Biomedicines
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2026
·Vol. 14
·期 9
·2015
·
IF 4.5
Junkai Zhao,Mengting Xie,Jianghao Yu,Ran Yan,Yue Wang
Background/Objectives: Thrombotic cardiovascular diseases remain a major cause of morbidity and mortality worldwide. Current antithrombotic therapies are limited by insufficient thrombus targeting. This study aimed to develop a fibrin-binding peptide-functionalized, hydrogen peroxide (H2O2)-responsive polymeric micelle and to evaluate its physicochemical properties and biological effects under H2O2-induced endothelial oxidative stress and preliminary FeCl3-induced thrombosis conditions.Methods: A fibrin-binding peptide, P2 (VTFIKC), was screened using computer-aided drug design and evaluated through microscale thermophoresis and in vitro thrombus adhesion assays. An all-trans retinoic acid (atRA)-based boronate ester prodrug, BORA, was synthesized to enable H2O2-triggered degradation and drug release. BORA was co-assembled with P2-modified Mal-PEG-b-PAsp to prepare P2-Mal-PEG-b-PAsp/BORA micelles. Their physicochemical properties, H2O2responsiveness, H2O2-scavenging activity, cytocompatibility, cytoprotective effects, anti-inflammatory activity, and preliminary in vivo efficacy were evaluated.Results: The resulting micelles exhibited a suitable nanoscale size, acceptable cytocompatibility, H2O2-responsive changes in particle size distribution, and concentration-dependent H2O2-scavenging activity. In H2O2-stimulated human umbilical vein endothelial cells, micelle treatment was associated with improved cell viability, lower intracellular ROS-associated fluorescence, and reduced TNF-α and IL-1β concentrations. In a FeCl3-induced rat carotid artery thrombosis model, P2-Mal-PEG-b-PAsp/BORA micelles altered platelet- and leukocyte-related hematological indices and exhibited preferential accumulation in the thrombotic carotid artery.Conclusions: P2-Mal-PEG-b-PAsp/BORA micelles combine P2-mediated fibrin-binding potential, H2O2-responsive release behavior, and H2O2-scavenging activity. The findings provide preliminary support for further investigation of this peptide-functionalized nanoplatform.
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CARBOHYDRATE POLYMERS
·
2026
·
IF 13.2
Yangyi Chen,Yue Wei,Qiao Li,Huajuan He,Hui Chen,Huajing Zhang,Xiaoqing Rong,Xiao Liang,Shiyuan Lin,Wei Zhang
A kind of novel pyrimidine nucleoside (PYN) and silybin (SB) conjugated chitosan (CS) (PYN-CS-SB) polymer micelles were designed for enhancing the oral absorption of doxorubicin (DOX) via the nucleoside transporters located at intestinal epithelial cell. The four types of endogenous PYNs selected respectively as the ligands of the transporter, along with SB, were conjugated to CS. The PYN-CS-SB were synthesized and identified by 1 H NMR and FT-IR. The drug-loaded micelles were prepared by ultrasound-assisted self-assembly, and their predominant characteristics, including the microscopic well-dispersed and regular globular shapes with the small particle sizes of 143 nm - 170 nm and the high loading capacities of 9–12%, the amorphous form of DOX encapsulated in micelles, the low critical micelle concentration of 23.1–31.6 μg/ml, and extremely sustained in-vitro release, were shown. Among them, the desoxycytidine (DCD) conjugated micelles (DCD-CS-SB@DOX) exhibited the highest oral bioavailability of 391% versus DOX·HCl. The enhanced absorption based on the nucleoside transporter-mediation, and the dual inhibition of PYN-CS-SB micelles on P-gp efflux and CYP3A4 enzyme, was confirmed by cellular uptake, immunofluorescence, enzyme activity inhibition test. The findings showed the extensive potential of intestinal nucleoside transporter mediated PYN-CS-SB micelles in oral drug delivery.
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INTERNATIONAL IMMUNOPHARMACOLOGY
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2026
·
IF 5.6
Bang-Yun Liu,Ya-Ni Zhang,Ge Zhang,Zi-Yan Hua,Yi-Fei Gao,Yu-Xin Niu,Yang-yang Deng,Ying-Qiang Lu,Xue-Tao Li,Yang Liu
Idiopathic pulmonary fibrosis (IPF) is a life-threatening respiratory disease characterized by excessive proliferation of myofibroblasts and abnormal accumulation of extracellular matrix. At present, the treatment is limited. M2 macrophages play a key role in the pathogenesis of IPF. M2 macrophages are the main source of pro-fibrotic cytokine TGF-β1, which drives the progression of IPF by inducing epithelial-mesenchymal transition (EMT) and fibroblast-to-myofibroblast transition (FMT), and highly express mannose (Man) specific surface receptors. This feature provides an important target basis for us to design targeted drug delivery systems. Emodin (Emo) is a potential anti-fibrosis drug, but its poor water solubility and low bioavailability are limited in clinical practice. Therefore, we constructed a self-assembling M2-targeting micellar (Man-Sa-Pnp-Emo@Ms) to target M2-type macrophages and inhibit the secretion of TGF-β1, blocking the core pathological process of pulmonary fibrosis. Cellular uptake, cytotoxicity, and anti-fibrotic effects (inhibition of fibroblast proliferation, invasion, and metastasis) were evaluated in vitro , and their targeting and anti-fibrotic effects were verified by in vivo imaging and histological staining (HE, Masson, immunofluorescence). The results showed that Man-Sa-Pnp-Emo@Ms had a homogeneous spherical structure, which improved the solubility of Emo and reduced the release of M2-type macrophage-derived TGF-β1. It inhibited FMT transformation and extracellular matrix accumulation (ECM) and exerted anti-fibrotic effects without damaging tissue-resident macrophages in vitro and in a bleomycin-induced mouse model. This work provides a novel nanodelivery strategy for the precision treatment of idiopathic pulmonary fibrosis.
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Frontiers in Pharmacology
·
2025
·
IF 4.8
Tangna Hao,Xiaokui Huo,Zhen Li,Changyuan Wang,Sha Wu,Anni Song,Fengyu Zhang,Kexin Liu
Introduction: Cisplatin (DDP), a platinum-based chemotherapy drug, shows broad antineoplastic activity, however, its clinical use is limited by dose-dependent nephrotoxicity, a major challenge in cancer therapy. The purpose of this study was to investigate the mechanism by which quercetin-polyethylene glycol-polycaprolactone (Que-PEG-PCL) micelles simultaneously enhance the cytotoxicity of DDP against cancer cells and reduce its nephrotoxicity.Methods: Rodent models and HEK293 cells were used to evaluate the renoprotective effects of Que-PEG-PCL micelles. Pharmacokinetics focused on OCT2-mediated renal DDP disposition. Antitumor activity was assessed in CT26 cells and syngeneic tumors. Key assessments included oxidative stress, apoptosis, renal markers, and histopathology.Results:: Que-PEG-PCL reduced DDP-induced nephrotoxicity, lowering creatinine and BUN to 42% and 38%. It also reduced oxidative stress and improved antioxidant activity. DDP plasma exposure increased to 323%, with renal clearance reduced to 14%, due to OCT2 inhibition. In a CT26 syngeneic model, combination therapy inhibited tumor volume by 84% compared to control group.Discussion: Que-PEG-PCL enhanced DDP’s therapeutic window by limiting renal accumulation and promoting tumor cell apoptosis. This dual-action strategy provides a novel approach for improving the clinical efficacy of DDP-based cancer therapy.
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JOURNAL OF THE INDIAN CHEMICAL SOCIETY
·
2026
·Vol. 103
·期 3
·102477
·
IF 3.4
Saima Ameen Ghoto,Muhammad Yar Khuhawar,Taj Muhammad Jahangir Khuhawar,Muhammad Farooque Lanjwani
A rapid, highly sensitive colorimetric nanosensor based on citrate-capped gold nanoparticles (Cit-AuNPs) is presented for screening total biogenic amines (TBAs) as a practical indicator of food quality and safety. Individual BAs like putrescine (PUT), histamine (HTM), spermine (SPM), and spermidine (SPD) were first investigated in aqueous and micellar media to elucidate the sensing mechanism, evaluate sensitivity, optimization of parameters and confirm uniform optical responses. Electrostatic and hydrogen-bonding interactions between the amines and Cit-AuNPs induce nanoparticle aggregation, triggering a distinct color change from burgundy red to dark grey accompanied by a surface plasmon resonance shift from 520 to 700 nm. The nanosensor was comprehensively characterized by UV–Vis spectroscopy, FTIR, SEM-EDX, dynamic light scattering, and zeta potential, validating surface chemistry, size, morphology, and colloidal stability. Detection limits of 0.842–2.018 μg/mL in aqueous medium were enhanced nearly tenfold (0.008–0.067 μg/mL) in a micellar environment. The method was applied to Labeo rohita fish muscle, TBAs (as HTM equivalents) ranging from 141.99 to 654.33 mg/kg, with excellent precision (RSD <0.1%) were calculated. Further the method's practical applicability was confirmed using HTM spiked samples, which demonstrated high accuracy and precision with recoveries of 96.26–101.65%, low standard deviations (0.002–0.006 mg/kg), and %RSD below 0.4%, highlighting the sensor as a fast, reliable, and cost-effective tool for food freshness and safety screening .
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JOURNAL OF COLLOID AND INTERFACE SCIENCE
·
2016
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IF 3.782
Hui Zhang,Jiangkang Xu,Liang Xing,Jianbo Ji,Aihua Yu,Guangxi Zhai
Doxorubicin (DOX) is one of the most common chemotherapeutic agents for the treatment of various cancers, but its clinical usage is limited by dose-dependent cardiotoxicity. We have recently synthesized a series of Chondroitin sulfate/poly ( d , l -lactideco-glycolide) block copolymers (Chs- b -PLGA) with different length of hydrophobic block by an end-to-end coupling strategy. The structure of the amphiphilic block copolymers with low critical micelle concentration (∼28 mg/L) were confirmed by 1 H NMR. The copolymers could self-assemble into stable micelles in aqueous environment with homogeneous size distribution and negative zeta potential . The hemolytic study indicated their excellent blood compatibility and potential application for intravenous administration. DOX can be efficiently encapsulated by the Chs- b -PLGA micelles. The DOX-loaded micelles showed a sustained and pH dependent drug release behavior. The cytotoxicity assay showed no associated toxicity with blank micelles while concentration-related cell inhibition with DOX-loaded micelles. Moreover, fast cellular uptake of DOX-loaded micelles was observed by fluorescent microscope. In vivo pharmacokinetics study showed that the Chs- b -PLGA micelles could significantly prolong the blood circulation time of DOX. The maximum tolerated dose (MTD) of DOX-loaded micelles in Kunming mice was about 2-fold higher of the MTD of free DOX, indicating a high tolerance of the DOX-loaded micelles. In conclusion, the Chs- b -PLGA micelles would be a potentially useful drug delivery system for cancer therapy.
研究领域:
药剂学
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药物递送
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纳米医学
·
高分子科学
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癌症治疗
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生物医学工程
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PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
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2022
·
IF 3.915
Xiaoli Xia,Jian Zhang,Michael Adu‑Frimpong,Xiaoxiao Li,Xinyi Shen,Qing He,Wanjing Rong,Hao Ji,Elmurat Toreniyazov,Ximing Xu,Jiangnan Yu,Qilong Wang
Hyperoside (Hyp) self-assembled polymeric micelles (Hyp-PMs) were purposely developed to enhance aqueous solubility, in vivo availability and anti-oxidative effect of Hyp. In preparing Hyp-PMs, we employed the thin film dispersion method with the micelles consisting of TPGs and mPEG2000-PDLLA3000. The particle size, polydispersity index and zeta potential of Hyp-PMs were 67.42 ± 1.44 nm, 0.229 ± 0.015 and −18.67 ± 0.576 mV, respectively, coupled with high encapsulation efficiency （EE）of 90.63 ± 1.45% and drug loading (DL) of 6.97 ± 1.56%. Furthermore, the value of critical micelle concentration (CMC) was quite low, which indicated good stability and improved self-assembly ability of Hyp-PMs. Also, trend of in vitro Hyp release from Hyp-PMs demonstrated enhanced solubility of Hyp. Similarly, in comparison with free Hyp, oral bioavailability of Hyp-PMs was improved (about 8 folds) whilst half-life of Hyp-PMs was extended (about 3 folds). In vitro anti-oxidative effect showed obvious strong scavenging DPPH capability of Hyp-PMs, which may be attributed to its smaller size and better solubility. Altogether, Hyp-PMs may serve as a possible strategy to potentially enhance aqueous solubility, bioavailability and anti-oxidative effect of Hyp, which may play a key role in Hyp application in the pharmaceutical industries.
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EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
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2022
·
IF 5.589
Qiangwei Liang,Yang Lan,Yifan Li,Yongjin Cao,Juan Li,Yanhua Liu
Chemotherapeutic agents can trigger the immune response via inducing immunogenic cell death (ICD), but the weak ICD effect induced by chemotherapy alone limits its lasting antitumor immunotherapy effect. A Cro polymerized prodrug carriers (POEG- b -PCro) with immunostimulatory by ICD induction was developed and co-delivered DOX to generate synergistic ICD induction for chemo-immunotherapy on breast cancer. DOX/POEG- b -PCro micelles displayed prolonged circulation in blood, efficient accumulation in tumors, internalization and then co-released DOX&Cro in tumor cells. Moreover, the DOX/POEG- b -PCro micelles synergistically triggered ICD induction by releasing the nuclear high mobility group box 1 (HMGB1) and down-regulation of c-Met level for generating chemo-immune anti-tumor actions. Importantly, the DOX/POEG- b -PCro micelles synergistically enhanced the tumor cytotoxic T lymphocytes infiltration , concomitant decreasing the immunosuppressive regulatory T (Treg) cells, accompanied with the increased cytokines secretion of IFN-γ and TNF-α, consequently displaying an improved anti-tumor activity in 4 T1 breast cancer mice. Overall, POEG- b -PCro prodrug micelles co-delivered DOX could be served as a promising nano drug delivery system for synergistic ICD induction on breast cancer chemo-immunotherapy.
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NEW JOURNAL OF CHEMISTRY
·
2022
·Vol. 46
·期 44
·21235-21244
·
IF 3.925
Huan Xu,Mingyue Yang,Yijing Du,Tian Gao,Yi Liu,Liwei Xiong,Na Peng
Nano-drug carriers have been widely used in chemotherapy to improve the efficacy of chemotherapeutic drugs. Polymer nano-carriers have greater potential for the enrichment of chemotherapeutic drugs at the target tumor site and controlled release. Herein, a series of amphiphilic copolymers (ITT) was synthesized via melt polymerization with a ROS-cleavable thioketal cross-linker, imidazole groups, and polyethylene glycol-conjugated triphenylphosphonium (PEG-TPP) segments; the actual proportions of the imidazole groups to the PEG-TPP segments were 5.2 : 1, 2.6 : 1, and 1.8 : 1, respectively. The amphiphilic copolymers could self-assemble into cationic micelles with hydrophobic imidazole groups as the core and hydrophilic PEG-TPP segments as the shell in deionized water. The cationic micelles with an average particle size of 124.6–187.3 nm showed a drug loading content (DLC) of 5.65–6.10%. In vitro release studies revealed the pH/ROS dual-responsiveness of the DOX-loaded ITT micelles, and the release behavior of DOX from the micelles strongly depended on the content of imidazole groups in the ITT micelles. Typically, the release of the encapsulated DOX was 27.2%, 30.0%, and 34.1% from DOX-loaded ITT-1 micelles in PBS (pH 6.5) containing 0, 100, and 500 μM H2O2, respectively. The release of the encapsulated DOX was 20.3%, 27.2%, and 42.5% from DOX-loaded ITT-1 micelles in PBS (pH 7.4), PBS (pH 6.5), and PBS (pH 5.0), respectively. The DOX-loaded micelles effectively inhibited the growth of 4T1 cells through being internalized into the 4T1 cells and releasing DOX into the mitochondria, with a cell viability of less than 65% when the DOX concentration was 2.5 μg mL−1. This work presents a novel mitochondria-targeting and pH/ROS-responsive polymer nanocarrier for potential chemotherapy applications.
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ENVIRONMENTAL SCIENCE AND POLLUTION RESEARCH
·
2021
·Vol. 28
·期 31
·42694-42705
·
IF 4.223
Wu Peng,Liu Yiqing,Fu Yongsheng,Zhou Gaofeng,Deng Jiewen
The solubilization laws of pollutants in micelles and their separation efficiency are very important in the successfully efficient application of micellar enhanced ultrafiltration (MEUF). The solubilization behavior of o -toluidine (OT) and tricyclazole (TC) into sodium dodecyl sulfate (SDS) micelles in MEUF was studied using nonlinear equation sets for concentration analysis, which resolved the issue on the overlap of absorption spectra of multicomponent compounds restricting the application of conventional ultraviolet (UV) spectroscopic method. The solubilization isotherms for both pollutants could be best explained by the Langmuir-Freudlich model ( R 2 >0.99) followed by the modes of Langmuir and Freudlich, inferring the complexity of solubilization mechanism and solubilization advantage of monolayer over multilayer. The calculated thermodynamic parameters ( ΔG 0 , ΔH 0 and ΔS 0 ) indicated that this process was endothermic and spontaneous. The solubilization of OT and TC well followed the pseudo second-order and pseudo first-order kinetics, respectively. The separation and recovery of SDS solubilizing these two pollutants were also investigated through lowering solution temperature to 2 °C followed by centrifugation. The best recovery rate of about 66% for SDS was achieved containing 10 and 5% of each initial amount of OT and TC, respectively, at near-neutral solution pH value. The recovery of SDS could decrease to some extent under alkaline and acidic conditions.
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COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
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2021
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IF 4.539
Mengna Zhang,Shujing Zhang,Kun Zhang,Zongyuan Zhu,Yalei Miao,Yudian Qiu,Panke Zhang,Xubo Zhao
Functionality of polymers is crucially fundamental to polymers. However, the application of polymers faces great challenges due to the insufficient function of hydrophobic chain, especially in drug delivery. One novel approach to solve this dilemma involves the use of medicated hydrophobic chains. Herein, the polymer-doxorubicin conjugates are synthesized from hydrophilic copolymer and hydrophobic chain composed of doxorubicin (DOX). DOX, a common hydrophobic anticancer drug , is used to serve as a hydrophobic pendant for inducing self-assembly of polymer-doxorubicin conjugates. The self-assembly of polymer-drug conjugates is employed to encapsulate the unreacted drug for the first time and form drug-loaded polyprodrug micelles that possess a low critical micelle concentration (CMC), which improves the use efficiency of expensive drug. The detachment of DOX moieties from polymer-doxorubicin conjugates caused by amidase facilitates the disintegration of DOX-loaded polyprodrug micelles to trigger the enhanced release of DOX in a slightly acidic medium. It is demonstrated that the DOX-loaded polyprodrug micelles have a higher suppression against cancer cells in in vitro investigations. This work thus proposes a strategy to modify the poor functionality of polymer-based nanostructures , through designing the medicated hydrophobic chains. This strategy facilitates the potential application of polymer-drug conjugates and provides profound insights into the effect of medicated polymer on drug delivery system.
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Drug Delivery and Translational Research
·
2021
·Vol. 12
·期 5
·1080-1095
·
IF 4.617
Su Meiling,Hu Heping,Zhao Xuan,Huang Chengyuan,Yang Bowen,Yin Zongning
This study evaluated the D-mannose modified polyethyleneimine-block-polycaprolactone biomacromolecule copolymer micelles (PCL-PEI-mannose) as a targeted delivery of the glucocorticoid dexamethasone (DXM) to lung inflammation tissues and enhances the vehicle for its anti-inflammatory effects. Dexamethasone was encapsulated in the hydrophobic core of cationic polymer micelles by solvent evaporation. The polymeric micelles exhibited sustained-release within 48 h, good blood compatibility, and colloidal stability in vitro. The cellular uptake of mannose-modified micelles was higher compared with the non-modified micelles. And drug-loaded targeted micelles could inhibit the production of inflammatory factors in activated RAW264.7 cells. The distribution results indicated that drug-loaded targeted micelles highly improved the lung targeting ability, reduced the wet/dry ratio of injured lung tissue, and relieved the lung inflammation, accompanied by the decrease of inflammatory cell infiltration, myeloperoxidase activity, and inflammatory mediator levels in bronchoalveolar lavage fluid. These findings suggested that PCL-PEI-mannose delivery system could facilitate the lung-specific delivery and inhibit the inflammatory response. Collectively, PCL-PEI-mannose polymer micelles could be used as a potential delivery system for the treatment of acute lung injury (ALI). Graphical abstract
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