Acta Biomaterialia
·
2017
·
IF 6.319
Shengjun Mu,Yongjun Liu,Tianqi Wang,Jing Zhang,Dandan Jiang,Xiaoyue Yu,Na Zhang
A novel and intelligent pH-controlled system having an “on-off” switch based on poly( l -histidine) (PLH) and poly(ethylene glycol) (PEG) coated mesoporous silica nanoparticles (MSNs) (MSNs-PLH-PEG) was designed and evaluated for tumor specific drug release. The unsaturated nitrogen-rich polymer, PLH, which can change its solubility at different pH values, was employed for establishing the reversible “on-off” switch. In vitro drug release results demonstrated that MSNs-PLH-PEG has a pH-controlled “on-off” profile with the change of pH value between pH 7.4 and 5.0. Furthermore, in vitro cellular uptake study results showed that the entrapped drug could be efficiently released from MSNs-PLH-PEG under acidic endosome/lysosome. In vitro cell cytotoxicity and in vivo antitumor studies results indicated that sorafenib loaded MSNs-PLH-PEG exhibited good anti-proliferation and tumor growth inhibition effects. Haemolysis assay and histological analysis of MSNs-PLH-PEG showed negligible haemolysis activity and no visible tissue toxicity at the test dose. This study represents a promising and intelligent pH-controlled intelligent system for drug delivery and controlled release. Statement of Significance A novel pH-controlled intelligent and reversible “on-off” switch system based on poly( l -histidine) and poly(ethylene glycol) coated mesoporous silica nanoparticles (MSNs-PLH-PEG) by “graft to” synthesis method was constructed for tumor specific drug release. The unsaturated nitrogen-rich pH-sensitive polymer, PLH, which can change its solubility in different pH values, was employed as the reversible “on-off” switch in MSNs for the first time. The pH-controlled “on-off” switch manner was observed in the drug release results in vitro . In the in vivo antitumor studies, sorafenib loaded MSNs-PLH-PEG could effectively suppressed tumor growth in H22 tumor bearing mice. It is expected that the pH-controlled intelligent “on-off” switch system we designed holds remarkable promise and provides valuable strategy for possible applications in cancer therapy.
研究领域:
药学
·
生物材料
·
肿瘤学
✓ 已验证
DOI
PubMed
高影响因子
CHEMICAL ENGINEERING JOURNAL
·
2026
·
IF 13.2
Liuzi Du,Xiaodong Zhai,Jianchun Wu,Xiaowei Huang,Xiaobo Zou,Zhihua Li
To address the challenge of short shelf life and microbial contamination in food preservation, this study aims to develop an intelligent pH-responsive antibacterial fiber film with controlled release capability. The modification of alkaline lignin improved the structural stability and specific surface area of HKUST-1 (from 547 to 1483 m 2 /g), while the composite film exhibited excellent mechanical properties (tensile strength: 3.74 MPa, elongation: 96.25%) and hydrophobicity (water contact angle: 120.55°). The film exhibited strong pH-dependent controlled release, with 81% of antibacterial agents released at pH 6.0 within 120 h. In vitro antibacterial tests demonstrated broad-spectrum activity against Escherichia coli ( E. coli ), Staphylococcus aureus ( S. aureus ), and Pseudomonas aeruginosa ( P. aeruginosa ). When applied to beef preservation, the film significantly reduced total volatile basic nitrogen (15.35 mg/100 g), total viable count (6.23 log CFU/g), and pH (6.02) after 9 days of storage, extending the shelf life by 4 days compared to the control. This work provides a feasible strategy for developing intelligent pH-controlled-release antibacterial packaging materials.
✓ 已验证
产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2026
·
IF 8.5
Chuyi Wang,Jingxin Chen,Nan Chen,Bingru Zhang,Wenyan Wu,Weiran Lin,Yuxin He,Jin Zhang,Yudong Lu,Zixing Yan
The half-life of the traditional Chinese medicine Anzhong Decoction (AZD) is relatively short. When administered orally, insufficient retention in the stomach and rapid clearance rates result in significantly reduced drug utilization efficiency. To address this limitation, we developed ternary composite sodium alginate/gelatin/guar gum hydrogel beads (SA/Gel/GG HBs) using ion-gelation technology. Research revealed that guar gum (GG) incorporation enhances hydrogen bonding and network heterogeneity, as confirmed by ATR-FTIR and rheological analysis. Specifically, the formulation containing 0.4% GG (SA/Gel/4GG) achieved an optimal balance of properties. It demonstrated an encapsulation efficiency of 76.09%, a loading capacity of 7.02% and a high-water retention of 85.24%. Crucially, SA/Gel/4GG sustained gastric flotation for over 6 h with a flotation rate exceeding 95.04%. This was attributed to its low-density closed-cell structure, featuring a density of 0.36 g/cm 3 and porosity of 17.10%. The optimized microsphere exhibited a first-order kinetic release mechanism with biphasic release characteristics. Within 6 h, 79.21% of AZD was released into gastric fluid, followed by sustained release in the intestine. The antioxidant activity of AZD against DPPH and ABTS was well preserved. This SA/Gel/GG system presents a promising gastric-floating oral delivery platform for traditional Chinese medicine compounds, effectively extending gastric retention and enabling controlled drug release.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Pharmaceutics
·
2026
·Vol. 18
·期 7
·872
·
IF 6.9
Weinan Li,Sisi Yan,Yingying Gao,Yuhan Fu,Yutong Mei,Yanhong Wang,Zhixin Yang
Background: The highly heterogeneous and dynamically evolving tumor microenvironment leads to the development of drug resistance and recurrence in traditional therapies. Although immunotherapy demonstrates unique advantages, its clinical utility remains constrained by the suboptimal immunogenicity and the limited effect of monotherapy. Herein, a hybrid drug delivery system based on a spatiotemporal hierarchical controlled-release strategy was proposed to achieve dual immunotherapy with immune checkpoint blockade (ICB) and immunogenic cell death (ICD) to promote synergistic anti-tumor therapy.Methods: A liposome–micelle hybrid drug delivery system (RUT-RPP-LP) was constructed using a lipid bilayer composed of dioleoyl phosphatidylethanolamine/hemisuccinyl cholesterol to encapsulate rutin (RUT) and to form an inner cavity-encapsulated resveratrol micelle (RPP). RUT-RPP-LP was characterized, and its pH sensitivity and release behavior were investigated. Subsequently, a colon cancer tumor-bearing mouse model was constructed to evaluate the in vivo targeted anti-tumor effect and biological safety. On this basis, the combined mechanism of ICB and ICD was preliminarily explored.Results: RUT-RPP-LP possessed excellent formulation characteristics, stability, and biocompatibility, achieving graded controlled release of drugs via responding to the TME and lysosomal acidity, respectively. Obviously, RUT-RPP-LP could specifically target the tumor site, induce the occurrence of ICD, and simultaneously block the PD-1/PD-L1 immune checkpoint signaling pathway, thereby enhancing the function of T cells and inducing apoptosis of tumor cells.Conclusions: The RUT-RPP-LP based on the hierarchical controlled-release strategy exerted a spatiotemporally coordinated enhancement of anti-tumor immunity, and may provide a novel combinatorial approach to overcome the low response of immunotherapy in solid tumors.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
PROGRESS IN ORGANIC COATINGS
·
2025
·
IF 7.3
Hao Yang,Yi Liu,Hao Chen,Hua Li
Epoxy resin coatings are widely used for corrosion protection due to their cost efficiency, strong chemical durability and favorable mechanical strength. Antifouling agents have also been commonly applied to epoxy coatings for further antifouling function. However, due to the lack of reliable control of continuous release of the antifouling agents, the antifouling effect and service life keeps elusive. This study used a zinc-based metal organic framework ZIF-8 as a nanocarrier to prepare a novel antifouling agent NH 2 -ZIF-8@BITEP. The antifouling agent has uniform particle size and can effectively kill E. coli and S. aureus . After blending with epoxy resin, the resulting ZB coating effectively achieves contact sterilization, especially the ZB coating containing 20wt%NH 2 -ZIF-8@BITEP shows pronounced capability of inhibiting the formation of bacterial biofilm and the adhesion of algae even after 14 days incubation. In addition, the coating shows significantly enhanced corrosion resistance due to the hindering effect of the nanoparticles in the coating. After 7 days of salt spray testing, the ZB coating exhibits the least corrosion occurrence and no decrease in |Z| during EIS testing. The results would give insight into further understanding and potential antifouling and anti-corrosion applications of the newly synthesized antifoulant.
✓ 已验证
产品关联
DOI
高影响因子
BIOORGANIC CHEMISTRY
·
2023
·
IF 5.1
Xinxin Liu,Lei Chen,Ze Chen
Photodynamic therapy (PDT) has emerged as a highly efficacious therapeutic modality for malignant tumors owing to its non-invasive property and minimal adverse effects. However, the pervasive hypoxic microenvironment within tumors significantly compromises the efficacy of oxygen-dependent PDT, posing a formidable challenge to the advancement of high-efficiency PDT. Here, we developed a nanostructured photosensitizer (PS) assembled by cationic and anionic zinc phthalocyanines to load oxygen-throttling drug atovaquone (ATO), which was subsequently coated with polydopamine to obtain the final product ATO/ZnPc-CA@DA. ATO/ZnPc-CA@DA exhibited excellent stability, particularly in the blood milieu. Interestingly, the acidic microenvironment can trigger drug release from ATO/ZnPc-CA@DA, leading to a significant enhancement in fluorescence and an augmented generation of reactive oxygen species (ROS). ATO/ZnPc-CA@DA can induce synergistic cytotoxicity of PS and ATO, and significantly enhance the killing ability against tumor cells under hypoxic conditions. The mechanism underlying cytotoxicity of ATO/ZnPc-CA@DA was demonstrated to be associated with augmented cell apoptosis, disruption of mitochondrial membrane potential, diminished ATP production, heightened intracellular ROS generation, and reduced intracellular oxygen consumption. The animal experiments indicated that ATO/ZnPc-CA@DA possessed enhanced tumor targeting capability, along with a reduction in PS distribution within normal organs. Furthermore, ATO/ZnPc-CA@DA exhibited enhanced inhibitory effect on tumor growth and caused aggravated damage to tumor tissue. The construction strategy of nanostructured PS and the synergistic antitumor principle of combined oxygen-throttling drugs can be applied to other PSs, thereby advancing the development of photodynamic antitumor therapy and promoting the clinical translation.
研究领域:
生物医学工程
·
肿瘤学
·
药剂学
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF CONTROLLED RELEASE
·
2025
·
IF 11.5
Cheng Chen,Qingyun Wei,Zhen Zhu,Wenhui Wu,Tiantian Gong,Yangbo Lv,Aimei Zhang,Chunping Hu,Qichen Zhan,Tao Cao,Peng Cao
Controlled drug delivery systems not only augment the therapeutic efficacy of drugs but also mitigate their adverse effects. Methotrexate (MTX) is a prominent first-line therapeutic agent in the management of rheumatoid arthritis (RA), yet it is characterized by its limited aqueous solubility, pronounced hemolytic activity, and propensity for off-target binding, which collectively contribute to its significant toxicity profile. To address these issues, a temperature-responsive controlled release system for MTX based on the analogous base pairing rule was designed for the RA treatment. Magnetic ferroferric oxide nanoparticles (Fe 3 O 4 NPs) coated with polydopamine (PDA) were modified with thymidine-1-acetic acid (TAA) to prepare nanocarrier (FPT NPs). Furthermore, the thymine molecules within the FPT NPs possessed the strong ability to specifically bind with the pteridine structure present in MTX, thereby enabling the fabrication of a nanomedicine (designated as FPT-MTX NPs) through the base pairing rule. Under the influence of an applied magnetic field, the FPT-MTX NPs demonstrated a remarkable capacity for precisely targeting the joint tissue in a mouse model of RA. Analogous to DNA, where double-strand breaks occurred due to heating-induced disruption of base pairing, MTX was released from FPT-MTX NPs following near-infrared irradiation-induced light-to-heat conversion. This mechanism facilitated the achievement of satisfactory therapeutic outcomes in the RA treatment.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
MOLECULAR PHARMACEUTICS
·
2026
·
IF 4.5
Hongyu Lin,Huwei Bian,Junyao Li,Laidi Xu,Tao Jiang,Yong Kong
To enhance the therapeutic efficacy of breast cancer, multimodal therapy with the aid of a pH-responsive controlled release platform is proposed in this work. Indocyanine green (ICG) is loaded in honeycomb MnO2 (hMnO2) synthesized by a template method, which is coencapsulated with 5-fluorouracil (5-FU) in the hydrogels cross-linked between carboxymethyl chitosan (CMCS) and oxidized hyaluronic acid (OHA). The imine linkage (−HC═N−) between CMCS and OHA is hydrolyzed under weakly acidic conditions, leading to the release of 5-FU for chemotherapy and ICG/hMnO2. The hMnO2 can convert the optical energy of near-infrared (NIR) light into heat for photothermal therapy (PTT). Additionally, the hMnO2 can be reduced to Mn2+ at low pH and high glutathione (GSH) level, and the produced Mn2+ can further react with H2O2 to generate hydroxyl radicals (·OH) through a Fenton-like reaction for chemodynamic therapy (CDT). ICG can be simultaneously released during the reduction of hMnO2, which can catalyze the conversion of oxygen to singlet oxygen (1O2) upon exposure to NIR light for photodynamic therapy (PDT). Due to the synergistic effects of chemotherapy, PTT, CDT, and PDT, the developed ICG/hMnO2/5-FU/CMCS/OHA hydrogels can significantly inhibit the growth of the 4T1 mouse breast cancer cell line.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF POLYMER RESEARCH
·
2018
·Vol. 25
·期 9
·1-9
·
IF 1.434
Du Huang,Han Ruitao,Tang Erjun,Zhou Jian,Liu Shaojie,Guo Xiaofeng,Wang Ruihong
A pH-responsive cellulose-g-P4VP copolymer was synthesized by atom transfer radical polymerization (ATRP) in ionic liquid 1-allyl-3-methylimidazolium chloride [AMIM]Cl. The polymer structure was characterized by Fourier transform infrared (FT-IR), 1 H nuclear magnetic resonance (NMR) and gel permeation chromatography (GPC). The P4VP brushes that were covalently bonded to the cellulose backbone had a narrow molecular weight distribution, which was helpful for use in drug loading. The loading and controlled release of drug using aspirin as model drug in the micelles obtained the cellulose-g-P4VP copolymer was investigated. The structure and size of the copolymeric micelles were characterized by transmission electron microscopy (TEM), dynamic light scattering (DLS) and ultraviolet–visible (UV-Vis) spectroscopy, respectively. Blank micelles presented a stably spherical morphology with dimeter about 90 nm in aqueous solution. The resultant micelles had clear pH-sensitivity with a pH-dependent phase transition point at a pH of about 5.7. Drug-loaded micelles had a spherical, core–shell structure with dimeter about 150 nm. The polymeric micelles revealed an excellent controlled drug release at different pH values and the cumulative release of aspirin in phosphate buffer reached to 86.4% at pH 5.8, 60.9% at pH 7.4 and 42.2% at pH 8.0.at 50 h. The pH-sensitive cellulose-g-P4VP copolymer had an enormous potential as carriers for released drug delivery.
研究领域:
材料科学
·
药学
·
高分子化学
✓ 已验证
DOI
高影响因子
JOURNAL OF BIOMATERIALS SCIENCE-POLYMER EDITION
·
2020
·
IF 2.69
Juan Wu,Xi Wang,Binglong Zhu,Qinting He,Fang Ren,Fei Tong,Wei Jiang,Xianghong He
Cancer is one of the biggest killers threat to human life and health and is still difficult to treat mainly due to the lack of targeted drug delivery stages and limitations associated with delivering drugs to targeted cancer tissues. The goal of this work was to develop a magnetic, pH-sensitive formulation for targeted delivery of chemotherapeutic agents to cancer cells. Then the functional drug delivery system (Fe3O4@CS/PEG-DOX) was synthesized by the layer-by-layer (LbL) self-assembly technique. And the drug loading content is calculated to be 19.1%. In addition, the Fe3O4@CS/PEG-DOX exhibited excellent pH-sensitivity, 73.1% DOX was released within 48 h at pH 4.0. Furthermore, all the release behaviors fit the Higuchi model very well and the dissolution of CS/PEG layers played a key role on DOX release from Fe3O4@CS/PEG-DOX. The results of toxicity analysis in human liver hepatocellular carcinoma cells (HepG2) revealed that Fe3O4@CS/PEG-DOX exhibited high anti-tumor activity, while the Fe3O4@CS/PEG nanocomposites were practically non-toxic. Therefore, all the results demonstrated that the Fe3O4@CS/PEG-DOX could have an important impact on the development of targeted intracellular delivery nanodevices for cancer therapy.
研究领域:
药学
·
纳米技术
·
癌症研究
·
药物递送系统
✓ 已验证
DOI
PubMed
高影响因子
Small
·
2023
·Vol. 19
·期 16
·2206124
·
IF 13.3
Futing Yang,Wenjie Yu,Qiying Yu,Xiyu Liu,Chunping Liu,Chong Lu,Xinghua Liao,Yi Liu,Na Peng
The apoptosis-resistant mechanism of photodynamic therapy (PDT) usually results in limited therapeutic efficacy. The development of new strategies for sensitizing targeted ferroptosis that bypass apoptosis resistance is of great significance to improve the antitumor efficacy of PDT. In this study, a novel amphiphilic copolymer whose main chain contains reactive oxygen species (ROS)-responsive groups and the end of side chains contains triphenylphosphine is synthesized, to encapsulate porphyrinic metal–organic framework PCN-224 via self-assembly which are hydrothermally synthesized by coordination of zirconium (IV) with tetra-kis(4-caboxyphenyl) porphyrin, and loaded carbon monoxide releasing molecule 401 (CORM-401) by their hollow structures (PCN-CORM), and finally, surface-coated with hyaluronic acid. The nanosystem can sequentially localize to mitochondria which is an important target to induce apoptosis and ferroptosis in cancer cells. Upon excitation with near-infrared light, PCN-224 is activated to produce amounts of ROS, and simultaneously triggers the rapid intracellular release of CO. More importantly, the released CO can sensitize ferroptosis and promote apoptosis to significantly enhance the antitumor efficacy of PCN-224 both in vitro and in vivo. These results illustrate that the mitochondria-targeted drug delivery system combined PDT with CO leads to an effective antitumor efficacy, which maybe a promising way to enhance the treatment efficiency of PDT.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
·
2022
·
IF 5.589
Jie Luo,Long Wan,Qiyan Zhang,Bufeng Cui,Chen Li,Yi Jiang,Mingyan Jiang,KeKe Wang
To study the release behavior of a thermosensitive controlled release drug delivery system and construct a predictable mathematical model of drug release, poly(N-isopropylacrylamide-co-Allylamine) (P(NIPA-AL17)) and ploy(styrene sulfonate) (PSS) were functionalized on the surface of hollow mesoporous carbon nanoparticles (HMCNs) through layer-by-layer (LBL) assembly to construct a photothermal responsive controlled release system. A five-level four-factorial central composite design (CCD) was performed to investigate the relationship between four independent variables including drug loading (A), number of polymer layers (B), temperature (C) and vibration rate of the shaker (D), and three dependent response variables, including cumulative release over 1 h (Y 1 ), cumulative release over 24 h (Y 2 ) and the release rate constant k (Y 3 ). The CCD results indicate that A and C significantly affect Y 1 (P < 0.05). C significantly affects Y 2 (P < 0.05). A and B is found to affect Y 3 (P < 0.05) significantly. When C is below 39 °C, Y 1 and Y 2 decrease with the increase of A and B, and when C is above 39 °C, they increase with the increase of A and B; Y 3 decreases as A and B increase; and D shows the least or even no influence on Y 1 , Y 2 and Y 3 . The constructed predictable mathematical model will provide a scientific reference for the further development and application of photothermal responsive controlled-release preparations.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）