Cancer Theranostic Agents Research Articles

Upconversion and NIR-II luminescent rare earth nanoparticles combined with machine learning for cancer theranostics.

How to develop contrast agents for cancer theranostics is a meaningful and challenging endeavor, and rare earth nanoparticles (RENPs) may provide a possible solution. In this study, we initially modified RENPs through the application of photodynamic agents (ZnPc) and targeted the bevacizumab antibody for cancer theranostics, which was aimed at improving the therapeutic targeting and efficacy. Subsequently, we amalgamated anthocyanin with the modified RENPs, creating a potential cancer diagnosis platform. When the spectral data were obtained from the composite of cells, the crucial information was extracted through a competitive adaptive reweighted sampling feature algorithm. Then, we employed a machine learning classification model and classified both the individual spectral data and fused spectral data to accurately predict distinctions between breast cancer and normal tissue. The results indicate that the amalgamation of fusion techniques with machine learning algorithms provides highly precise predictions for molecular-level breast cancer detection. Finally, in vitro and in vivo experiments were carried out to validate the near-infrared luminescence and therapeutic effectiveness of the modified nanomedicine. This research not only underscores the targeted effects of nanomedicine but also demonstrates the potent synergy between optical spectral technology and machine learning. This innovative approach offers a comprehensive strategy for the integrated treatment of breast cancer.

Synthesis, in silico and biodistribution studies of a novel 47Sc-radiolabeled α-amino acid ester derivative attached to pyrazine and tetrazole rings for tumor targeted radiotherapy

Abstract Recently, tumor-targeted radionuclide therapy has gained much recognition for the treatment of metastasized cancer. There is a growing interest in using the theranostic radionuclide 47Sc, owing to its excellent chemical and nuclear properties. However, the available chelating agents require a relatively high temperature for their radiolabeling, which could denature biomolecules. The aim of the present study is to synthesize a dipeptide agent that forms a thermodynamically more stable complex with 47Sc at room temperature. A novel α-amino acid ester derivative attached to pyrazine and tetrazole heterocyclic rings has been prepared by the azide coupling method. Different spectroscopic methods (FT-IR, 1H NMR, and mass spectra) were used for characterization of the target compound. The newly synthesized dipeptide was radiolabeled with 47Sc, and a high radiochemical yield of 98.5 ± 1.5 % and in vitro serum stability up to 72 h were attained at room temperature within 20 min. The quantum chemical calculations at B3PW91/6-31G(d) level were employed to establish the molecular structure of the dipeptide and its complexation with 47Sc. The selectivity of 47Sc-dipeptide toward localization in tumor cells was performed by molecular docking on different receptors in addition to in vivo biodistribution on solid tumor-bearing mice. A high T/NT ratio of 8.16 was obtained after 4 h p.i, suggesting that this complex could be used as a potential cancer theranostic agent.

Preclinical Toxicity Assessment of Ti‐Based MXene Nanomaterials for Advanced Theranostic Applications

AbstractMXene, a novel class of 2D materials, has garnered widespread attention from researchers worldwide due to its remarkable physicochemical properties. Its exceptional physical, chemical, optical, and electronic characteristics have opened up exciting possibilities for its application in biomedical fields. The easily modifiable surface makes it particularly attractive to be used in nanomedicine as the surface can be made hydrophilic, with facile drug loading, for imaging, anti‐microbial, and photothermal applications. To fully harness its potential in the biomedical field, a comprehensive understanding of its toxicological effect is of utmost importance. This review presents a concise introduction to MXene, encompassing commonly employed synthesis procedures, followed by an in‐depth exploration of biomedical studies conducted on diverse MAX and MXene phases. The use of MXene has been discussed as a cancer theranostic agent followed by its toxicity evaluation in microorganisms, zebrafish, in vitro, and in vivo toxicity. Additionally, the review emphasizes the need to advance and standardize the toxicity study. This review provides an overview on the various toxicological aspects related to the MXene nanostructures and advocates their utilization in the near future.

Cytotoxicity of Laser-Synthesized Nanoparticles of Elemental Bismuth.

High X-ray absorption combined with photothermal properties make bismuth nanoparticles (Bi NP) a promising agent for multimodal cancer theranostics. However, the synthesis of Bi NP by the "classical" chemical methods has numerous limitations, including potential toxicity of the produced nanomaterials. Here we studied in vitro toxicity of laser-synthesized Bi NP coated with Pluronic F-127 on mouse fibroblast cell line L929. The survival of L929 cells decreased linearly with increasing the concentration of Bi NP in a concentration range of 3-500 μg/ml; the LC50 value was 57 μg/ml. The unique combination of functional properties and moderate toxicity of the laser-synthesized Bi NP makes them a new promising platform for sensitization of multimodal cancer theranostics.

DNA-Targeted Complexes of Tc and Re for Biomedical Applications.

Due to their favorable chemical features, Re and Tc complexes have been widely used for the development of new therapeutic agents and imaging probes to solve problems of biomedical relevance. This review provides an update of the most relevant research efforts towards the development of novel cancer theranostic agents using Re and Tc-based compounds interacting with specific DNA structures. This includes a variety of homometallic complexes, namely those containing M(CO)3 (M=Re, Tc) moieties, that exhibit different modes of interaction with DNA, such as covalent binding, intercalation, groove binding or G-quadruplex DNA binding. Additionally, heterometallic complexes, designed to potentiate synergistic effects of different metal centers to improve DNA-targeting, cytotoxicity and fluorescence properties, are also reviewed. Particular attention is also given to 99m Tc- and 188 Re-labeled oligonucleotides that have been widely explored to develop imaging and therapeutic radiopharmaceuticals through the in vivo hybridization with a specific complementary DNA or RNA target sequence to provide useful molecular tools in precision medicine for cancer diagnosis and treatment. Finally, the need for further improvement of DNA-targeted Re and Tc-based compounds as potential therapeutic and diagnostic agents is highlighted, and future directions are discussed.

Embedding Atomically Dispersed Manganese/Gadolinium Dual Sites in Oxygen Vacancy-Enriched Biodegradable Bimetallic Silicate Nanoplatform for Potentiating Catalytic Therapy.

Due to their atomically dispersed active centers, single-atom nanozymes (SAzymes) have unparalleled advantages in cancer catalytic therapy. Here, loaded with chlorin e6 (Ce6), a hydrothermally mass-produced bimetallic silicate-based nanoplatforms with atomically dispersed manganese/gadolinium (Mn/Gd) dual sites and oxygen vacancies (OVs) (PMnSA GMSNs-V@Ce6) is constructed for tumor glutathione (GSH)-triggered chemodynamic therapy (CDT) and O2 -alleviated photodynamic therapy. The band gaps of silica are significantly reduced from 2.78 to 1.88eV by doping with metal ions, which enables it to be excited by a 650nm laser to produce electron-hole pairs, thereby facilitating the generation of reactive oxygen species. The Gd sites can modulate the local electrons of the atom-catalyzed Mn sites, which contribute to the generation of superoxide and hydroxyl radicals (• OH). Tumor GSH-triggered Mn2+ release can convert endogenous H2 O2 to • OH and realize GSH-depletion-enhanced CDT. Significantly, the hydrothermally generated OVs can not only capture Mn and Gd atoms to form atomic sites but also can elongate and weaken the O-O bonds of H2 O2 , thereby improving the efficacy of Fenton reactions. The degraded Mn2+ /Gd3+ ions can be used as tumor-specific magnetic resonance imaging contrast agents. All the experimental results demonstrate the great potential of PMnSA GMSNs-V@Ce6 as cancer theranostic agent.

Accelerator production, radiochemical separation and nanoradiopharmaceutical formulation using 69Ge: A next generation PET probe

Positron emission tomography (PET) has revolutionized the field of molecular imaging of cancer. The driving forces in the latest resurgence of PET are the advances in nano-oncology and availability of newer radioisotopes with attractive nuclear decay characteristics. Germanium-69 (69Ge; T½ = 39 h, 21 % β+, Emax = 1205 keV) is one such radioisotope whose potential is yet to be fully explored for PET imaging. The adequately long half-life of 69Ge, makes it an ideal choice for PET imaging using radiolabeled nanoformulations, which are expected to circulate for a relatively longer time in the biological system. In this study, we report the production of 69Ge via 69Ga (p, n) 69Ge reaction using natural Ga2O3 target. A facile radiochemical separation method based on selective precipitation of Ga at pH ∼7 was developed for isolating no-carrier-added (NCA) 69Ge from the irradiated target in a form suitable for in vivo animal studies. A chelator-free approach was optimized for radiolabeling superparamagnetic arginine grafted iron oxide nanoparticles (AMNPs) with 69Ge for potential use in dual modality PET/magnetic resonance imaging (MRI) and magnetic hyperthermia therapy of cancer. The radiolabeling yield of 69Ge-AMNPs was >95 % and the radiolabeled nanoformulation was stable even after 72 h. As a proof of concept, the suitability of the radiolabeled nanoformulation for in vivo PET imaging was demonstrated in Wistar rats. Overall, this strategy of production, radiochemical separation and radiopharmaceutical formulation might aid towards development of potent agents for cancer theranostics.

Bioinspired theranostic quantum dots: Paving the road to a new paradigm for cancer diagnosis and therapeutics

Despite extensive research, a complete cure remains lacking for most types of cancer. Nanotechnology-based carriers, such as liposomes, nanoparticles (NPs), dendrimers, nanoemulsions, and other nanocarriers, can target cancer cells, but their in vivo fate is unpredictable. Bioinspired quantum dots (BQDs) offer enhanced aqueous solubility, exceptionally low toxicity, biocompatibility, easy biofunctionalization, and selective cancer targeting. Due to their photoluminescence, high longitudinal relaxation value, photothermal effect upon laser irradiation, generation of singlet oxygen, and production of H2S for gas therapy, BQDs are excellent cancer theranostic agents. In this review, we highlight the theranostic application of, and existing challenges relating to BQDs.

Baicalin functionalized PEI-heparin carbon dots as cancer theranostic agent

The worldwide prevalence of cancer and its significantly rising risks with age have garnered the attention of nanotechnology for prompt detection and effective therapy with minimal or no adverse effects. In the current study, heparin (HP) polymer derived heteroatom (N, S-) co-doped CDs were synthesized using hydrothermal synthesis method to efficiently deliver natural anticancer compound baicalin (BA). Heparin carbon dots (HCDs) were passivated with polyethylenimine (PEI) to improve its fluorescence quantum yield. The surface passivation of CDs by polycationic PEI polymer not only facilitated loading of BA, but also played a crucial role in the pH-responsive drug delivery. The sustained release of BA (up to 80 %) in mildly acidic pH (5.5 and 6.5) conditions endorsed its drug delivery potential for cancer-specific microenvironments. BA-loaded PHCDs exhibited enhanced anticancer activity as compared to BA/PHCDs indicating the effectiveness of the nanoformulation, Furthermore, the flow cytometry analysis confirmed that BA-PHCDs treated cells were arrested in the G2/M phase of cell cycle and had a higher potential for apoptosis. Bioimaging study demonstrated the excellent cell penetration efficiency of PHCDs with complete cytoplasmic localization. All this evidence comprehensively demonstrates the potency of BA-loaded PHCDs as a nanotheranostic agent for cancer.

Design of One-for-All Near-Infrared Aggregation-Induced Emission Nanoaggregates for Boosting Theranostic Efficacy.

Fluorescence-guided phototherapy, including photodynamic and photothermal therapy, is considered an emerging noninvasive strategy for cancer treatments. Organic molecules are promising theranostic agents because of their facile construction, simple modification, and good biocompatibility. Organic systems that integrated multifunctionalities in a single component and achieved high efficiency in both imaging and therapies are rarely reported as the inherently competitive energy relaxation pathways are hard to modulate, and fluorescence quenching occurs upon molecular aggregation. Herein, a versatile theranostic platform with near-infrared emission, high fluorescence quantum yield, robust reactive oxygen species production, and excellent photothermal conversion efficiency was developed based on an aggregation-induced emission luminogen, namely, TPA-TBT. In vivo studies revealed that the TPA-TBT nanoaggregates exhibit outstanding photodynamic and photothermal therapy efficacy to ablate tumors inoculated in a mouse model. This work offers a design strategy to develop one-for-all cancer theranostic agents by modulating and utilizing the relaxation energy of excitons in full.

Bimetallic Hyaluronate-Modified Au@Pt Nanoparticles for Noninvasive Photoacoustic Imaging and Photothermal Therapy of Skin Cancer.

Although spherical gold (Au) nanoparticles have remarkable photothermal conversion efficiency and photostability, their weak absorption in the near-infrared (NIR) region and poor penetration into deep tissues have limited further applications to NIR light-mediated photoacoustic (PA) imaging and noninvasive photothermal cancer therapy. Here, we developed bimetallic hyaluronate-modified Au-platinum (HA-Au@Pt) nanoparticles for noninvasive cancer theranostics by NIR light-mediated PA imaging and photothermal therapy (PTT). The growth of Pt nanodots on the surface of spherical Au nanoparticles enhanced the absorbance in the NIR region and broadened the absorption bandwidth of HA-Au@Pt nanoparticles by the surface plasmon resonance (SPR) coupling effect. In addition, HA facilitated the transdermal delivery of HA-Au@Pt nanoparticles through the skin barrier and enabled clear tumor-targeted PA imaging. Compared to conventional PTT via injection, HA-Au@Pt nanoparticles were noninvasively delivered into deep tumor tissues and completely ablated the targeted tumor tissues by NIR light irradiation. Taken together, we could confirm the feasibility of HA-Au@Pt nanoparticles as a NIR light-mediated biophotonic agent for noninvasive skin cancer theranostics.

Recent Applications of Titanium Dioxide Nanoparticles as Cancer Theranostic Agents

In medicine, the application of nanotechnology is related to the use of nanoscale materials to improve and develop new diagnostic and therapeutic methods. Due to the unique physicochemical and optical characteristics of titanium dioxide nanoparticles (TiO2 NPs), such as high biocompatibility, surface properties, and relative stability, they have been widely investigated for medical purposes, particularly as a theranostic agent in cancer diagnosis and treatment. This review concentrates on current progress in the applications of TiO2 nanostructures in cancer diagnosis and treatment domains. Studies have shown that TiO2 NPs can be promising in various medical imaging techniques. In the field of cancer treatment, researchers have evaluated the ability of TiO2 NPs in up-to-date therapeutic approaches, including drug delivery, sonodynamic, photodynamic, photothermal, and ionizing radiation therapies. In the current review, we focus on the ability of TiO2 NPS as a radiation sensitizer to improve the efficiency of cancer diagnosis and treatment. Finally, according to the studies that have been conducted on controlling and optimizing the factors involved in the TiO2 NP radiosensitization, the mechanism of TiO2 NPs in producing the radiosensitivity effect has been discussed.

Polyethyleneimine-Based Drug Delivery Systems for Cancer Theranostics.

With the development of nanotechnology, various types of polymer-based drug delivery systems have been designed for biomedical applications. Polymer-based drug delivery systems with desirable biocompatibility can be efficiently delivered to tumor sites with passive or targeted effects and combined with other therapeutic and imaging agents for cancer theranostics. As an effective vehicle for drug and gene delivery, polyethyleneimine (PEI) has been extensively studied due to its rich surface amines and excellent water solubility. In this work, we summarize the surface modifications of PEI to enhance biocompatibility and functionalization. Additionally, the synthesis of PEI-based nanoparticles is discussed. We further review the applications of PEI-based drug delivery systems in cancer treatment, cancer imaging, and cancer theranostics. Finally, we thoroughly consider the outlook and challenges relating to PEI-based drug delivery systems.

Albumin-templated platinum (II) sulfide nanodots for size-dependent cancer theranostics

Transition-metal chalcogenides, such as noble metal chalcogenides, hold tremendous potential as efficient agents for photo-induced cancer theranostics due to their unique physicochemical properties. However, a critical bottleneck still lies in exploring simple and controllable methods to synthesize noble metal chalcogenides especially PtS for in vivo photo-induced cancer imaging and simultaneous therapy. Herein, we proposed the albumin-templated synthesis of size-controllable platinum (II) sulfide nanodots (PtS-NDs) for multimodal cancer imaging and potent photothermal therapy. PtS-NDs were precisely synthesized with a tunable size ranging from 2.1 nm to 4.5 nm through a thermodynamically controlled growth inside albumin nanocages. PtS-NDs yielded significant near-infrared (NIR) absorbance and outstanding photothermal conversion under NIR laser irradiation, as well as effective resistance to photobleaching, thereby generating remarkable in vivo photoacoustic signals and distinct hyperthermia at tumor site. Moreover, these nanodots possessed efficient cellular uptake and tumor targeting capabilities in a size-dependent manner, thus leading to controllable diagnostic and thermo-therapeutic efficacy. Specifically, PtS-NDs with core diameter of 4.5 nm displayed preferable in vivo photoacoustic and CT imaging with high sensitivity, spatially and anatomically enhanced imaging contrast, together with hyperthermia mediated tumor ablation. Thus, the albumin-templated biomimetic synthesis provided an insightful strategy on fabricating theranostic PtS-NDs for potential clinical applications. Statement of significanceNoble metal chalcogenides especially PtS are of particular importance in the field of precise nanomedicine to improve both accuracy of cancer diagnosis and efficiency of tumor treatment. However, the intensively preclinical investigation of PtS was limited due to the lack of simple and controllable synthetic methods. Here, we report an albumin-templated biomineralization synthesis of platinum (II) sulfide nanodots (PtS-NDs). Specifically, albumin-templated biomineralization of PtS-NDs was induced by the electrostatic interactions between albumin and Pt2+, followed by the nucleation and growth inside the albumin nanocages. The resulting PtS-NDs showed good dispersibility and biosafety, as well as size-dependent photophysical properties and biological behaviors. Therefore, albumin-based biomineralization is a promising and safe strategy to facilely fabricate Pt-based chalcogenide for tumor theranostics.

Multifunctional croconaine nanoparticles for efficient optoacoustic imaging of deep tumors and photothermal therapy

Abstract The proper design of near-infrared light-absorbing agents enables efficient optoacoustic imaging-guided phototherapy. In particular, several croconaine-based organic agents with excellent optical properties have been recently reported for this purpose. However, most of them absorb light below 800 nm, limiting deep-tissue imaging applications. To this end, we utilized a recently described novel croconaine derivative (CR880) to develop CR880-based nanoparticles (CR880-NPs) for effective in vivo delivery, deep tissue optoacoustic imaging and photothermal therapy applications. Radicals and strong π–π stacking in CR880 result in an 880 nm absorption peak with no blue-shift upon condensing to the solid phase. DSPE-PEG2000-formulated CR880-NPs exhibited high optoacoustic generation efficiency and photostability, and could be visualized in the tumors of three different mouse tumor models (breast, brain, and colon tumor) with high image contrast. The high photothermal conversion efficiency of CR880-NPs (∼58%) subsequently enabled efficient in vivo tumor elimination using a low energy laser, while remaining biocompatible and well-tolerated. This work introduces a promising novel agent for cancer theranostics of challenging deep-seated tumors.

Rational surface modification of gadolinium borate nanoparticles enhancing colloidal stability in physiological media for potential neutron capture therapy and magnetic resonance imaging

Colloidal stability of nanomaterials in physiological media is an indispensable property for their biomedical applications. However, gadolinium borate (GdBO3) nanoparticles that hold promise as a theranostic agent for neutron capture therapy (NCT) and magnetic resonance imaging (MRI) of cancer tend to precipitate in phosphate buffered saline (PBS) owing to formation of insoluble gadolinium phosphate. To address this issue, in this work 10B-enriched GdBO3 nanoparticles were prepared and coated with mesoporous silica (mSiO2) of ~ 40 nm in thickness and subsequently grafted with hydrophilic polyglycerol (PG). The resulting GdBO3 @mSiO2-PG nanoparticles showed excellent colloidal stability in PBS due to the protection of the mSiO2 coating as well as superior dispersibility because of the high hydrophilicity of the PG layer. In vitro experiments revealed that GdBO3 @mSiO2-PG possessed low cytotoxicity and could be taken up by cancer cells in a concentration-dependent manner. In vivo studies indicated that GdBO3 @mSiO2-PG can circulate in mouse body for a considerably long time without obvious acute toxicity. In addition, GdBO3 @mSiO2-PG also showed promise as a T1-weighted MRI contrast agent with a proton longitudinal relaxivity of 0.67 mM−1 s−1. Our results indicate that GdBO3 @mSiO2-PG with enhanced colloidal stability in physiological media could serve as a promising multifunctional agent for cancer theranostics.

Novel seven-membered ring-fused naphthalimide derivatives with potentials for cancer theranostics

Naphthalimide derivatives have good planarity and large conjugated structure and therefore possess photophysical properties and biological activities. Previously, our group discovered seven-membered heterocyclic derivatives via modifying 4- and 5-positions of naphthalimide skeleton and found the derivatives had good water solubility and showed large stokes shift and strong fluorescence in water. In this article, we designed and synthesized more seven-membered ring-fused naphthalimide derivatives (Y1-Y16) by introducing different substitutions on the imide group. Among them, Y1, Y5, Y9 were found to show similar cytotoxic activities with Amonafide against A549 and HL60 cells, with IC50 values at 10−6 mol/L. What is more, the asymmetry derivatives (Y1 and Y5) showed high fluorescent quantum yields in the aqueous phase (Ф = 0.47). Considering the great fluorescence quantum yields in water and the potent anti-tumor activities of the representative seven-membered ring-fused naphthalimides, they have potentials to be used as agents for cancer theranostics.

Immune Checkpoint Inhibitor-Mediated Cancer Theranostics with Radiolabeled Anti-Granzyme B Peptide.

Although immune checkpoint inhibitors (ICI) have revolutionized cancer management, patient response can be heterogeneous, and the development of ICI resistance is increasingly reported. Novel treatment strategies are necessary not only to expand the use of ICI to previously unresponsive tumor types but also to overcome resistance. Targeted radionuclide therapy may synergize well with ICIs since it can promote a pro-inflammatory tumor microenvironment. We investigated the use of a granzyme B targeted peptide (GZP) as a cancer theranostic agent, radiolabeled with 68Ga (68Ga-GZP) as a PET imaging agent and radiolabeled with 90Y (90Y-GZP) as a targeted radionuclide therapy agent for combinational therapy with ICI in murine models of colon cancer. Our results demonstrate that GZP increasingly accumulates in tumor tissue after ICI and that the combination of ICI with 90Y-GZP promotes a dose-dependent response, achieving curative response in some settings and increased overall survival.

Porphyrin NanoMetal-Organic Frameworks as Cancer Theranostic Agents.

Metal-Organic Frameworks (MOFs) are hybrid multifunctional platforms that have found remarkable applications in cancer treatment and diagnostics. Independently, these materials can be employed in cancer treatment as intelligent drug carriers in chemotherapy, photothermal therapy, and photodynamic therapy; conversely, MOFs can further be used as diagnostic tools in fluorescence imaging, magnetic resonance imaging, computed tomography imaging, and photoacoustic imaging. One essential property of these materials is their great ability to fine-tune their composition toward a specific application by way of a judicious choice of the starting building materials (metal nodes and organic ligands). Moreover, many advancements were made concerning the preparation of these materials, including the ability to downsize the crystallites yielding nanoporous porphyrin MOFs (NMOFs) which are of great interest for clinical treatment and diagnostic theranostic tools. The usage of porphyrins as ligands allows a high degree of multifunctionality. Historically these molecules are well known for their reactive oxygen species formation and strong fluorescence characteristics, and both have proved helpful in cancer treatment and diagnostic tools. The anticipation that porphyrins in MOFs could prompt the resulting materials to multifunctional theranostic platforms is a reality nowadays with a series of remarkable and ground-breaking reports available in the literature. This is particularly remarkable in the last five years, when the scientific community witnessed rapid development in porphyrin MOFs theranostic agents through the development of imaging technologies and treatment strategies for cancer. This manuscript reviews the most relevant recent results and achievements in this particular area of interest in MOF chemistry and application.

Synchronously boosting type-I photodynamic and photothermal efficacies via molecular manipulation for pancreatic cancer theranostics in the NIR-II window

In view of the fact that pancreatic cancer, called as the king of cancer, is one of the most lethal malignancies, exploring effective technologies for pancreatic cancer diagnosis and therapy remains an appealing yet significantly challenging task. Phototheranostics has recently received considerable attention by virtue of its various distinctive advantages. However, the limited penetration depth, strong oxygen-dependence and high heat shock protein-inhibition of conventional phototheranostic materials severely hamper their overall theranostic efficacy, especially for deep-seated hypoxia tumors, such as pancreatic tumor. In this study, an aggregation-induced emission (AIE)-featured photosensitizer, namely DCTBT, synchronously sharing NIR-II fluorescence imaging (FLI), diminished oxygen-dependent type-I photodynamic therapy (PDT) and high-efficiency photothermal therapy (PTT) functions was subtly constructed by molecular engineering. With the aid of an EGFR-targeting-peptide-modified amphiphilic polymer, the as-prepared DCTBT-loaded liposomes is capable of effectively accumulating at and visualizing pancreatic tumor, as well as significantly suppressing the tumor growth on both subcutaneous and orthotopic PANC-1 tumor mice models. This study thus brings useful insights into designing the next generation of cancer theranostic agents for potential clinical applications.