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COLLOIDS AND SURFACES B-BIOINTERFACES · 2017 · IF 3.887

Cube-shaped theranostic paclitaxel prodrug nanocrystals with surface functionalization of SPC and MPEG-DSPE for imaging and chemotherapy

Fuqiang Guo,Jiajia Shang,Hai Zhao,Kangrong Lai,Yang Li,Zhongxiong Fan,Zhenqing Hou,Guanghao Su

As one of nanomedicine delivery systems (NDSs), drug nanocrystals exhibited an excellent anticancer effect. Recently, differences of internalization mechanisms and subcellular localization of both drug nanocrystals and small molecular free drug have drawn much attention. In this paper, paclitaxel (PTX) as a model anticancer drug was directly labeled with 4-chloro-7-nitro-1, 2, 3-benzoxadiazole (NBD-Cl) (a drug-fluorophore conjugate Ma et al. (2016) and Wang et al. (2016) [1,2] (PTX-NBD)). PTX-NBD was synthesized by nucleophilic substitution reaction of PTX with NBD-Cl in high yield and characterized by fluorescence, XRD, ESI–MS, and FT-IR analysis. Subsequently, the cube-shaped PTX-NBD nanocrystals were prepared with an antisolvent method followed by surface functionalization of SPC and MPEG-DSPE. The obtained specific shaped [email protected] NCs had a hydrodynamic particle size of ∼50   nm, excellent colloidal stability, and a high drug-loading content of ∼64%. Moreover, in comparison with free PTX-NBD and the sphere-shaped PTX-NBD nanocrystals with surface functionalization of SPC and MPEG-DSPE ( [email protected] NSs), [email protected] NCs remarkably reduced burst release and improved cellular uptake efficiency and in vitro cancer cell killing ability. In a word, the work highlights the potential of theranostic prodrug nanocrystals based on the drug-fluorophore conjugates for cell imaging and chemotherapy.

研究领域: 药学 · 纳米技术 · 癌症研究
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LASERS IN MEDICAL SCIENCE · 2025 ·Vol. 40 ·期 1 ·1-11 · IF 2.4

ICG/MnO2-HFn-mPEG-DSPE-Lip enhances the anticancer activity of ICG phototherapy

Ma Dan,Lu Huixiang,Zhang Hai,Liao Anru,Peng Qianrong,Yang Min

Hypoxia poses a significant challenge to the efficacy of photodynamic therapy (PDT) for cancer treatment. This study aims to design and synthesize PEGylated liposomes encapsulating MnO₂, indocyanine green (ICG), and H-chain ferritin (HFn) to potentially address hypoxia and enhance the therapeutic outcomes of PDT. PEGylated liposomes (ICG/MnO₂-HFn-mPEG-DSPE-Lip) were constructed with a rod-like structure, incorporating MnO₂ as a hypoxia-modulating agent and ICG as a photosensitizer. The drug loading capacity, stability and safety of liposomes were characterized. Singlet oxygen quantum yield (Φ Δ ) was measured under simulated tumor microenvironment conditions. In vitro phototoxicity was evaluated using A549 human lung adenocarcinoma cells. Liposomes have a high drug loading capacity, good biocompatibility and good long-term stability. Under tumor-simulated conditions, Φ Δ was significantly improved, increasing from 0.210 for free ICG to 0.507. The liposomes demonstrated remarkable phototoxic effects on A549 cells (90.5% cell death under combined PDT/PTT vs. 15% for free ICG). This nanoplatform proposes a novel strategy to overcome hypoxia-induced PDT resistance, and the enhanced efficacy may be attributed to the increased oxygen supply mediated by MnO 2 carried by HFn. These findings provide important insights for the development of next-generation therapeutic systems targeting tumor hypoxia.

研究领域: 药学 · 肿瘤学 · 生物医学工程
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SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY · 2025 · IF 4.6

A dual-modality sensor for pre-clicinal imaging of diabetes-associated copper dysregulation in vivo and in urine

Shuqin Chen,Miaowei Jiang,Hangbiao Wei,Fangkun Yang,Kai Wang,Li Li,Jinhui Shang

Copper ions (Cu 2+ ) play a critical role in physiological and pathological processes, including diabetes. However, detecting Cu 2+ with high sensitivity and specificity in diabetes remains challenging. In this study, we developed a hemicyanine-based copper ion probe (CUP) encapsulated in mPEG-DSPE nanoparticles (CUNP) for dual-modality fluorescence and photoacoustic (PA) imaging of Cu 2+ . CUNP exhibited excellent aqueous solubility, biocompatibility, and a turn-on response to Cu 2+ , with activate signals. In vivo studies in streptozotocin (STZ)-induced diabetic mice revealed elevated hepatic Cu 2+ levels, which were attenuated by metformin treatment, as confirmed by PA and fluorescence imaging. Urine analysis further revealed elevated Cu 2+ in diabetic patients. These findings highlight CUNP as a promising tool for non-invasive Cu 2+ monitoring in diabetes, with potential clinical applications in disease diagnosis and therapeutic evaluation.

研究领域: 生物医学工程 · 分子影像学 · 代谢疾病研究 · 纳米医学 · 转化医学 · 生物分析化学
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Nanoscale · 2020 ·Vol. 12 ·期 20 ·11288-11296 · IF 6.895

AgFeS2 nanoparticles as a novel photothermal platform for effective artery stenosis therapy

Xuan Peng,Junchao Liu,Chen Ming,Bo Li,Zhen Zhao,Kaichuang Ye,Min Zeng,Rujia Zou,Xinwu Lu,Junqing Hu

Ternary I–III–VI2 semiconductors usually have narrow band gaps and large absorption coefficients arising from the unique characteristics of their outer-d valence electrons, which are intimately connected with the photothermal conversion properties. AgFeS2 is known as one such material that has the potential to absorb near-infrared light. In this work, we utilized density functional theory (DFT) calculations to evaluate the electronic structure and optical absorption properties of AgFeS2. Strong absorptions were predicted over a wide Vis-NIR region due to the localized 3d electron of Fe atoms, which agree quite well with the UV-Vis-NIR spectra measured by experiment. The as-prepared AgFeS2 nanoparticles were then modified with mPEG-DSPE, an efficient photothermal agent for artery stenosis therapy. Its photothermal conversion effect has been systematically studied, indicating the potential for causing the hyperthermia of macrophages, an essential part of the artery inflammation response. More importantly, both in vitro cell experiments and in vivo mouse-model studies show that the induction of hyperthermia in artery stenosis by using AgFeS2 nanoparticles is safe and effective when injected at a very low concentration. This study provides a novel photothermal platform derived from the inheritability of bandgap structure and also promotes the process of artery inflammation and stenosis therapy.

CAS / MDL: 112-90-3
研究领域: 材料科学 · 纳米技术 · 生物医学工程 · 治疗学
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ACS Applied Materials & Interfaces · 2017 · IF 7.504

GSH-Activated NIR Fluorescent Prodrug for Podophyllotoxin Delivery

Yajing Liu,Shaojia Zhu,Kaizhi Gu,Zhiqian Guo,Xiaoyu Huang,Mingwei Wang,Hesham M. Amin,Weihong Zhu,Ping Shi

Theranostic prodrug therapy enables the targeted delivery of anticancer drugs with minimized adverse effects and real-time in situ monitoring of activation of the prodrugs. In this work, we report the synthesis and biological assessment of the near-infrared (NIR) prodrug DCM-S-PPT and its amphiphilic copolymer (mPEG-DSPE)-encapsulated nanoparticles. DCM-S-PPT is composed of podophyllotoxin (PPT) as the anticancer moiety and a dicyanomethylene-4H-pyran (DCM) derivative as the NIR fluorescent reporter, which are linked by a thiol-specific cleavable disulfide bond. In vitro experiments indicated that DCM-S-PPT has low cytotoxicity and that glutathione (GSH) can activate DCM-S-PPT resulting in PPT release and a concomitant significant enhancement in NIR fluorescence at 665 nm. After being intravenously injected into tumor-bearing nude mice, DCM-S-PPT exhibited excellent tumor-activated performance. Furthermore, we have demonstrated that mPEG-DSPE as a nanocarrier loaded with DCM-S-PPT (mPEG-DSPE/DCM-S-PPT) showed even greater tumor-targeting performance than DCM-S-PPT on account of the enhanced permeability and retention effect. Its tumor-targeting ability and specific drug release in tumors make DCM-S-PPT a promising prodrug that could provide a significant strategy for theranostic drug delivery systems.

CAS / MDL: 70-18-8
研究领域: 药学 · 生物医学工程 · 癌症研究 · 纳米技术 · 药物递送系统
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SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY · 2025 · IF 4.6

Monitoring hepatic cysteine dynamics in obesity models with sulfur-substituted hemicyanine-based nanoprobes

Jing-Jing Qiao,Lu Fan,Jie-Li Zhou,Kai Wang

Cysteine (Cys) plays pivotal roles in redox homeostasis and metabolic regulation, with its dysregulation implicated in obesity-related hepatic disorders. Here, we developed a sulfur-substituted hemicyanine-based nanoprobe (Cys-NP) for photoacoustic imaging of hepatic Cys dynamics. The Cys-responsive molecular probe (Cys-MP) was encapsulated in mPEG-DSPE nanoparticles to overcome aqueous solubility limitations, yielding monodisperse nanoparticles with an average diameter of 28.7 nm and excellent colloidal stability. Sulfur substitution endowed the probe enhanced photoacoustic signals compared to oxygenated analogs, while selective Cys recognition triggered a bathochromic shift and yielded a detection limit of 0.13 μM. In high-fat-diet-induced obese mice, Cys-NP revealed significantly elevated hepatic Cys levels correlating with histopathological steatosis and hypercholesterolemia. This work establishes a nanotechnology-enabled strategy for mapping redox metabolism in metabolic diseases, offering both mechanistic insights and diagnostic potential.

研究领域: 纳米技术 · 分子成像 · 代谢性疾病 · 氧化还原生物学 · 生物医学工程
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