Polymers
·
2017
·Vol. 9
·期 12
·698
·
IF 3.364
Yinglei Zhai,Xing Zhou,Lina Jia,Chao Ma,Ronghua Song,Yanhao Deng,Xueyao Hu,Wei Sun
The differences in micro-environment between cancer cells and the normal ones offer the possibility to develop stimuli-responsive drug-delivery systems for overcoming the drawbacks in the clinical use of anticancer drugs, such as paclitaxel, doxorubicin, and etc. Hence, we developed a novel endosomal pH-sensitive paclitaxel (PTX) prodrug micelles based on functionalized poly(ethylene glycol)-poly(ε-caprolactone) (mPEG-PCL) diblock polymer with an acid-cleavable acetal (Ace) linkage (mPEG-PCL-Ace-PTX). The mPEG-PCL-Ace-PTX5with a high drug content of 23.5 wt % was self-assembled in phosphate buffer (pH 7.4, 10 mM) into nanosized micelles with an average diameter of 68.5 nm. The in vitro release studies demonstrated that mPEG-PCL-Ace-PTX5micelles was highly pH-sensitive, in which 16.8%, 32.8%, and 48.2% of parent free PTX was released from mPEG-PCL-Ace-PTX5micelles in 48 h at pH 7.4, 6.0, and 5.0, respectively. Thiazolyl Blue Tetrazolium Bromide (MTT) assays suggested that the pH-sensitive PTX prodrug micelles displayed higher therapeutic efficacy against MCF-7 cells compared with free PTX. Therefore, the PTX prodrug micelles with acetal bond may offer a promising strategy for cancer therapy.Keywords:prodrug;polymer micelles;pH-sensitive;acetal;paclitaxel
研究领域:
药学
·
肿瘤学
✓ 已验证
DOI
PubMed
高影响因子
INDUSTRIAL & ENGINEERING CHEMISTRY RESEARCH
·
2013
·
IF 2.206
Yan-Ling Luo,Li-Li Chen,Yan Miao,Feng Xu
Novel AB4-type polyurethane (PU) micelle-like amphiphilic block copolymers consisting of hydroxyl-functionalized carboxyl-terminated poly(butadiene-co-acrylonitrile) (f-CTBN) as the hydrophobic cores and methoxy poly(ethylene glycol) (MPEG) as the hydrophilic branched blocks were synthesized via esterification, followed by coupling reaction. Their chemical structure and molecular weight were characterized by FTIR, NMR, and SEC measurements. The block copolymers could easily self-assemble to form core–shell micelle nanoparticles in various media. The micelles bear a critical micelle concentration (CMC) in a range from 0.740 to 6.310 mg L–1 and were very stable even in PBS solutions. The TEM and DLS findings revealed that the micelles were almost spherical and narrow-size-distribution, with TEM mean diameters from 13 to 24 nm, and average hydrodynamic diameter about 124–151 nm. All these depended on chain lengths and compositional ratios of hydrophilic MPEG blocks. The drug loading and in vitro release indicated that the self-assembled micelle nanoparticles could effectively load hydrophobic prednisone, with encapsulation capacity of about 27–30%, and the drug release from the nanoparticles was dependent on MPEG chain lengths and the molar ratios of f-CTBN to MPEG. Cytotoxicity assays disclosed that the as-prepared block copolymer micelle nanoparticles exhibit good biocompatibility and could be employed as potential drug controlled release carriers.
研究领域:
生物材料
·
药物递送
·
纳米医学
·
高分子化学
·
药剂学
✓ 已验证
DOI
高影响因子
Biomaterials Science
·
2026
·
IF 6.1
Qi Zhang,Luyao Wang,Zhaofan Yang,Hao Meng,Shixian Lv,Linlin Liu
Chemo-immunotherapy aims to integrate chemotherapy-induced antigen release with innate immune activation to achieve enhanced antitumor efficacy. However, the pharmacokinetic mismatch and systemic toxicity of free small molecules often compromise the synergistic effects. Herein, we propose a reactive oxygen species (ROS)-responsive nanoplatform based on mPEG–PCL for the co-delivery of a paclitaxel (PTX) prodrug and the TLR7/8 agonist R848. The nanoparticles remain stable under physiological conditions while releasing drug in oxidative tumor microenvironments, thereby achieving synchronous intratumoral delivery and activation. In vitro, the system exhibited efficient intracellular uptake and potent cytotoxicity against tumor cells while maintaining low toxicity toward normal cells due to prodrug design. Moreover, the platform effectively induced immunogenic cell death and promoted dendritic cell maturation, highlighting its capacity for chemo-immunotherapeutic synergy. This co-delivery strategy provides a versatile approach to realize controllable and safe chemo-immunotherapy through stimuli-responsive nanomedicine design.
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF LUMINESCENCE
·
2026
·
IF 3.8
Jingran Zhang,LiYan Zheng,Guifu Zuo,Yuchen Yue,Qian Zhang,Mengnan Zhang
Lead-free copper halides have emerged as promising self-trapped exciton (STE) emitters for broadband white-light generation, yet the direct construction of compositionally regulated single-matrix white emitters remains challenging. This study presents an mPEG-NH 2 -directed phase-engineering strategy for the one-step in situ construction of biphasic Cs 3 Cu 2 I 5 /CsCu 2 I 3 copper halides. By introducing methoxy polyethylene glycol amine into the ligand-assisted reprecipitation (LARP) process, the local coordination environment and supersaturation-driven nucleation behavior of Cs + , Cu + , and I − species are regulated, enabling the coexistence of blue-emitting Cs 3 Cu 2 I 5 and yellow-emitting CsCu 2 I 3 within one crystallization system. The amino and ether oxygen sites of mPEG-NH 2 further promote interfacial coupling with the copper halide matrix, reducing non-radiative STE deactivation and improving radiative recombination. The optimized CCI:3P sample exhibits broadband white-light emission with Commission Internationale de l’Éclairage (CIE) coordinates of (0.3236, 0.3347), a photoluminescence (PL) quantum yield of 42.8%, and a prolonged exciton lifetime. A UV-pumped WLED based on CCI:3P emits white light with a correlated color temperature of 6052 K. In addition, the biphasic material exhibits distinct water- and heat-induced luminescence changes, demonstrating stimulus-dependent optical contrast. This work provides a polymer-directed strategy for designing lead-free copper halide emitters with integrated white-light emission and responsive optical functionality.
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产品关联
DOI
高影响因子
Nanomaterials
·
2025
·Vol. 15
·期 8
·615
·
IF 4.3
Ren Li,Yi Zhu
Sulforaphane (SFN) is a natural isothiocyanate compound with multiple bioactive effects, abundantly found in cruciferous vegetables. SFN and cadmium (Cd) were limited in their application as chemotherapeutic agents due to insufficient cellular uptake, low bioavailability, and high systemic toxicity, respectively. In this study, mPEG-PLGA nanoparticles were used as a carrier to load Cd-γ-PGA conjugates and SFN, enabling favorable drug release under acidic microenvironments with excellent pH responsiveness. The NP-Cd-SFN nanoparticles exhibited a particle size of 102.1 nm, a zeta potential of -14.48 mV, and a PDI value of 0.257. These characteristics contribute to the nanoparticles’ prolonged circulation in the bloodstream and their ability to passively target tumors. Compared to the single-dose groups and the combined Cd + SFN group, the NP-Cd-SFN group significantly reduced the viability of HepG2 cells and increased their apoptosis rate by inducing mitochondrial oxidative stress and promoting cell apoptosis. Overall, the addition of SFN and the encapsulation of mPEG-PLGA enhanced the therapeutic effects of Cd on HepG2 cells.
研究领域:
药剂学
·
肿瘤学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF MATERIALS SCIENCE-MATERIALS IN MEDICINE
·
2015
·Vol. 27
·期 2
·1-13
·
IF 2.587
Guan Qingxia,Sun Shuang,Li Xiuyan,Lv Shaowa,Xu Ting,Sun Jialin,Feng Wenjing,Zhang Liang,Li Yongji
This study investigated the therapeutic efficiency of monomethoxy polyethylene glycol-poly(lactic-co-glycolic acid) (mPEG-PLGA) co-loaded with syringopicroside and hydroxytyrosol as a drug with effective targeting and loading capacity as well as persistent circulation in vivo. The nanoparticles were prepared using a nanoprecipitation method with mPEG-PLGA as nano-carrier co-loaded with syringopicroside and hydroxytyrosol (SH-NPs). The parameters like in vivo pharmacokinetics, biodistribution in vivo, fluorescence in vivo endomicroscopy, and cellular uptake of SH-NPs were investigated. Results showed that the total encapsulation efficiency was 32.38 ± 2.76 %. Total drug loading was 12.01 ± 0.42 %, particle size was 91.70 ± 2.11 nm, polydispersity index was 0.22 ± 0.01, and zeta potential was −24.5 ± 1.16 mV for the optimized SH-NPs. The nanoparticle morphology was characterized using transmission electron microscopy, which indicated that the particles of SH-NPs were in uniformity within the nanosize range and of spherical core shell morphology. Drug release followed Higuchi kinetics. Compared with syringopicroside and hydroxytyrosol mixture (SH), SH-NPs produced drug concentrations that persisted for a significantly longer time in plasma following second-order kinetics. The nanoparticles moved gradually into the cell, thereby increasing the quantity. ALT, AST, and MDA levels were significantly lower on exposure to SH-NPs than in controls. SH-NPs could inhibit the proliferation of HepG2.2.15 cells and could be taken up by HepG2.2.15 cells. The results confirmed that syringopicroside and hydroxytyrosol can be loaded simultaneously into mPEG-PLGA nanoparticles. Using mPEG-PLGA as nano-carrier, sustained release, high distribution in the liver, and protective effects against hepatic injury were observed in comparison to SH.
研究领域:
药剂学
·
药理学
·
纳米技术
·
药物递送系统
·
肝病学
✓ 已验证
DOI
PubMed
高影响因子
PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
·
2022
·
IF 3.915
Yujia Liu,Xiaoyu Lu,Zhenhai Zhang,Shulong Jiang,Huixia Lv
In this study, amphiphilic block copolymer mPEG-cholic acid was synthesized in conjunction with TPGS as stabilizer to prepare multifunctional micelles. The formed polymeric micelles (PCTm) were used for the delivery of paclitaxel (PTX) and bufalin (BF). PEG group could enhance solubility and extend circulation time, while cholic acid groups achieved the liver targeted function. Combinations of these approaches could realize a synergistic therapeutic effect in the treatment of advanced hepatocellular carcinoma. CLSM in vitro results demonstrated that drug capsulation into PCTm could enhance cellular uptake. FCM results confirmed the uptake amount of C6/PCTm was 7.5-fold higher than that of free C6 after incubation for 2 h. Competitive inhibition test proved the Na+-taurocholate co-transporting polypeptide (NTCP) involved in the uptake mechanism of PCTm. Meanwhile, in vivo imaging assays demonstrated that the fluorescence intensity of Cy5.5/PCTm was higher than that of free Cy5.5 on liver and tumor with extended circulation time to 48 h. In addition, in vivo studies confirmed that the combined therapy exhibited the strongest tumor inhibition rate of 82.29% with lower systemic toxicity. Hence, these results indicated that PCTm could provide a promising strategy for targeting hepatocellular carcinoma and achieve the goal of synergism and attenuation.
研究领域:
药学
·
癌症研究
·
药物递送系统
·
生物医学工程
✓ 已验证
DOI
PubMed
高影响因子
ENGINEERING IN LIFE SCIENCES
·
2019
·
IF 1.936
Xianpan Ye,Jiugang Yuan,Zhe Jiang,Shuoxuan Wang,Ping Wang,Qiang Wang,Li Cui
Wool keratin is a natural material with excellent properties, which is considered as scaffold biomaterial for tissue engineering. Polyethylene glycol can improve the mechanical properties of keratin materials because of its excellent biocompatibility and plasticity. In the present work, poly (ethylene glycol) methyl ether methacrylate (MPEGMA) was grafted onto keratin by thiol-ene photoclick reaction. The results of FTIR and SDS-PAGE verified the successful reaction between MPEGMA and keratin. Compared with the keratin, circular dichroism and XRD results showed that the β-sheet ratio increased in MPEG-g-keratin. Additionally, it can be found that the exposure of keratin hydrophobic amino acids increased quickly and the micelle size became larger due to the introduction of MPEG from the results of fluorescence spectroscopy and particle size analysis. The MPEG-g- keratin was formed into a membrane to further study the application of the modified keratin. Compared with the keratin membrane, the flexibility and biocompatibility of modified keratin have been improved. This work provides an eco-friendly and facile approach for preparation of the keratin biomaterials.
研究领域:
材料科学
·
生物医学工程
·
高分子化学
·
组织工程
✓ 已验证
DOI
高影响因子
International Journal of Nanomedicine
·
2019
·
IF 4.471
Wenchao Wu,Jiangqing Wu,Qiafan Fu,Chenhao Jin,Fangyuan Guo,Qinying Yan,Qingliang Yang,Danjun Wu,Yan Yang,Gensheng Yang
Purpose: Clinical applications of curcumin (Cur) have been greatly restricted due to its low solubility and poor systemic bioavailability. Three-arm amphiphilic copolymer tricarballylic acid-poly (ε-caprolactone)-methoxypolyethylene glycol (Tri-CL-mPEG) nanoparticles (NPs) were designed to improve the solubility and bioavailability of Cur. The present study adopted a microchannel system to precisely control the preparation of self-assembly polymeric NPs via liquid flow-focusing and gas displacing method.Methods: The amphiphilic three-arm copolymer Tri-CL-mPEG was synthesized and self-assembled into nearly spherical NPs, yielding Cur encapsulated into NP cores (Cur-NPs). The obtained NPs were evaluated for physicochemical properties, morphology, toxicity, cellular uptake by A549 cells, release in vitro, biodistribution, and pharmacokinetics in vivo.Results: Rapidly fabricated and isodispersed Cur-NPs prepared by this method had an average diameter of 116±3 nm and a polydispersity index of 0.197±0.008. The drug loading capacity and entrapment efficiency of Cur-NPs were 5.58±0.23% and 91.42±0.39%, respectively. In vitro release experiments showed sustained release of Cur, with cumulative release values of 40.1% and 66.1% at pH 7.4 and pH 5.0, respectively, after 10 days post-incubation. The results of cellular uptake, biodistribution, and in vivo pharmacokinetics experiments demonstrated that Cur-NPs exhibited better biocompatibility and bioavailability, while additionally enabling greater cellular uptake and prolonged circulation with possible spleen, lung, and kidney targeting effects when compared to the properties of free Cur.Conclusion: These results indicate that Tri-CL-mPEG NPs are promising in clinical applications as a controllable delivery system for hydrophobic drugs.
研究领域:
药剂学
·
纳米医学
·
生物材料
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF APPLIED POLYMER SCIENCE
·
2021
·Vol. 138
·期 30
·50731
·
IF 3.125
Mengqing Jiang,Yihua Yin,Weiquan Cai,Jingli Zhang,Lihong Fan,Ying Yi,Yue Dai,Ting Zhou,Jinsheng Liu
To improve photostability and enhance utilization rate and reduce pest resistance, a new strategy based on the combination of photodynamic insecticide action and stimulus-responsive polymer micelles is developed. 4-(phenylazo)benzoic acid (PBA)-modified poly(ethylene glycol) monomethyl ether (mPEG) conjugate is prepared by the esterification reaction of mPEG and PBA, and followed by self-assembly in aqueous solution to obtain polymeric nanoparticles. TEM shows that the nanoparticles have a core-shell structure and an average diameter of 78 nm. DLS shows that the nanoparticles are stability in water solution but can change their structure in response to UV light and/or esterase stimulation. The photodegradation of Protoporphyrin IX (PpIX) encapsulated in the nanoparticles can be effectively inhibited because of aggregation-caused quenching effect, whose maximum photodegradation rate is about 20.54% after 8 h exposure to daylight compared with the complete photodegradation of free PpIX. UV light and/or esterase stimulus can trigger PpIX release and result in a high photodynamic activity. Compared with free PpIX, the PpIX-loaded nanoparticles show a higher phototoxicity to insect cells and the daylight pretreatment has little influence on the phototoxicity.
研究领域:
农业科学
·
材料科学
·
生物学
✓ 已验证
产品关联
DOI
高影响因子
MACROMOLECULAR RESEARCH
·
2023
·Vol. 31
·期 3
·181-191
·
IF 2.4
Li Jiyu,Zhu Li,Wu Shuai,Wang Guixue,Chen Yidan,Wu Wei
Chemotherapy is the main strategy for inhibiting the tumor growth. However, during the therapy, the side effect of anti-cancer drug will injure normal cells. For reducing the toxic of the free drug, stimuli responsive nanoparticles (NPs) have been prepared base on the pathological acidic environment around tumor for safe and efficient anti-tumor applications. In this study, we fabricated the phenylboronic acid (PBA) modified monomethoxy polyethylene glycol (MEPG) for encapsulating doxorubicin (DOX NPs). In the drug delivery system (DDS), the pH-responsive boric ester could be stable during drug delivery, and enhance DOX rapidly release in tumor lesion under the acidic stimuli. In vitro studies further demonstrated that DOX NPs could efficiently endocytose by tumor cells, and exhibit the similar anti-tumor activity as the free DOX resulting from the pH-responsive drug release profiles under tumor acidic stimuli. In summary, DOX NPs could be a feasible candidate to improve the safe and efficient DOX delivery for improving the potential anti-tumor applications. Graphical abstract
研究领域:
药学
·
纳米技术
·
癌症研究
✓ 已验证
产品关联
DOI
高影响因子
RSC Advances
·
2014
·Vol. 4
·期 98
·55139-55149
·
IF 3.708
Jinlong Yang,Chunmei Gao,Shaoyu Lü,Xinggang Wang,Mingjia Chen,Mingzhu Liu
A novel amphiphilic polymer (mPEGylated starch-deoxycholic acid, mPEG-St-DCA) was successfully prepared by grafting hydrophobic deoxycholic acid (DCA) into mPEGylated starch. According to the characterization of 1H NMR and FTIR, mPEG-St-DCA polymers could self-assemble into micelles with spherical core–shell structures. With the degree of substitution (DS) of DCA increasing, the average size of micelles (pH 7.4) decreased to below 200 nm. Correspondingly, the critical micelle concentration (CMC) decreased from 0.048 to 0.022 mg mL−1. And zeta potential values were near −2 mV. But under the condition of pH 6.5, the size and CMC showed an increasing trend. Doxorubicin (DOX), a model anticancer drug, was efficiently loaded into mPEG-St-DCA micelles, and in vitro release exhibited that DOX-loaded micelles had a good in vitro pH-induced drug release. MTT assays confirmed that mPEG-St-DCA micelles were biocompatible with HeLa cells, and DOX-loaded micelles had a relatively better cytotoxicity against HeLa cells with a remarkably high IC50 of 5.74 μg mL−1. Confocal laser scanning microscopy (CLSM) analyses demonstrated that mPEG-St-DCA micelles could be internalized efficiently by HeLa cells to realize intracellular DOX release, which further enhanced the inhibition of cell proliferation. On the basis of the above results, it was indicated that novel amphiphilic mPEG-St-DCA micelles with pH-response could be used as drug delivery carriers for cancer therapy.
研究领域:
生物材料学
·
药剂学
·
肿瘤学
✓ 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）