EUROPEAN POLYMER JOURNAL
·
2019
·
IF 3.621
Suzhen Liu,Li Zhang,Xiaohong Chen,Tingting Chu,Yanzhu Guo,Meihong Niu
A novel kind of cationic cellulose- g -oligo(ε-caprolactone) amphiphilic polymer (QC- g -OCL) was obtained by homogeneous ring-opening polymerization of ε-caprolactone (ε-CL) from quaternized cellulose (QC) in 1-butyl-3-methylimidazolium chloride (BmimCl) ionic liquids. Chemical structures and properties of the copolymers were characterized by FT-IR, 1 H NMR, 13 C NMR, XRD and TGA techniques. The grafting ratios of OCL chain onto QC- g -OCL were adjusted by changing the molar ratio of CL to QC. The micelles self-assembled from QC- g -OCL were prepared by ultrasonic-assisted dissolution method, and comprehensively analyzed by dynamic light scattering (DLS), TEM and fluorescence spectroscopy techniques. The micelles were in spherical shape with average hydrodynamic radiuses (R h ) in the range of 170–237 nm. Moreover, their critical micelle concentration (CMC) values were decreased from 0.302 mg/mL to 0.089 mg/mL with increasing the degree substitution values of OCL (DS OCL ) from 0.16 to 0.60. The ζ-potentials of micelles in water were ranged from 37.2 mV to 48.3 mV, indicating that the shells of micelles were constituted by ationic quaternary ammonium group. All of these findings established that the cationic cellulose-based micelles would be a promising aqueous carrier for hydrophobic drug.
研究领域:
材料科学
·
药物传递系统
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DOI
高影响因子
MATERIALS RESEARCH INNOVATIONS
·
2024
·
IF 0
Shuai Li,Hongzhu Lai,Li Jiang,Wenyan Huang,Hongjun Yang,Qimin Jiang,Bibiao Jiang
Polymeric patchy micelles (PPMs) are nanostructures with distinct regions on their surfaces, offering unique properties for various applications. Herein, we present a straightforward method for monitoring the structure of PPMs formed via non-covalent post-assembly modification (NCPAM). By employing 1-pyrenemethylamine, a pyrene-based molecule, as both a modifier and fluorescent probe, we demonstrate that the formation of PPMs with a higher order aggregation state of pyrene induces a stronger pyrene excimer emission. This leads to variations in the excimer-to-monomer emission ratio, serving as a parameter for studying structural changes in PPMs during NCPAM. In situ monitoring of PPM formation and temperature-dependent transformations is achieved using fluorescent analytical method, providing valuable insights into their structural evolution and dynamic behaviour. This study offers a straightforward approach to understanding and controlling PPM structures, facilitating the design of advanced nanomaterials for diverse applications.
研究领域:
材料科学
·
化学
·
纳米技术
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DOI
ACS Biomaterials Science & Engineering
·
2020
·
IF 4.152
Yanzhe Qin,Xinwen Peng
Patients with cancer suffer from severe side effects and reduced life quality, as chemotherapeutic drugs are cytotoxic toward normal cells as well as toward cancer cells. In recent years, nanoparticles have been explored as targeted drug delivery systems; however, problems such as toxicity and instability prevent their practical application. Here, we report the synthesis of cholesteryl–carboxymethyl xylan (CCMX) via an esterification reaction between the carboxyl group of carboxymethyl xylan and the hydroxyl group of cholesterol to form biocompatible micelles as a vehicle for targeted drugs. With its critical micelle concentration (CMC) depending on the degree of substitution (DS) of cholesteryl and ranging from 0.0024 to 0.017 mg/mL, CCMX could self-assemble and form nanoscale micelles in aqueous media. Taking doxorubicin (DOX) as a model drug, the drug encapsulation efficiency (EE%) of CCMX-3 (DS of 0.35 for cholesteryl) reached 91.3%, and this system exhibited excellent internalization ability, as verified by tumor cellular uptake tests. The results of in vitro cytotoxicity and in vivo antitumor activity tests of nude mice demonstrated that CCMX-3/DOX micelles effectively suppressed the growth of tumor cells by maintaining the cytotoxicity of commercial DOX injection while reducing the toxicity against normal cells and increasing the survival time.
研究领域:
药剂学
·
肿瘤学
·
纳米医学
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DOI
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
·
2026
·
IF 5.9
Zishuo Hou,Tianyi Chen,Gangfeng Li,Ronghui Ma,Tengjiao Wang
Near-quantitative polymer functionalization enabled high NO-donor loading. • NO-releasing micelles were not cysteine-responsive, revealing new insights into NO release. • NO-releasing micelles accelerated burn wound healing and promoted vascular regeneration. Burn injuries are often accompanied by severe vascular damage, local tissue hypoxia, and subsequent scar formation. Although nitric oxide (NO) has been widely recognized for its ability to promote angiogenesis and tissue regeneration, achieving sustained NO delivery remains a major challenge. Herein, we developed a formylfuroxan-conjugated NO-releasing micelle (NORM) for burn wound repair. Compared with conventional small-molecule NO donors, the micellar architecture effectively mitigates burst NO release and enables prolonged, sustained NO delivery. In vitro studies demonstrated that NORM exhibits excellent hemocompatibility, minimal cytotoxicity, and a pronounced pro-angiogenic effect. Furthermore, therapeutic evaluation in a murine burn wound model revealed that NORM significantly accelerated wound closure. Collectively, these results demonstrate that sustained NO delivery through NORM effectively promotes vascularized tissue regeneration and highlight its potential as a promising therapeutic strategy for burn wound management. Download: Download high-res image (277KB) Download: Download full-size image
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DOI
高影响因子
JOURNAL OF DRUG TARGETING
·
2026
·
IF 4.7
Pingping Zhao,Wenhao Yuan,Yuhong Xu,Caifei Jin,Chu Chu,Yan Yang
The transdermal delivery of poorly water-soluble drugs is limited by low aqueous solubility and the stratum corneum permeability barrier. In this study, curcumin was formulated into self-assembled micelles using Tween 20 and polyethylene glycol 400, which exhibited a particle size of 12.5 nm, a zeta potential of −12.5 mV, and a 170-fold increase in solubility. The curcumin micelles (CM) were combined with constant-current iontophoresis (0.45 mA/cm2), to investigate the synergistic enhancement effects and underlying mechanisms. The results showed a 44.2-fold increase in cumulative release over 60 min, with a linear flux–current density relationship (R2 = 0.99). CM exhibited electro-responsive release with an approximate 20-min lag. Under a fixed 2 h total stimulation, pulsed current (4 pulses) nearly doubled the 8-h cumulative release compared to continuous current. Furthermore, both current density and electrode configuration were shown to influence penetration depth and width. Iontophoresis enabled CM to penetrate rat skin to a depth of 270 μm and increased intradermal retention by 258%. In a rat second-degree burn model, the combination therapy significantly accelerated wound healing via promoting angiogenesis, downregulating inflammatory cytokines, and enhancing collagen deposition.
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DOI
高影响因子
MICROCHEMICAL JOURNAL
·
2026
·
IF 5.2
Zhanghao You,Zhuang Zhang,Hao Zhang,Yuping Shan
Evaluating the impact of stiffness on the entry cell dynamic parameters of micelles at the single-particle level. • The dynamic parameters of TAT and fluorinated TAT interacting with cell membranes was analyzed at single-molecule level. • Visualizing the morphology and structure changes of cell membranes after interacting with TAT and fluorinated TAT. • The mechanical properties of cell membranes were evaluated after interacting with TAT and fluorinated TAT • The effects of FTAT and TAT on the endocytic pathway of micelles was studied. Taking the advantage of unique amphiphilic structure, nanoscale size, and tunable surface, micelles has been a key platform for targeted nano-drug delivery. To enhance the delivery efficiency, regulating the stiffness and modifying the micelles with ligand is necessary. In this study, the effect of stiffness on the dynamic parameters of micelles entry cell was evaluated at single-particle level, the probability for rigid micelles entry cell is higher, but they need larger force and longer duration. The modification of cationic cell-penetrating peptide TAT and its fluorinated derivative (FTAT) could promote the probability of cellular uptake. The promoting effect was further evaluated by measuring the kinetics of TAT and FTAT interacting with cell membrane at single-molecule level. The FTAT could rapidly bind with cell membrane with higher probability, however, it is also easier to detach from cell membrane. These findings can provide insights into optimizing the micelles for targeted nano-drug delivery. Download: Download high-res image (171KB) Download: Download full-size image
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DOI
高影响因子
PHOTOCHEMICAL & PHOTOBIOLOGICAL SCIENCES
·
2026
·
IF 3.5
Wu Xingjie,Zhu Guihua,Guo Qianqian,Chen Ying,Wang Yu-E,Yang Naijia,Mei Ju,Shen Xiangchun,Tao Ling
Lipopolysaccharide (LPS) contamination in biopharmaceuticals poses severe clinical risks, yet its detection and removal remain enduring challenges. Conventional detection methods are frequently hindered by low endotoxin recovery. Established clearance techniques often compromise the integrity of sensitive biologics or introduce secondary contaminants. To overcome these constraints, we developed an integrated platform for simultaneous LPS detection and removal. This system employs aptamer-conjugated micelles that encapsulate an aggregation-induced emission photosensitizer with high reactive oxygen species quantum yield. The surface aptamers facilitate specific LPS capture, followed by efficient light-triggered oxidative degradation. The capture-first design concentrates LPS near the photosensitizer-loaded core to maximize degradation efficiency. When validated in endotoxin-contaminated insulin solutions, the platform markedly reduced the ELISA-detectable LPS signal under the tested conditions, without measurably impairing insulin-induced glucose uptake in 3T3-L1 adipocytes in this preliminary assay. This biocompatible strategy bridges the gap between LPS monitoring and safe decontamination.
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产品关联
DOI
高影响因子
JOURNAL OF CONTROLLED RELEASE
·
2024
·
IF 10.5
Qiuyu Wei,Chenchen Zhu,Guiping Yuan,Jiahui Jin,Jing Zhang,Wufa Fan,Ying Piao,Shiqun Shao,Sen Lin,Jiajia Xiang,Youqing Shen
Efficient and noninvasive drug delivery for glaucoma therapy necessitates prolonged retention on the ocular surface and deep penetration into the cornea. However, inherent physiological defenses such as rapid tear clearance and low cornea permeability present significant challenges that hinder the effectiveness of trans-corneal drug delivery. In this study, we demonstrate the potential of zwitterionic micelles composed of poly(2-(N-oxide-N,N-diethylamino)ethyl methacrylate)- block -poly(ε-caprolactone) (OPDEA-PCL) amphiphiles as a biocompatible carrier for trans-corneal drug delivery. These micelles exhibit enhanced adhesion to ocular tissues and resistance to tear clearance due to their unique affinity for cell membranes. These characteristics facilitate adsorptive-mediated transcytosis, significantly augmenting trans-corneal transport and intraocular accumulation of the glaucoma medication brinzolamide (BRZ). As a result, OPDEA-PCL/BRZ formulations effectively normalize intraocular pressure in an open-angle glaucoma rat model, surpassing PEGylated and free BRZ formulations. This research underscores the potential utility of OPDEA-PCL micelles as a promising vehicle for noninvasive topical trans-corneal drug delivery in glaucoma therapy.
研究领域:
药剂学
·
眼科
·
药物递送系统
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
·
IF 8.5
Qiao Qiao,Jie Li,Chunying Tao,Meiyang Yang,Weijun Chen,Lipeng Qiu,Huiming Tu
Studies have shown that inflammation is closely linked to the cancer development, and the patients with inflammatory bowel disease (IBD) have a higher risk of colon cancer. Celecoxib (CXB) and camptothecin (CPT) showed potential treatment for IBD and colon cancers, respectively. However, their applications are limited by synchronous delivery, water insolubility, and off-target side effects. Herein, a glutathione (GSH) responsive chondroitin sulfate A (CSA)-SS-CXB micelle loaded with CPT (CSA-SS-CXB@CPT) was prepared as a targeted system to treat colon cancer by anti-inflammatory and antitumor synergistic effect. Specifically, CSA had tumor tumor-targeting effect due to colon cancer lesion-high expression of CD44 receptors. In vitro results verified that CSA-SS-CXB@CPT selectively internalized into colon cancer HT-29 cells and had strong reactive oxygen species (ROS) elimination ability. The CSA-SS-CXB@CPT could rapidly release CXB and CPT in the tumor microenvironment for playing an anti-tumor role. In vivo experiments illustrated that CSA-SS-CXB@CPT significantly targeted tumor tissues and suppressed tumor growth without producing serious side effects in tumor-bearing nude mice. Therefore, this work provides an opportunity for targeted co-delivery of anti-inflammatory and chemotherapy drugs to treat colon cancer.
研究领域:
药学
·
肿瘤学
·
生物医学工程
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产品关联
DOI
PubMed
高影响因子
Pharmaceuticals
·
2025
·Vol. 18
·期 4
·448
·
IF 4.8
Xueli Guo,Zhongyan Liu,Lina Wu,Pan Guo
Background : Liver cancer, especially hepatocellular carcinoma, a prevalent malignant tumor of the digestive system, poses significant therapeutic challenges. While traditional chemotherapy can inhibit tumor progression, its clinical application is limited by insufficient efficacy. Hydrophobic therapeutic agents further encounter challenges including low tumor specificity, poor bioavailability, and severe systemic toxicity. This study aimed to develop a liver-targeted, glutathione (GSH)-responsive micellar system to synergistically enhance drug delivery and antitumor efficacy. Methods : A GSH-responsive disulfide bond was chemically synthesized to conjugate glycyrrhetinic acid (GA) with curcumin (Cur) at a molar ratio of 1:1, forming a prodrug Cur-GA (CGA). This prodrug was co-assembled with glycyrrhizic acid (GL) at a 300% w / w loading ratio into micelles. The system was characterized for physicochemical properties, in vitro drug release in PBS (7.4) without GSH and in PBS (5.0) with 0, 5, or 10 mM GSH, cellular uptake in HepG2 cells, and in vivo efficacy in H22 hepatoma-bearing BALB/c mice. Results : The optimized micelles exhibited a hydrodynamic diameter of 157.67 ± 2.14 nm (PDI: 0.20 ± 0.02) and spherical morphology under TEM. The concentration of CUR in micelles can reach 1.04 mg/mL. In vitro release profiles confirmed GSH-dependent drug release, with 67.5% vs. <40% cumulative Cur release observed at 24 h with/without 10 mM GSH. Flow cytometry and high-content imaging revealed 1.8-fold higher cellular uptake of CGA-GL micelles compared to free drug ( p < 0.001). In vivo, CGA-GL micelles achieving 3.6-fold higher tumor accumulation than non-targeted controls ( p < 0.001), leading to 58.7% tumor volume reduction ( p < 0.001). Conclusions : The GA/GL-based micellar system synergistically enhanced efficacy through active targeting and stimuli-responsive release, providing a promising approach to overcome current limitations in hydrophobic drug delivery for hepatocellular carcinoma therapy.
研究领域:
药剂学
·
肿瘤学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
RSC Advances
·
2014
·Vol. 4
·期 90
·48943-48951
·
IF 3.708
Bing Liu,Hongying Chen,Xiao Li,Chaonan Zhao,Yakun Liu,Lijuan Zhu,Hongping Deng,Jichen Li,Guolin Li,Fulin Guo,Xinyuan Zhu
A new type of pH-responsive flower-like micelle based on backbone-cleavable triblock copolymer polycaprolactone-oxime-poly(ethylene glycol)-oxime-polycaprolactone (PCL-OPEG-PCL) was developed for anticancer drug delivery. Firstly, PCL-OPEG-PCL was synthesized by ring-opening polymerization. The structure of PCL-OPEG-PCL was confirmed by 1H NMR and Fourier transform infrared spectroscopy (FTIR). Benefiting from the amphiphilic character and unique molecular architecture with the hydrophilic PEG and hydrophobic PCL segments, PCL-OPEG-PCL could self-assemble into flower-like micelles in aqueous solution, which has been demonstrated by transmission electron microscopy (TEM) and dynamic light scattering (DLS). The cytotoxicity of the flower-like micelles was evaluated by MTT assay against NIH/3T3 normal cells. Doxorubicin (DOX), a model anticancer drug, was encapsulated into these flower-like micelles with high efficiency. The in vitro study showed that DOX-loaded flower-like micelles possessed high stability at physiological pH of 7.4, whereas the DOX release from the flower-like micelles was significantly accelerated at mildly acidic pH of 5.0, demonstrating the pH-responsive feature of the drug carrier with oxime linkages. DOX-loaded flower-like micelles were investigated for proliferation inhibition of Hela cells in vitro, and the DOX dose required for 50% cellular growth inhibition was found to be 1.81 μg mL−1. All of these results demonstrate that flower-like micelles self-assembled from PCL-OPEG-PCL triblock copolymers can be used as effective and promising drug nanocarriers.
研究领域:
生物材料学
·
药剂学
·
肿瘤学
✓ 已验证
DOI
高影响因子
Expert Opinion on Drug Delivery
·
2014
·
IF 4.116
Jinming Zhang,Yingbo Li,Wei Gao,Michael A Repka,Yitao Wang,Meiwan Chen
Background: Andrographolide (ADG) isolated from Andrographis paniculata exhibits anti-inflammatory and anticancer activities, but high hydrophobicity and poor bioavailability greatly restricts its clinical application.Objectives: In this study, ADG was encapsulated in a micelle formulation based on poly (D,L-lactide-co-glycolide)-b-poly (ethylene glycol)-b-poly (D,L-lactide-co-glycolide) (PLGA-PEG-PLGA) amphiphilic triblock copolymers, in order to enhance the anticancer efficacy and bioavailability in vivo.Methods: The physicochemical properties of the ADG-loaded PLGA-PEG-PLGA micelles were investigated for encapsulation efficiency, particle size, zeta potential and critical micelle concentration. These micelles were further evaluated for in vitro cytotoxicity, including proliferation inhibition, cell cycle arrest and pro-apoptosis effects against human breast cancer MAD-MB-231 cells, cellular uptake and pharmacokinetics study in rat.Results: ADG-loaded PLGA-PEG-PLGA micelles had a high encapsulation and loading efficiency of about 92 and 8.4% (w/w), respectively, and a stable particle size of 124.3 ± 6.4 nm. In vitro cytotoxicity testing demonstrated that ADG-loaded PLGA-PEG-PLGA micelles exhibited higher proliferation inhibition, cell cycle arrest at the G2/M phase and pro-apoptosis effects in MAD-MB-231 cells, which would be contributed to higher efficiency of cellular uptake and intracellular transport. Further, the plasma AUC(0 – ∞) and mean resident time of ADG-loaded PLGA-PEG-PLGA micelles were increased by 2.7- and 2.5-fold, respectively, when compared to the raw suspension.Conclusion: All of these investigations suggest that PLGA-PEG-PLGA micelles may be a potential drug delivery strategy for improving ADG bioavailability and efficacy in cancer therapy.
研究领域:
药剂学
·
肿瘤学
·
纳米医学
✓ 已验证
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）