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Frontiers in Microbiology · 2025 · IF 4.5

Synthetic niclosamide-loaded controlled-release nanospheres with high solubility and stability exerting multiple effects against Clostridioides difficile

Yulei Tai,Meng Zhang,Yuning Han,Hui Hu,Shan Lin,Fangya Zhai,Menglun Tian,Xiaojun Song,Shuangshuang Wan,Yu Chen,Dazhi Jin

Introduction: Niclosamide (NIC) has significant potential as a clinical therapeutic agent for Clostridioides difficile infection (CDI); however, its strong hydrophobicity hampers its oral bioavailability, and its active effects against C. difficile remain unclear.Methods: Niclosamide-loaded controlled-release hyaluronic acid-modified poly (lactic-co-glycolic acid) naosphernes (NIC@PLGA-HAs) were synthesized using an oil-in-water emulsion technique and their effects on C. difficile cell growth, spore germination, biofilm formation, and NIC interaction sites with C. difficile toxin B (TcdB) were analyzed.Results: NIC@PLGA-HAs exhibited enhanced solubility and stability, with a water contact angle on a hydrophilic surface of 65.1° and a zeta potential of 31.57 ± 2.08 mV, and pH-responsive (pH 7.4) controlled-release characteristics compared to free NIC. The NIC@PLGA-HAs killed C. difficile vegetative cells at a minimum inhibitory concentration (MIC) of 4 μg/mL. When C. difficile cells were treated with NIC@PLGA-HAs at the 1/4 MIC, spore germination and biofilm formation were significantly inhibited compared to those in untreated cells (P < 0.01). NIC was found to interact with the receptor-binding domain of TcdB at 24 amino acid sites via an enthalpy-driven reaction (enthalpy change, 36.21 kJ/mol and entropy change, 212.9 J⋅mol/K). In vivo experimental findings in Mongolian gerbils indicated that NIC@PLGA-HAs outperformed free NIC in reducing pathological damage, diarrhea severity, weight loss, and TcdB production and enhanced the survival rate.Conclusion: These findings presented the therapeutic potential of NIC@PLGA-HAs with high solubility and stability, which simultaneously exerted multiple biological activities against C. difficile.

CAS / MDL: 26780-50-7
研究领域: 药剂学 · 微生物学 · 纳米技术 · 药物递送 · 传染病学
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ACS Applied Materials & Interfaces · 2026 · IF 7.8

Controllable Silicone Rubber Curing via Controlled Release of Homogeneous Pt from a Metal–Organic Framework-Based Capsule

Ya-Qi Xue,Lei Wang,Yin Wang,Xiao Liu,Bin Lei,Xi-Ze Liu,Bo Li,Qian Yang,Jin Chang,Wei-Wei Ding,Jian-Gong Ma,Peng Cheng

Platinum-based hydrosilylation catalysts are primarily applied in the curing of silicone rubber. However, the commercial Karstedt catalysts used in industrial applications seriously suffer from rapid oxidation in air, uncontrolled activity at room temperature, rigorous storage conditions yet short pot-life, poor thermal stability, and complicated operation packages. Herein, Pt@MOFs, constructed by immobilizing catalytically active sites Pt inside the pores of a metastable MOF-based host with selected decomposition temperature, acts as a “controlled-release MOF-based capsule” to keep a long pot-life during storage and transport at ambient conditions, control the curing temperature of hydrosilylation, and releases the catalytically active Pt sites at required temperature for in situ polymer formation. Additionally, the unique nanosized crystalline MOF carriers are dominant for uniform dispersion in polysiloxanes and guarantee the excellent oxidation resistance in the Pt@MOFs catalytic system, which provides a new generation catalyst for widely used silicone rubber packages and an innovative pathway for the application of metastable MOF materials. Honeywell® has initiated kilogram-scale silicon rubber packages with Pt@MOFs.

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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2026 · IF 8.7

Dual pH/temperature-responsive cellulose nanocrystals with tailored dual-triggered structural adaptability for controlled-release oral tablet

Yi Chen,Bowen Jia,Junjie Zhou,Guojun Jin,Hou-Yong Yu

Designing oral solid preparations with responsive release mechanisms is crucial for achieving precise therapeutic efficacy in gastrointestinal diseases. In this work, a dual pH/temperature-responsive cellulose nanocrystal (CNCs-D-N) was engineered by grafting a stimuli-sensitive copolymer onto carboxylated cellulose nanocrystal, thereby endowing tailored dual-triggered structural adaptability. The CNCs-D-N exhibited pH-dependent protonation–deprotonation equilibria and thermally induced chain conformational transitions, which cooperatively regulated molecular extension and contraction, enabling rapid and controllable drug release. Tetracycline hydrochloride was subsequently wet-loaded into CNCs-D-N to fabricate stimuli-sensitive tablets (CNC@DNWT), which showed excellent mechanical robustness (hardness: 32.64 N; brittleness: 0.31%), high drug loading capacity (99%), and ultrafast release initiation (7 s). Importantly, CNC@DNWT achieved a cumulative release of 99% under simulated gastric conditions (pH = 3, 37 °C), underscoring synergistic role of dual stimuli in tuning release kinetics. By bridging molecular-level adaptability with macroscopic delivery performance, this study provides a mechanistic strategy for the development of intelligent cellulose-based oral formulations with promising potential for targeted gastric cancer therapy.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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LANGMUIR · 2021 · IF 3.882

Synthesis of Photo, Oxidative, and Reductive Triple-Stimuli-Responsive Block Copolymer Micelles as Nanocarriers for Controlled Release

Qiong Guo,Jiangtao Liu,Hong Yang,Zhongli Lei

With the rapid development of nanotechnology, stimuli-responsive nanomaterials have provided an alternative for designing controllable drug delivery systems due to their spatiotemporally controllable properties. The environment of the human body is complex and cancer cells proliferate rapidly; the traditional nanocarriers could not release the loaded drugs sufficiently, and the release level of the drug is not sufficient for the requirement of treatment. Herein, a photoresponsive, glutathione, and reactive oxygen species block copolymer mPEG2k-ONB-SS-PO-mPEG2k is prepared by Cu(I)-catalyzed azide–alkyne cycloaddition click polymerization. The ο-nitrobenzyl groups, peroxalate ester bonds, disulfide bonds, and triazole units are regularly and repeatedly arranged in hydrophobic blocks. The photo, oxidative, and reductive responsive characteristics of the copolymers in different conditions were investigated by ultraviolet and visible spectrophotometry, dynamic light scattering, and transmission electron microscopy. Nile Red is encapsulated into the core of micelles as a model drug and exhibits the drug release behaviors in various environments. This research provides a way to design potential drug carriers and a promising platform for efficient intracellular drug delivery in cancer therapy.

研究领域: 材料科学 · 生物医学工程 · 药学
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CHEMICAL ENGINEERING JOURNAL · 2024 · IF 13.3

Tough and anisotropic Janus hydrogel for tendon injury repair with controlled release of bFGF in tendon microenvironment

Yingxue Jiang,Chenhui Zhu,Xiaoxuan Ma,Daidi Fan

To address the high complexity and challenging nature of large-scale tendon injury repair, an innovative Janus structured hydrogel patch (JAHP@bFGF) was designed in this study. The patch combines microenvironmental responsiveness with efficient repair function, aiming to optimise and accelerate the tendon healing process. The outer layer is a PVA/SA/Na 3 Cit hydrogel with excellent mechanical properties, protein resistance, and low friction, which provides firm support to the tendon and reduces adhesions to ensure the recovery of gliding function. The inner layer of TCSB@bFGF microgel responds intelligently to changes in the microenvironment, precisely regulates the release of bFGF, promotes cell proliferation and migration, accelerates tissue regeneration, and has high adhesion strength and antimicrobial properties, which significantly reduces the risk of postoperative infection. Experimental results show that JAHP@bFGF significantly optimises the healing process, accelerates the repair speed and improves the repair quality under simulated large-scale tendon injury conditions. The unique Janus surface design and the intelligent drug release function, in synergy, not only bring new hope to patients with large-scale tendon injuries, but also provide an important reference for the application of biomedical materials in the repair of complex tissues, which heralds the arrival of the era of more efficient and personalised tendon repair.

研究领域: 生物医学工程 · 组织工程 · 材料科学 · 再生医学
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Journal of Materials Chemistry B · 2013 ·Vol. 1 ·期 26 ·3304-3313 · IF 0

Controlled release of gentamicin from gelatin/genipin reinforced beta-tricalcium phosphate scaffold for the treatment of osteomyelitis

Tianyi Wu,Qingchun Zhang,Weiping Ren,Xiang Yi,Zubin Zhou,Xiaochun Peng,Xiaowei Yu,Meidong Lang

Infection of the bone (osteomyelitis) remains one of the most challenging problems in the field of orthopedic surgery. The limitations of systemic antibiotics administration include undesired side effects, systemic toxicity, patient discomfort, and development of bacterial resistance. In this study, we developed a bactericidal gentamicin-doped beta-tricalcium phosphate (TCP) scaffold reinforced with a gelatin/genipin hydrogel (G-TCP). Our data showed that the gentamicin-doped G-TCP had a much longer drug releasing period, while the gentamicin was completely released from pure TCP cements (B-TCP) within one day. In addition, the release profile of G-TCP exhibited an initial burst followed by a zero-order release. One standard strain, Staphylococcus aureus (S. aureus, ATCC25923) was selected to evaluate the antibacterial activity and therapeutic effect of this scaffold. G-TCP significantly inhibited growth of S. aureus both in vitro and in vivo. In a rat osteomyelitis model, osteomyelitis could be totally cured after implantation of G-TCP for three weeks. We propose that the gelatin/genipin–gentamicin TCP scaffold represents one of the promising gentamicin releasing bone scaffolds in treating osteomyelitis.

研究领域: 骨科手术 · 药剂学 · 生物材料
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JOURNAL OF COLLOID AND INTERFACE SCIENCE · 2023 · IF 9.9

Silk fibroin-based coating with pH-dependent controlled release of Cu2+ for removal of implant bacterial infections

Tongyao Lin,Jinglin Zhang,Dongliang Huo,Fengjuan Yang,Jingxian Zhang,Langhuan Huang,Sui-Ping Deng,Shaozao Tan,Huifang Chen

The implantation of medical devices is frequently accompanied by the invasion of bacteria, which may lead to implant failure. Therefore, an intelligent and responsive coating seems particularly essential in hindering implant-associated infections. Herein, a self-defensive antimicrobial coating, accompanied by silk fibroin as a valve, was successfully prepared on the titanium ( [email protected] ) for pH-controlled release of Cu 2+ . The results showed that the layer could set free massive Cu 2+ to strive against E. coli and S. aureus for self-defense when exposed to a slightly acidic condition. By contrary, a little Cu 2+ was released in the physiological situation, which could avoid damage to the normal cells and showed excellent in vitro pH-dependent antibiosis. Besides, in vivo experiment confirmed that [email protected] could work as an antibacterial material to kill S. aureus keenly and display negligible toxicity in vivo . Consequently, the design provided support for endowing the layer with outstanding biocompatibility and addressing the issue of bacterial infection during the implantation of Ti substrates.

研究领域: 材料科学 · 生物医学工程 · 生物材料
✓ 已验证 DOI PubMed 高影响因子
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NANOTECHNOLOGY · 2017 ·Vol. 28 ·期 37 ·375101 · IF 3.44

Multifunctional halloysite nanotubes for targeted delivery and controlled release of doxorubicin in-vitro and in-vivo studies

Yuwei Hu,Jian Chen,Xiufang Li,Yanhua Sun,Shen Huang,Yuqing Li,Hui Liu,Jiangfeng Xu,Shian Zhong

The current state of cancer therapy encourages researchers to develop novel efficient nanocarriers. Halloysite nanotubes (HNTs) are good nanocarrier candidates due to their unique nanoscale (40–80 nm in diamter and 200–500 nm in length) and hollow lumen, as well as good biocompatibility and low cost. In our study, we prepared a type of folate-mediated targeting and redox-triggered anticancer drug delivery system, so that Doxorubicin (DOX) can be specifically transported to tumor sites due to the over-expressed folate-receptors on the surface of cancer cells. Furthermore, it can then be released by the reductive agent glutathione (GSH) in cancer cells where the content of GSH is nearly 103-fold higher than in the extracellular matrix. A series of methods have demonstrated that per-thiol-β-cyclodextrin (β-CD-(SH)7) was successfully combined with HNTs via a redox-responsive disulfide bond, and folic acid-polyethylene glycol-adamantane (FA-PEG-Ad) was immobilized on the HNTs through the strong complexation between β-CD/Ad. In vitro studies indicated that the release rate of DOX raised sharply in dithiothreitol (DTT) reducing environment and the amount of released DOX reached 70% in 10 mM DTT within the first 10 h, while only 40% of DOX was released in phosphate buffer solution (PBS) even after 79 h. Furthermore, the targeted HNTs could be specifically endocytosed by over-expressed folate-receptor cancer cells and significantly accelerate the apoptosis of cancer cells compared to non-targeted HNTs. In vivo studies further verified that the targeted HNTs had the best therapeutic efficacy and no obvious side effects for tumor-bearing nude mice, while free DOX showed damaging effects on normal tissues. In summary, this novel nanocarrier system shows excellent potential for targeted delivery and controlled release of anticancer drugs and provides a potential platform for tumor therapy.

研究领域: 纳米技术 · 药学 · 癌症研究 · 生物医学工程
✓ 已验证 DOI PubMed 高影响因子
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CHEMICAL ENGINEERING JOURNAL · 2023 · IF 15.1

Smart controlled-release avermectin nanopesticides based on metal–organic frameworks with large pores for enhanced insecticidal efficacy

Jincan Liu,Dejin Xu,Guangchun Xu,Xiaona Li,Jiangtao Dong,Xingkun Luan,Xuezhong Du

Nanopestcides based on metal–organic frameworks (MOFs) have attracted great attention. Highly stable mesoporous metal–organic framework PCN-777 with large pores can accommodate the biologically active insecticide avermectin (AVM) of relatively large molecular dimensions. In this work, PCN-777 nanoparticles were synthesized for the creation of double-gated nanopesticides with sodium lignosulfonate (SL) and chitosan. The double gatekeepers could realize excellent sealing performance to prevent premature leakage of AVM. The double-gated PCN-777 based nanopesticides could achieve the controlled release of AVM in response to pH, laccase, phosphate, and phytic acid (PA), which are related to the physiological environments of pests and crops. The PA-triggered controlled release of loaded cargos in MOF-based delivery systems was reported for the first time. This is the first example of PCN-777 drug/pesticide delivery system and also the first case of controlled-release MOF-based AVM nanopesticides, and the mechanisms of the stimuli-responsive controlled pesticide release were clearly elucidated. The nanopesticides prevented the ultraviolet photolysis of AVM owing to the PCN-777 organic ligands and SL coating. The nanopesticides had high insecticidal efficacy and field control efficacy against the pests Spodoptera litura Fabricius on cabbage, in comparison with traditional pesticide formulations, and the nanopesticides had no influence on plant growth and showed high biosafety toward non-target organisms and human cells. The smart controlled-release nanopesticides show high potential and application prospect in ecological agriculture.

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Materials Science & Engineering C-Materials for Biological Applications · 2017 · IF 4.164

Multimodal nanoporous silica nanoparticles functionalized with aminopropyl groups for improving loading and controlled release of doxorubicin hydrochloride

Xin Wang,Chang Li,Na Fan,Jing Li,Zhonggui He,Jin Sun

The purpose of this study was to develop amino modified multimodal nanoporous silica nanoparticles (M-NSNs-NH 2 ) loaded with doxorubicin hydrochloride (DOX), intended to enhance the drug loading capacity and to achieve controlled release effect. M-NSNs were functionalized with aminopropyl groups through post-synthesis. The contribution of large pore sizes and surface chemical groups on DOX loading and release were systemically studied using transmission electron microscope (TEM), nitrogen adsorption/desorption measurement, Fourier transform infrared spectroscopy (FTIR), zeta potential analysis, X-ray photoelectron spectroscopy (XPS) and ultraviolet spectrophotometer (UV). The results demonstrated that the NSNs were functionalized with aminopropyl successfully and the DOX molecules were adsorbed inside the nanopores by the hydrogen bonding. The release performance indicated that DOX loaded M-NSNs significantly controlled DOX release, furthermore DOX loaded M-NSNs-NH 2 performed slower controlled release, which was mainly attributed to its stronger hydrogen bonding forces. As expected, we developed a novel carrier with high drug loading capacity and controlled release for DOX.

CAS / MDL: 919-30-2 78-10-4
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ACS Agricultural Science & Technology · 2023 · IF 2.5

Multifunctional γ-Cyclodextrin-Based Metal–Organic Frameworks as Avermectins Carriers for Controlled Release and Enhanced Acaricidal Activity

Huiping Chen,Yongpan Shan,Chunli Xu,Muhammad Bilal,Pengyue Zhao,Chong Cao,Hongjun Zhang,Qiliang Huang,Lidong Cao

A controlled pesticide delivery system has attracted considerable attention in recent years. Metal–organic frameworks (MOFs), which are one of the most rapidly developing porous materials, have been used as pesticide carriers. However, the inherent toxicity of reported metal nodes or the expensiveness of organic ligands is not desirable, which limits the practical application of such pesticide-loaded MOF delivery systems. γ-Cyclodextrin-based MOFs (γ-CD–MOFs) are considered as a green renewable framework material; however, it has been less exploited as a multifunctional pesticide carrier in agricultural applications. In this study, avermectins (AVM) were loaded into γ-CD–MOFs (AVM−γ-CD–MOFs) with a loading content of 20.41% by physical absorption. AVM−γ-CD–MOFs exhibited pH-responsive release profiles and had better stability under photoirradiation. Moreover, it could promote the growth of cotton roots and stems, improve the chlorophyll content, and decrease malondialdehyde content to a certain extent by facilitating the activities of peroxidase. Compared with AVM technical concentrate wettable powder, the AVM−γ-CD–MOF wettable powder exhibited a better acaricidal activity against Panonychus citri (McGregor). In short, this research explores the feasibility of γ-CD–MOFs as a platform for potential application in sustainable plant protection.

CAS / MDL: 57-09-0
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SURFACE & COATINGS TECHNOLOGY · 2023 · IF 5.4

Vancomycin-loaded silica coatings for controlled release of drug and Si ions to repair infected bone defects

Shiqi Xiao,Li Yuan,Jiangshan Liu,Gen Li,Qin Zou,Yi Zuo,Jidong Li,Yubao Li

Promoting bone regeneration while inhibiting bacterial infection is still clinical challenge in the repair of infectious bone defects. Herein, a vancomycin-loaded silica coating with controlled release of drug and Si ions was prepared on polymer matrix via layer-by-layer assembly, to construct a functional composite coating scaffold with antibacterial function and enhanced bone regeneration capacity. Different release behavior and antibacterial effect were achieved by alternating or sequential deposition on the scaffold surface. In vitro study showed that both the alternating and the sequential coatings could promote osteogenic differentiation of bone mesenchymal stem cells, and the sequential coating exhibited a higher bacteriostatic rate of 97 % against Staphylococcus aureus . In vivo study of infectious bone defect model demonstrated that the sequential coating with an outer layer of vancomycin allowed more sufficient antibacterial treatment in the early stage of infection and achieved superior bone regeneration consequently. Transcriptomic analysis indicated that the vancomycin loading in the silica coating played an antibacterial role without interfering with the bone-promoting process of silicon ions, and revealed that the mechanism of osteogenic promotion was based on the activation of osteo/angio-genic related genes expression and corresponding signaling pathways. This study demonstrates an effective strategy to design functional composite scaffolds for complex infectious bone repair.

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