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Polydopamine-functionalized black phosphorus quantum dots for cancer theranostics
摘要： Black phosphorus (BP) is a promising theranostic agent owing to its excellent photothermal property, biocompatibility and biodegradability. However, the rapid degradation of BP with oxygen and moisture causes the innate instability that is the Achilles’ heel of BP, hindering its further applications in cancer theranostics. Herein, a facile surface passivation strategy was developed to prepare polydopamine (PDA) coated BP quantum dots (QDs) (denoted as BP@PDA) through self-polymerization method. PDA with enriched phenol groups plays as a scavenger of reactive oxygen, which can efficiently prevent the oxidation of BP quantum dots and make them much stable in water (～90% for BP@PDA vs. only 10% for pure BP QDs after 10 days storage). Furthermore, PDA with strong near-infrared (NIR) absorption could greatly improve the photothermal conversion efficiency (PCE) of BP QDs from 22.6% to 64.2% (～2.84-fold higher). Considering the excellent biodegradability and good biocompability of both BP QDs and PDA, the as-prepared BP@PDA hold great potential for cancer theranostics.
关键词： Photoacoustic imaging,Black phosphorus,Photothermal therapy,Cancer theranostics,Polydopamine
更新于2025-11-19 16:56:42
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CD146-Targeted Multimodal Image-Guided Photoimmunotherapy of Melanoma
摘要： For melanoma resistant to molecularly targeted therapy and immunotherapy, new treatment strategies are urgently needed. A molecularly targeted theranostic pair may thus be of importance, where the diagnostic probe facilitates patient stratification and the therapeutic companion treats the selected cases. For this purpose, flow cytometry is used to assess the CD146 level in melanoma cells. Based on YY146, a CD146-specific monoclonal antibody, an imaging probe 89Zr-Df-YY146 is synthesized and its diagnostic performance is evaluated by positron emission tomography (PET) imaging. Furthermore, a photoimmunotherapy (PIT) agent IR700-YY146 is developed and the therapeutic effect of IR700-YY146 PIT is assessed comprehensively. CD146 is highly expressed in A375 and SK-MEL-5 cells. 89Zr-Df-YY146 PET readily detects CD146-positive A375 melanomas. Tumor accumulation of 89Zr-Df-YY146 peaks at 72 h with an uptake value of 26.48 ± 3.28%ID g?1, whereas the highest uptake of the nonspecific 89Zr-Df-IgG is 4.80 ± 1.75%ID g?1. More importantly, IR700-YY146 PIT effectively inhibits the growth of A375 tumors, owing to production of reactive oxygen species, decreased glucose metabolism, and reduced expression of CD146. To conclude, 89Zr-Df-YY146 and IR700-YY146 are a promising theranostic pair with the former revealing CD146 expression in melanoma as a PET probe and the latter specifically treating CD146-positive melanoma as an effective PIT agent.
关键词： YY146,immunoPET,melanoma,photoimmunotherapy,theranostics
更新于2025-11-19 16:56:35
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New Magneto-Fluorescent Hybrid Polymer Nanogel for Theranostic Applications
摘要： Herein we have reported a new magneto-fluorescent nanogel built on photoluminescent co-macromer [PEG-maleic acid-glycine], N, N Dimethyl amino ethyl methacrylate and citrate capped superparamagnetic iron oxide nanoparticles (SPION). The nanogel was found to have core-shell morphology (SPION core and PEG shell) with particle size around 80 nm. The cytocompatibility of the synthesized nanogel studied using MTT, live dead assays and flow cytometry. The cellular uptake of the nanogel on cervical cancer cell line Hela evaluated through Prussian blue staining and fluorescence microscopy have revealed good cancer cell imaging capability. Magnetic hyperthermia experiments have shown that the synthesized nanogel caused the lysis of cancer cells. The fluorescence bio-imaging capability of the nanogel in murine model has shown good near IR imaging capability. Overall, the reported results suggest that the magneto-fluorescent nanogel shows promising future potential for cancer theranostic applications.
关键词： theranostics,Magneto-fluorescent,nanogel
更新于2025-09-23 15:23:52
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Stimuli-Responsive Nanotheranostics for Real-Time Monitoring Drug Release by Photoacoustic Imaging
摘要： Molecular photoacoustic imaging (PA) is a promising technology to understand tumor pathology and guide precision therapeutics. Despite the capability of activatable PA probes to image tumor-specific biomarkers, limitations in their molecular structure hamper them from effective drug delivery and the drug release monitoring. Herein, we developed a perylene diimide (PDI) based theranostic platform that provides noninvasive PA imaging signals to monitor tumor-specific pH-responsive drug release. Methods: we first designed and synthesized an acid-responsive amine-substituted PDI derivative. The pH sensitive properties of the PDI was demonstrated by density functional theory (DFT) calculations, UV-vis experiments and PA studies. The theranostic platform (THPDINs) was fabricated by self-assembly of the acid-responsive PDI, a pH irrelevant IR825 dye, and anti-cancer drug doxorubicin (DOX). The PA properties in various pH environment, drug delivery, cytotoxicity, cell uptake, ratiometric PA imaging and anti-tumor efficacy of the THPDINs were investigated in vitro and in vivo by using U87MG glioma cell line and U87MG tumor model. Results: We found that our designed PDI was sensitive to the tumor specific pH environment, reflected by absorbance shift, PA intensity and aggregation morphology changes in aqueous solution. The as-synthesized pH sensitive PDI acted as a molecular switch in the THPDINs, in which the switch can be triggered in the mild acidic tumor microenvironment to accelerate DOX release. Meanwhile, the DOX release could be monitored by ratiometric PA imaging. Conclusions: We developed a multifunctional PDI based theranostic platform for noninvasive real-time ratiometric PA imaging of tumor acidic pH and monitoring of drug release in living mice simultaneously. This strategy will shed light on the development of smart activatable theranostic nanoplatforms and will significantly advance the application of PA theranostics in biology and medicine.
关键词： photoacoustic imaging,drug delivery,pH-responsive,ratiometric imaging,theranostics
更新于2025-09-23 15:22:29
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Smart Supramolecular “Trojan Horse”-Inspired Nanogels for Realizing Light-Triggered Nuclear Drug Influx in Drug-Resistant Cancer Cells
摘要： Efficient nuclear delivery of anticancer drugs evading drug efflux transporters (DETs) on the plasma and nuclear membranes of multidrug-resistant cancer cells is highly challenging. Here, smart nanogels are designed via a one-step self-assembly of three functional components including a biocompatible copolymer, a fluorescent organosilica nanodot, and a photodegradable near-infrared (NIR) dye indocyanine green (ICG). The rationally designed nanogels have high drug encapsulation efficiency (≈99%) for anticancer drug doxorubicin (Dox), self-traceability for bioimaging, proper size for passive tumor targeting, prolonged blood circulation time for enhanced drug accumulation in tumor, and photocontrolled disassemblability. Moreover, the Dox-loaded nanogels can effectively kill multidrug-resistant cells via two steps: 1) They behave like a “Trojan horse” to escape from the DETs on the plasma membrane for efficiently transporting the anticancer “soldier” (Dox) into the cytoplasm and preventing the drugs from being excreted from the cells; 2) Upon NIR light irradiation, the photodegradation of ICG leads to the disassembly of the nanogels to release massive Dox molecules, which can evade the DETs on the nuclear membrane to exert their intranuclear efficacy in multidrug-resistant cells. Combined with their excellent biocompatibility, the nanogels may provide an alternative solution for overcoming cancer multidrug resistance.
关键词： nuclear delivery,photocontrollable drug release,cancer theranostics,silicon-based nanomaterials,supramolecular assembly
更新于2025-09-23 15:22:29
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PEGylated mesoporous Bi2S3 Nanostars loaded with Chlorin e6 and doxorubicin for fluorescence/CT imaging-guided multimodal therapy of Cancer
摘要： Taking advantage of the mesoporous structure of bismuth sulfide nanostars (Bi2S3 NSs), a chemotherapeutic drug of doxorubicin (DOX) and a photosensitizer of chlorin e6 (Ce6) were concurrently loaded in the PEGylated Bi2S3 NSs to formulate a multifunctional nanocomplex (BPDC NSs) for theranostics. BPDC NSs have excellent photothermal conversion efficiency and a capacity of yielding reactive oxygen species (ROS) upon laser irradiation, and can realize on-demand drug release by either pH-activation or thermal induction. Accumulation of the nanodrug could be monitored in real-time by infrared thermal imaging, fluorescence imaging and computed tomography (CT). More importantly, the combination effects of photothermal therapy (PTT), photodynamic therapy (PDT) and chemotherapy was demonstrated to dramatically suppress solid tumors without recurrence in vivo. Featured by the low systemic toxicity and high biocompatibility, this nanoplatform could be a promising derivative of Bi2S3 NSs for imaging-guided theranostics of cancer.
关键词： Controlled drug release,Cancer theranostics,Doxorubicin,Chlorin e6,Bismuth (Bi) chalcogenides
更新于2025-09-23 15:22:29
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Tracing Boron with Fluorescence and PET Imaging of Boronated Porphyrin Nanocomplex for Imaging Guided Boron Neutron Capture Therapy
摘要： Boron neutron capture therapy (BNCT) induces high-energy radiation within cancer cells while avoiding damage to normal cells that without uptake of BNCT drugs, which is holding great promise to provide excellent control over locally invasive malignant tumors. However, lack of quantitative imaging technique to determine local boron concentration has been a great challenge for nuclear physicians to apply accurate neutron irradiation during the treatment, which is a key factor that has limited BNCT’s application in clinics. To meet this challenge, this study describes coating boronated porphyrins with a biocompatible Poly(lactide–co-glycolide)–monomethoxy-poly(polyethylene-glycol) (PLGA-mPEG) micelle for selective tumor accumulation and reduced toxicity comparing with previously reported boronated porphyrin drugs. Fluorescence imaging and PET imaging were performed, unveiling the potential imaging properties of this boronated porphyrin nanocomplex (BPN) to locate tumor region and to determine tissue-localized boron concentration which facilitates treatment planning. By studying the pharmacokinetics of BPN with Cu-64 PET imaging, the treatment plan was adjusted from single bolus injection to multiple times of injections of smaller doses. As expected, high tumor uptake of boron (125.17±13.54 ppm) was achieved with an extraordinarily high tumor to normal tissue ratio: tumor to liver, muscle, fat and blood were 3.24±0.22, 61.46±20.26, 31.55±10.30 and 33.85±5.73, respectively. At last, neutron irradiation with BPN showed almost complete tumor suppression, demonstrating that BPN holds a great potential for being an efficient boron delivery agent for imaging-guided BNCT.
关键词： copper-64,boron neutron capture therapy,theranostics,positron emission tomography,micelle
更新于2025-09-23 15:21:21
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Self-assembly of porphyrin-grafted lipid into nanoparticles encapsulating doxorubicin for synergistic chemo-photodynamic therapy and fluorescence imaging
摘要： The limited clinical efficacy of monotherapies in the clinic has urged the development of novel combination platforms. Taking advantage of light-triggered photodynamic treatment combined together with the controlled release of nanomedicine, it has been possible to treat cancer without eliciting any adverse effects. However, the challenges imposed by limited drug loading capacity and complex synthesis process of organic nanoparticles (NPs) have seriously impeded advances in chemo-photodynamic combination therapy. In this experiment, we utilize our previously synthesized porphyrin-grafted lipid (PGL) NPs to load highly effective chemotherapeutic drug, doxorubicin (DOX) for synergistic chemo-photodynamic therapy.
关键词： photodynamic therapy,doxorubicin,theranostics,chemotherapy,porphyrin
更新于2025-09-23 15:21:21
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Integrin α <sub/>γ</sub> β <sub/>3</sub> -targeted [ <sup>64</sup> Cu]CuS Nanoparticles for PET/CT Imaging and Photothermal Ablation Therapy
摘要： Copper sulfide (CuS) nanoparticles have been considered one of the most clinical relevant nanosystems because of their straightforward chemistry, small particle size, low toxicity, and intrinsic theranostic characteristics. In our previous studies, radioactive [64Cu]CuS nanoparticles were successfully developed to be used as efficient radiotracers for positron emission tomography and for photothermal ablation therapy of cancer cells using near-infrared laser irradiation. However, the major challenge of CuS nanoparticles as a theranostic platform is the lack of a means for effective targeted delivery to the tumor site. To overcome this challenge, we designed and synthesized angiogenesis-targeting [64Cu]CuS nanoparticles, which are coupled with cyclic RGDfK peptide [c(RGDfK)] through polyethylene glycol (PEG) linkers using click chemistry. In assessing their tumor-targeting efficacy, we found that the tumor uptakes of [64Cu]CuS-PEG-c(RGDfK) nanoparticles at 24 h after intravenous injection were significantly greater (8.6%±1.4% injected dose/gram of tissue) than those of nontargeted [64Cu]CuS-PEG nanoparticles (4.3%±1.2% injected dose/gram of tissue, p < 0.05). Irradiation of tumors in mice administered [64Cu]CuS-PEG-c(RGDfK) nanoparticles induced 98.7% necrotic areas. In contrast, irradiation of tumors in mice administered non-targeted CuS-PEG nanoparticles induced 59% necrotic areas (p < 0.05). The angiogenesis-targeting [64Cu]CuS nanoparticles may serve as a promising platform for image-guided ablation therapy with high efficacy and minimal side effects in future clinical translation of this novel class of multifunctional nanomaterials.
关键词： PET/CT imaging,RGD peptide,Copper sulfide nanoparticles,photothermal ablation therapy,integrin αvβ3,theranostics
更新于2025-09-23 15:21:21
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<sup>86/90</sup> Y-Labeled Monoclonal Antibody Targeting Tissue Factor for Pancreatic Cancer Theranostics
摘要： Pancreatic cancer is highly aggressive, with a median survival time of less than 6 months and a 5-year overall survival rate of around 7%. The poor prognosis of PaCa is largely due to its advanced stage at diagnosis and the lack of efficient therapeutic options. Thus, the development of an efficient, multifunctional PaCa theranostic system is urgently needed. Overexpression of tissue factor (TF) has been associated with increased tumor growth, angiogenesis, and metastasis in many malignancies, including pancreatic cancer. Herein, we propose the use of a TF-targeted monoclonal antibody (ALT836) conjugated with the pair 86/90Y as a theranostic agent against pancreatic cancer. For methods, serial PET imaging with 86Y-DTPA-ALT836 was conducted to map the biodistribution the tracer in BXPC-3 tumor-bearing mice. 90Y-DTPA-ALT836 was employed as a therapeutic agent that also allowed tumor burden monitoring through Cherenkov luminescence imaging. The results were that the uptake of 86Y-DTPA-ALT836 in BXPC-3 xenograft tumors was high and increased over time up to 48 h postinjection (p.i.), corroborated through ex vivo biodistribution studies and further confirmed by Cherenkov luminescence Imaging. In therapeutic studies, 90Y-DTPA-ALT836 was found to slow tumor growth relative to the control groups and had significantly smaller (p < 0.05) tumor volumes 1 day p.i. Histological analysis of ex vivo tissues revealed significant damage to the treated tumors. The conclusion is that the use of the 86/90Y theranostic pair allows PET imaging with excellent tumor-to-background contrast and treatment of TF-expressing pancreatic tumors with promising therapeutic outcomes.
关键词： pancreatic cancer,yttrium-86,radioimmunotherapy,tissue factor,yttrium-90,theranostics,positron emission tomography (PET)
更新于2025-09-23 15:21:01