MICROCHEMICAL JOURNAL
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2025
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IF 5.1
Raj Kumar Parajuli,Jin Liu,Shree Krishna Tamang,Govinda Gurung,Kumar Neupane,Yao Wang,Christopher D. Snow,Matt J. Kipper,Laurence A. Belfiore,Jianguo Tang
Patient urine may provide relatively convenient access to biomarkers, but it is challenging to directly and visibly sense drugs via fluorescence quenching or enhancement. This study reports the synthesis of water-soluble and fluorescence-stable terbium-induced nanoaggregates (TIPAs) of polystyrene-poly(acrylic acid) (PS- b -PAA), containing a novel [Tb( acac )Cl 2 ( phen )Cyclen] complex, to sense doxorubicin ( dox ) in urine. The TIPAs demonstrated remarkable water stability, maintaining high fluorescence intensity in aqueous environments, with a fluorescence lifetime of 55.5 ms and a quantum yield (QY) of 4.60 %, making them ideal for smart sensing applications. The novel aggregate exhibits an orthorhombic structure, with its photophysical properties elucidated through simulated modeling. Fluorescence quenching studies indicate dynamic interactions between TIPAs and dox in urine, achieving a limit of detection (LOD) of 13.77 μM, highlighting the method's sensitivity for real-time dox monitoring. The emission of TIPAs in the visible range (450–600 nm) overlaps with the absorption spectrum of dox , enabling efficient energy transfer and fluorescence quenching. These findings highlight the potential of TIPAs as stable, fluorescence-based sensors for drug monitoring, with promising applications in bioimaging and diagnostics within cancer therapy.
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高影响因子
Materials Express
·
2021
·Vol. 11
·期 10
·1619-1627
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IF 0
Zhang Yue,Liu Yuanfen,Hu Yumin,Pan Lei
In this study, we developed an active targeting nano-immunoplatform of doxorubicin (DOX)-loaded bovine serum albumin (BSA) modified with the humanized antibody cetuximab, which can target the epidermal growth factor receptor (EGFR) of EGFR-overexpressing colon cancer, and subjected
it to a series of in vitro evaluation. The obtained cetuximab-modified nanoparticles (cetuximab-DOX-immuno-NPs) had an average particle size of 218.2±2.2 nm, a polydispersity index of 0.162±0.023, a zeta potential of −23.28±0.75 mV, and a cetuximabloading
efficiency of 33.6%±3.5%. The results of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide cytotoxicity experiments showed that the cytotoxic of cetuximab-DOX-immuno-NPs in EGFR-overexpressing RKO colon cancer cells was significantly higher than it was in EGFR-under-expressing
LS174 T cells. The results of flow cytometry showed that when DOX-immuno-NPs were used, DOX was eliminated soon after entering the cells, whereas when cetuximab-DOX-immuno-NPs were used, DOX efflux was reduced. Confocal laser-scanning microscopy was used to visualize the endocytosis of nanoparticles,
and revealed that the fluorescence intensity of cetuximab-DOX-immuno-NPs was significantly higher than that of non-specific IgG-DOX-immuno-NPs in RKO cells. Moreover, in EGFR-under-expressing LS174 T cells, both cetuximab-DOXimmuno-NPs and Immunoglobulin G-DOX-immuno-NPs showed weak DOX fluorescence
intensity, reflecting the specificity and selectivity of cetuximab-modified nanoparticles toward EGFR-overexpressing cancer cells. This study demonstrated that cetuximab modification of DOX-loaded BSA nanoparticles can increase their selectivity and reduce their toxicity. As this would decrease
the side effects of these treatments in patients, this study shows that cetuximab-modified doxorubicin-loaded bovine serum albumin nanoparticles are promising candidates for targeted colon cancer therapy.
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JOURNAL OF NANOSCIENCE AND NANOTECHNOLOGY
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2016
·Vol. 16
·期 7
·7530-7538
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IF 1.338
Wang Yang,Nie Jinshan,Wang Wei,Gu Zhun
In this work, redox and pH responsive vesicles of PEGylated hyperbranched poly(amidoamine)-doxorubicin (PPCD) conjugates were prepared for the improvement of cancer therapy. The PPCD 3/1 and PPCD 6/1 conjugates were respectively prepared by the acid sensitive cis-aconityl linkage
between doxorubicin and differently PEGylated hPAMAM (PEG3-g-hPAMAM and PEG6-g-hPAMAM). The PPCD vesicles were prepared by disulfide-crosslinking the micelles formed in THF and then transferring them from THF into water. The crosslinked
PPCD vesicle with a higher PEGylated degree showed a measurable decrease in size and zeta potential. Both the crosslinked PPCD vesicles could be disassembled into small-sized conjugates under the redox condition. The drug release profiles showed that the both vesicles presented stimuli-triggered
drug release in acidic and reducing environment and lower DOX leakage under neutral condition. The cytotoxicity assay reflected that both the PPCD vesicles could effectively kill the gastric cancer MGC803 cells, and PPCD 6/1 vesicle with smaller size presented higher cytotoxicity than PPCD
3/1 vesicle. Considering the more applicable size (about 100 nm), higher capacity of killing tumor cells and better compatibility, the PPCD-6 vesicle with higher PEGylation degree is more favorable to promote the therapeutic effect of cancer, and will be more suitable as drug delivery system
for solid tumor treatment.
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高影响因子
Biomaterials Advances
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2025
·
IF 6
Chen Wang,Yin Li,Xiaoxue Shen,Shiwei Xiao,Huiying Du,Qianye Zhao,Ying Wang,Qiangtao Zhang,Shuxin Wen
Background Patients with locally advanced head and neck squamous cell carcinoma (HNSCC) exhibit poor survival due to tumor microenvironment (TME) barriers and systemic toxicity of chemo-immunotherapy associated with chemo-immunotherapy. Methods An injectable thermoresponsive hydrogel was engineered by crosslinking D-α-tocopheryl polyethylene glycol succinate (TPGS) with Na₂CO₃ (15 % w/v TPGS: 9 % w/v Na₂CO₃). This platform co-encapsulated doxorubicin-loaded nanoparticles (DOX NP) synthesized via PEI-cis-aconitic acid conjugation and CpG-loaded adjuvant nanoparticles (CpG NP) prepared through genipin-mediated PEI crosslinking. The hydrogel exhibited rapid temperature-triggered gelation, shear-thinning injectability, and a macroporous architecture that enabled dual drug retention and immune cell infiltration. Results In vitro , the hydrogel provided the sustained release of DOX NP with pH-responsive acceleration in acidic TME. In vivo , localized delivery of Gel-DOX NP-CpG NP significantly suppressed tumor growth ( p < 0.05) and enhanced cytotoxic CD8 + T-cell infiltration in TME (3.1-fold) and spleens (2.4-fold). RNA sequencing revealed 88 immune-related differentially expressed genes, including downregulated immunosuppressors and enriched cytokine pathways. Conclusion This TPGS/Na₂CO₃ hydrogel platform coordinates chemotherapy-induced immunogenic cell death (DOX NP) with CpG-driven innate immunity, overcoming TME barriers to enhance localized and systemic anti-tumor responses in HNSCC.
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PubMed
高影响因子
Journal of Physical Chemistry C
·
2016
·
IF 4.509
Xiaojun Zhou,Liang Chen,Wei Nie,Weizhong Wang,Ming Qin,Xiumei Mo,Hongsheng Wang,Chuanglong He
The combination of chemotherapy and gene therapy could induce the enhanced therapeutic efficacy in the cancer therapy. To achieve this goal, a new mesoporous silica nanoparticles (MSNs)-based codelivery system was developed for targeted simultaneous delivery of doxorubicin (DOX) and Bcl-2 small interfering RNA (siRNA) into breast cancer cells. The multifunctional MSNs (MSNs-PPPFA) were prepared by modification of polyethylenimine–polylysine copolymers (PEI-PLL) via the disulfide bonds, to which a targeting ligand folate-linked poly(ethylene glycol) (FA-PEG) was conjugated. The multifunctional MSNs-PPPFA nanocarrier has the ability to encapsulate DOX into the mesoporous channels of MSNs, while simultaneously carrying siRNA via electrostatic interaction between cationic MSNs-PPPFA and anionic siRNA. The resulting MSNs-PPPFA nanoparticles were characterized with various techniques. The drug release results reveal that DOX released from DOX-loaded MSNs-PPPFA are both pH- and redox-responsive, and the results of cell viability and hemolysis assays show that the functional nanocarrier has excellent biocompatibility. Importantly, the folate-conjugated MSNs-PPPFA showed significantly enhanced intracellular uptake in the folate receptor overexpressed MDA-MB-231 breast cancer cells than nontargeted counterparts and thus results in more DOX and siRNA being codelivered into the cells. Furthermore, the delivery of Bcl-2 siRNA obviously downregulate the Bcl-2 protein expression, and thus targeted codelivery of DOX and Bcl-2 siRNA by DOX@MSNs-PPPFA/Bcl-2 siRNA in MDA-MB-231 cells could induce remarkable cell apoptosis as indicated by the results of cell viability and cell apoptosis assays. These results indicate that the constructed DOX@MSNs-PPPFA/Bcl-2 siRNA codelivery system is promising for targeted treatment of breast cancer.
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高影响因子
APPLIED CATALYSIS B-ENVIRONMENTAL
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2021
·
IF 19.503
Haoyang Fu,Ruizhao Wang,Qianyu Xu,Minwang Laipan,Chenliu Tang,Weixian Zhang,Lan Ling
Typical antineoplastic agent doxorubicin (DOX) contamination is a major environmental concern and its efficient purification remains a daunting challenge so far. This work explored the potential of Fe/Pd-doped graphite carbon nitride (g-C 3 N 4 @Fe/Pd) for DOX removal from water, involving the removal performance, mechanism, and pathway. Structural characterization of g-C 3 N 4 @Fe/Pd showed that the metallic Pd clusters are decorated on the surface of uniformly distributed iron nanoparticles (~ 28 nm) on g-C 3 N 4 . The existence of g-C 3 N 4 effectively relieved the agglomeration and overgrowth of iron nanoparticles, the strong coupling effect among the Fe, Pd and N demonstrates the excellent DOX removal performance (k = 0.115 min −1 ) with versatility under different initial concentrations (30–150 mg/L) and material dosages (0.1–0.4 g/L). Three possible degradation pathways of DOX were proposed, where catalytic saccharide moiety elimination is the primary pathway. Importantly, intermediates exhibit lower toxicity and the final degradation product is efficiently adsorbed by g-C 3 N 4 @Fe/Pd.
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高影响因子
International Journal of Nanomedicine
·
2026
·
IF 8.7
Ling Li,Wenjing Xie,Haixia Sun,Houqiang Yu,Cai Wang,Min Zheng,Peng Shi,Hongan Tian,Tongqiang Xiong
Background Tumor recurrence and metastasis are important factors affecting the efficacy of transhepatic arterial chemoembolization. To prolong the survival of patients, comprehensive interventional therapy and antitumor drugs that can control their release need to be developed.Methods Poly(N-isopropylacrylamide-co-acrylic acid) nanogels are firstly self-assembled with doxorubicin, the constructed doxorubicin-loaded nanogels were then emulsified with iodized oil under high-shear conditions to form doxorubicin–iodized oil nanogel suspensions (Dox-TIPE). The structural characteristics, thermosensitive properties and rheological properties were evaluated. The in vitro biocompatibility and drug release behavior of Dox-TIPE were assayed and in vivo interventional therapy was examined in a VX2 rabbit liver cancer model.Results Dox-TIPE can effectively exert the dual advantages of chemoembolization therapy, achieving a superior therapeutic effect on inhibiting rabbit liver tumor growth. It promotes TUNEL expression in the tumor boundary region while reducing Ki67 expression, which results in decreased tumor cell proliferation and increased apoptosis rates. Furthermore, Dox-TIPE effectively suppresses the expressions of HIF-1α, VEGF, and CD31 in tumor target areas, thereby preventing the formation of tumor neovascularization and collateral circulation.Conclusion We successfully produced Dox-TIPE which offers a multifunctional platform combining embolization, chemotherapy, imaging, and immunomodulation. This novel embolic material shows strong potential to address current limitations of TACE in liver cancer treatment and may serve as a promising candidate for next-generation embolization therapies.
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高影响因子
JOURNAL OF MEDICINAL CHEMISTRY
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2026
·
IF 6.8
Xinyue Zhao,Naijie Wei,Ziyang Fang,Yingyan Xie,Xiaowen Yan,Qiuquan Wang
To address the low cytotoxicity and drug resistance issues of targeted covalent inhibitor (TCI) ibrutinib and severe side effects of chemotherapeutics doxorubicin (DOX), we developed a novel targeted covalently activated chemotherapy strategy. We designed and synthesized a targeted covalently activated chemotherapy drug, Ibt-DOX, which features a targeting ligand of ibrutinib, a DOX, an electrophilic warhead α-methylated acrylamide (α-MAA) and a self-immolative linker p-hydroxybenzyl alcohol. Upon specifically binding to BTK, Ibt-DOX inhibits the BTK-mediated BCR signaling, meanwhile releases DOX and induces immunogenic cell death (ICD), ultimately resulting in not only significantly enhanced targeted B-cell lymphoma cells death compared with ibrutinib, but also reduces the toxic side effects of DOX on BTK- cells. Our work offers a novel strategy through leveraging the synergistic effect of targeted covalent inhibition and the high cytotoxicity of chemotherapy drug, which will inspire the development of new targeted covalent chemotherapeutics for different cancers treatment.
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高影响因子
INTERNATIONAL IMMUNOPHARMACOLOGY
·
2026
·
IF 5.6
Ning Jiang,Fengying Yin,Qianqian Dang,Guoliang Chen,Xiaoxia Wu,Saining Wang,Xuelin Wang,Lin Sun
MOF-ABZ significantly improved apparent aqueous dispersibility of ABZ. • MOF-ABZ induced ROS-associated ICD signaling in HCC cells. • MOF-ABZ potentiated the antitumor efficacy of low-dose DOX while reducing systemic toxicity in vivo . Doxorubicin (DOX) is widely used to treat hepatocellular carcinoma, but its dose-dependent cardiotoxicity limits its clinical application. Although dose reduction can mitigate cardiac injury, it often weakens antitumor efficacy, underscoring the need for effective sensitization strategies. Albendazole (ABZ) can induce reactive oxygen species (ROS) production, which may promote immunogenic cell death (ICD); however, its poor aqueous solubility restricts therapeutic application. To overcome this limitation, γ-cyclodextrin-based metal-organic frameworks were used to encapsulate ABZ, generating MOF-ABZ for low-dose DOX sensitization. MOF-ABZ improved ABZ dispersion and induced ROS-associated immunogenic responses in HepG2 cells, as indicated by the release of damage-associated molecular patterns (DAMPs), dendritic cell maturation, and early CD8 + T-cell activation; these effects were attenuated by N -acetylcysteine. MOF-ABZ further sensitized HepG2 cells to DOX, reducing the DOX IC₅₀ from 119.5 to 91.3 ng/mL. In H22 tumor-bearing mice, the combination of low-dose DOX and MOF-ABZ achieved tumor inhibition comparable to that of high-dose DOX alone and superior to that of low-dose DOX monotherapy, with less body-weight loss, milder histological myocardial damage, and cytokine changes consistent with immunomodulatory activity. In conclusion, through efficient ABZ delivery, MOF-ABZ enhances the antitumor efficacy of low-dose DOX, and these ROS-associated immunogenic responses potentially contribute to this sensitization effect, providing a promising strategy to improve the therapeutic index of DOX in HCC models. Download: Download high-res image (174KB) Download: Download full-size image
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高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
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2026
·
IF 6
Yue Wei,Yangyi Chen,Huajing Zhang,Qiao Li,Huajuan He,Xiao Liang,Shiyuan Lin,Hui Chen,Wei Wu,Wei Zhang
A kind of purine nucleoside-chitosan-silybin (PN-CS-SB) polymeric micelles were developed for enhancing the oral absorption of doxorubicin (DOX) by intestinal nucleoside transporter mediation, the inhibition of P-glycoprotein (P-gp) efflux and CYP3A4 metabolism. The four types of PN, including adenosine, deoxyadenosine, guanosine and deoxyguanosine, respectively, and silybin, were conjugated to chitosan via the linker succinic acid. The synthesized PN-CS-SB were identified by 1 H NMR and FT-IR, and the doxorubicin (DOX)-loaded micelles were prepared by ultrasonication. The micelles demonstrated a series of the excellent properties, including the high drug loading capacity of above 8.2%, the regular spherical shapes with the small particle sizes of below 150 nm, and the low critical micelle concentration of below 5.82 × 10⁻⁶ g/mL. The oral bioavailability of the DOX-loaded micelles against DOX solution achieved to as high as 453.28%. The rapid and tremendous absorption of micelles was visually demonstrated by in vivo imaging. The micelle absorption mechanism was proved to be nucleoside transporter-mediation as well as the dual inhibition of P-gp and CYP3A4 by the cellular uptake, enzyme inhibition and immunofluorescence location test. The cellular endocytosis and transportation pathway of micelles across intestinal epithelial cells involved nucleoside transporter target, caveolin mediation or macropinocytosis with energy consumption. Download: Download high-res image (234KB) Download: Download full-size image
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高影响因子
MICROCHEMICAL JOURNAL
·
2025
·
IF 5.1
Qian Bi,Hongmei Zhang,Han He,Qian Li,Baoting Dou
Doxorubicin (DOX) is a frequently prescribed chemotherapy medication for a range of cancers. It is essential to monitor the levels of doxorubicin in human biological fluids to ensure effective treatment. An efficient electrochemical sensor for amplified detection of DOX is developed in this work. The strand displacement reaction is initiated when the blocking probe, which attaches to the terminal toehold sequence of the immobilization probe, is released due to the selective recognition of DOX with the aptamer probe. The secondary toehold region is then available for hybridization with the methylene blue (MB)-labeled signal probe, causing the blocking probe to be displaced and activating the molecular machine. Consequently, the blocking probe is reused in a cyclical manner, with numerous signal probes being attached to the sensor surface, resulting in a significant increase in current for quantitative analysis. This technique successfully detected DOX in human serum samples with high selectivity and sensitivity, reaching a detection limit of 670 fM. The proposed research offers a novel approach to identifying various biomarkers, with the potential to significantly advance clinical diagnosis and drug research.
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高影响因子
BIOMACROMOLECULES
·
2012
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IF 5.479
Longlong Chang,Liandong Deng,Weiwei Wang,Zesheng Lv,Fuqiang Hu,Anjie Dong,Jianhua Zhang
A novel biodegradable amphiphilic diblock copolymer methoxy poly(ethylene glycol)-b-poly(ε-caprolactone-co-γ-hydroxyl-ε-caprolactone) (mPEG-b-P(CL-co-HCL)) bearing pendant hydroxyl groups on the PCL block was prepared. The hydroxyl groups were formed through the reduction of ketones by sodium borohydride without protection and deprotection. The obtained polymers were well characterized by 1H NMR, Fourier transform infrared (FT-IR), gel permeation chromatography (GPC), differential scanning calorimetry (DSC), X-ray diffraction (XRD), and contact angle measurement. mPEG-b-P(CL-co-HCL) could self-assemble into stable nanoparticles (NPs) with critical micellar concentrations (CMC) of 6.3 × 10–4 ∼ 8.1 × 10–4 mg/mL. The NPs prepared from mPEG-b-P(CL-co-HCL) were spherical in shape with diameters about 100 to 140 nm. The hydrophobic doxorubicin (DOX) was chosen as a drug model and successfully encapsulated into the NPs. The encapsulation efficiency and release kinetics of DOX were investigated. The results indicated that the introduction of hydroxyl groups onto the core-forming block could decrease the hydrophobicity of copolymers, thus improving the storage stability of NPs in aqueous solution. Moreover, higher loading capacity and slower in vitro release of DOX were observed, which was due to the hydrogen-bonding formation between DOX and hydroxyl groups. Meanwhile, the MTT assay demonstrated that the blank NPs were biocompatible to HepG2 cell,s while free DOX and DOX-loaded NPs showed significant cytotoxicity against the cells. Moreover, Compared to the free DOX, the DOX-loaded NPs were more efficiently internalized by HepG2 cells. In sum, the introduction of hydroxyl groups on the polyester block in mPEG-b-P(CL-co-HCL) exhibited great potentials for modifications in the stability, drug solubilization, and release properties of NPs.
研究领域:
高分子科学
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药物递送
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纳米医学
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生物材料
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制药技术
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高影响因子
危险品化学品经营许可证（带存储）