.44

Calcium Phosphate-Reinforced Reduction-Sensitive Hyaluronic Acid Micelles for Delivering Paclitaxel in Cancer Therapy

Bing Deng,Mengxin Xia,Jin Qian,Rui Li,Lujia Li,Jianliang Shen,Guowen Li,Yan Xie

For addressing the dilemma of in vivo stability and antitumor effects of micellar drugs, novel organic and inorganic hybridized nanoparticle, that is, hyaluronic acid-mineralized micelles, are designed to efficiently deliver paclitaxel (PTX). The resulting micelles exhibit excellent drug loading (30.6%) and entrapment efficiency (87.8%) for PTX with a small size (134.8 nm). Notably, the dual-sensitive release of PTX-loaded mineralized micelles is obtained in the conditions of 40 mM GSH and pH 5.0, whereas release is slow in the physiological environment. With favorable cell uptake, mineralized micelles show decent tumor accumulation, which corresponds to their significant targeting capacity from the observed real-time images. Compared with Taxol, PTX-loaded mineralized micelles show a lower half-maximal inhibitory concentration value (0.025 μg/mL), higher cell apoptosis rate (23.5%) in MDA-MB-231 cells, lower systemic toxicity to nude mice, and more potent in vivo tumor inhibition (1.57-times higher than that of Taxol (p < 0.05)).

研究领域: 药剂学 · 肿瘤学 · 纳米医学
✓ 已验证 DOI PubMed 高影响因子
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Acta Biomaterialia · 2015 · IF 6.025

Enhanced antitumor efficacy by cyclic RGDyK-conjugated and paclitaxel-loaded pH-responsive polymeric micelles

Yajie Gao,Yanxia Zhou,Lei Zhao,Chao Zhang,Yushu Li,Jinwen Li,Xinru Li,Yan Liu

Cyclic RGDyK (cRGDyK)-conjugated pH-sensitive polymeric micelles were fabricated for targeted delivery of paclitaxel to prostate cancer cells based on pH-sensitive copolymer poly(2-ethyl-2-oxazoline)-poly( d , l -lactide) (PEOz-PLA) and cRGDyK-PEOz-PLA to enhance antitumor efficacy. The prepared micelles with an average diameter of about 28   nm exhibited rapid release behavior at endo/lysosome pH, effectively enhanced the cytotoxicity of paclitaxel to PC-3 cells by increasing the cellular uptake, which was correlated with integrin α v β 3 expression in tumor cells. The active targeting activity of the micelles was further confirmed by in vivo real time near-infrared fluorescence imaging in PC-3 tumor-bearing nude mice . Moreover, the active targeting and pH-sensitivity endowed cRGDyK-conjugated micelles with a higher antitumor effect in PC-3 xenograft-bearing nude mice compared with unmodified micelles and Taxol with negligible systemic toxicity. Therefore, these results suggested that cRGDyK-conjugated pH-sensitive polymeric micelles may be a promising delivery system for efficient delivery of anticancer drugs to treat integrin α v β 3 -rich prostate cancers.

研究领域: 药剂学 · 肿瘤学 · 生物材料学
✓ 已验证 DOI PubMed 高影响因子
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EUROPEAN POLYMER JOURNAL · 2015 · IF 3.005

Zwitterionic polymeric micelles that undergo a pH-triggered positive charge for enhanced cellular uptake

Jiawei Lu,Huiyan Jia,Leijia Guo,Genghui Zhang,Youjia Cao,Husheng Yan,Keliang Liu

To achieve a good stealth property and to enhance the uptake by tumor cells, polymeric micelles containing a slightly negatively charged and zwitterionic corona at pH 7.4 (i.e., blood pH) and a positively charged surface at a slightly acidic pH (i.e., tumor extracellular pH) were prepared. The amphiphilic diblock copolymer which was used to prepare the polymeric micelles contains a hydrophilic block comprised of nonionic hydrophilic groups, negatively charged groups (carboxyl groups) and pH-triggered positive charge-generation groups (morpholino groups). The zeta potential of the micelles was found to increase as the pH decreased over the pH range covering the blood and tumor tissue pH ranges, and the corona of the micelles should contain zwitterionic groups. This could be due to that, in the pH range studied, more morpholino groups become protonated as the pH decreased, whereas the carboxyl groups were almost completely deprotonated to form carboxylate anions. Furthermore, by adjusting the molar ratio of morpholino to carboxyl groups, the zeta potential of the polymeric micelles was controlled to achieve a slightly negative value at pH 7.4. Thus, the combination of a slightly negatively charged surface and a zwitterionic corona suggests that these micelles would possess good stealth property. When the pH decreased from 7.4 to 6.8 or 6.5, the zeta potential value of the micelles became positive due to increased protonation of the morpholino groups. Correspondingly, the cellular uptake of the micelles by HeLa cells was enhanced.

研究领域: 生物材料 · 药剂学
✓ 已验证 DOI 高影响因子
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Acta Biomaterialia · 2015 · IF 6.025

Redox-responsive micelles self-assembled from dynamic covalent block copolymers for intracellular drug delivery

Qinglai Yang,Lianjiang Tan,Changyu He,Bingya Liu,Yuhong Xu,Zhenggang Zhu,Zhifeng Shao,Bing Gong,Yu-Mei Shen

Redox-responsive micelles self-assembled from dynamic covalent block copolymers with double disulfide linkage in the backbone have been developed successfully. The amphiphilic block copolymers PEG–PLA associated with complementary H-bonding sequences can self-assemble into spherical micelles in aqueous media with sizes from 34   nm to 107   nm with different molar mass of PEG and PLA . Moreover, in vitro drug release analyses indicate that reductive environment can result in triggered drug release profiles. The glutathione (GSH) mediated intracellular drug delivery was investigated against HeLa human cervical carcinoma cell line. Flow cytometry and fluorescence microscopy measurements demonstrated that the micelles exhibited faster drug release in glutathione monoester (GSH-OEt) pretreated HeLa cells than that in the nonpretreated cells. Cytotoxicity assay of DOX-loaded micelles indicated the higher cellular proliferation inhibition against 10   mM of GSH-OEt pretreated HeLa cells than that of the nonpretreated ones. These reduction-responsive, biodegradable and biocompatibility micelles could provide a favorable platform to construct excellent drug delivery systems for cancer therapy.

研究领域: 生物材料 · 药剂学 · 肿瘤学
✓ 已验证 DOI PubMed 高影响因子
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POLYMER · 2011 · IF 3.829

Sheddable micelles based on disulfide-linked hybrid PEG-polypeptide copolymer for intracellular drug delivery

Tian-Bin Ren,Wen-Juan Xia,Hai-Qing Dong,Yong-Yong Li

A novel reduction-sensitive sheddable micelle based on disulfide-linked hybrid PEG-polypeptide mPEG-SS-Pleu was demonstrated for intracellular drug delivery . These micelles are composed of an mPEG shell and polypeptide core, characterized by FT-IR, 1 H NMR, fluorescence techniques, TEM , and DLS . Interestingly, they would undergo a fast sheddable process when encounter the reduction sensitive condition, indicated by the aggregation phenomena in the presence of DTT, a reduction agent, which could cleave the disulfide bond between the micellar core and shell and consequently leading to the aggregation of hydrophobic core. Cytotoxicity study revealed that copolymers in this system have good biocompatibility and their self-assembled micelles showed a high drug loading efficiency for DOX , a hydrophobic drug model, and released DOX quantitatively in response to the intracellular level of reducing potential. Cellular uptake experiments demonstrated that the fluorescently labeled micelles could be successfully internalized into human liver carcinoma HepG2 cells, evidenced by confocal laser scanning microscopy . Above results indicate that the copolymers may have great potential in drug delivery to achieve improved cancer therapy.

研究领域: 药剂学 · 生物材料学 · 肿瘤学
✓ 已验证 DOI 高影响因子
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COLLOIDS AND SURFACES B-BIOINTERFACES · 2016 · IF 3.902

Arginine modified polymeric micelles as a novel drug delivery system with enhanced endocytosis efficiency

Song Luo,Yixin Zhang,Jun Cao,Bin He,Sai Li

A new drug delivery system with improved endocytosis efficiency based on arginine modified poly(ethylene glycol)- b -poly(ε-caprolactone) (PEG-PCL) diblock copolymers was developed successfully. The structures of amphiphilic copolymers were verified by proton Nuclear Magnetic Resonance ( 1 H NMR), Fourier Transform Infrared (FTIR) and Gel Permeation Chromatography (GPC). The amphiphilic copolymers could self-assemble into spherical micelles with critical micelle concentration (CMC) at approximately 0.03   mg/mL. Biocompatibility, cellular internalization efficiency and in vitro antitumor effect of the polymeric micelles were studied. Results showed that drug-free micelles were nontoxic to cells. The Confocal Laser Microscopy (CLSM) and the flow cytometry as well as the antitumor activity tests all revealed that drug-loaded micelles modified by arginine groups (guanidino) exhibited higher endocytosis efficiency than those without modification, resulting in a lower IC 50 value to kill tumor cells and meanwhile averting the “competitive binding” problem. Also, in vivo results demonstrated that arginine modified polymeric micelles could deliver the drug to tumor site more efficiently than ones without any modification, thus indicating guanidino in polymeric micelles could benefit the internalization of micelles to fully exert the function of killing tumors. In general, guanidinylation strategy in this splendid novel micelle system has a great potential to improve the therapeutic effect of nanoparticle-based drug delivery system for cancer therapy in the future.

研究领域: 药学 · 生物医学工程 · 肿瘤学
✓ 已验证 DOI PubMed 高影响因子
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