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ZnO Quantum Dots Modified by pH-Activated Charge-Reversal Polymer for Tumor Targeted Drug Delivery
摘要： In this paper, we reported a pH responsive nano drug delivery system (NDDS) based on ZnO quantum dots (QDs) for controlled release of drugs. Zwitterionic poly(carboxybetaine methacrylate) (PCBMA) and poly(2-(dimethylamino) ethyl methacrylate) (PDMAEMA) were introduced to modify ZnO QDs, which can help enhance water stability, increase blood circulation time, and promote endocytosis. After tuning of PCBMA/PDMAEMA ratios, the ZnO@P(CBMA-co-DMAEMA) nanoplatform shows a sensitive switch from strong protein adsorption resistance (with negatively charged surface) at physiological pH to strong adhesion to tumor cell membranes (with positively charged surface) at the slightly acidic extracellular pH of tumors. Anti-cancer drug, Doxorubicin (DOX), molecules were demonstrated to be successfully loaded to ZnO@P(CBMA-co-DMAEMA) with a relatively large drug loading content (24.6%). In addition, ZnO@P(CBMA-co-DMAEMA) loaded with DOX can achieve lysosomal acid degradation and release of DOX after endocytosis by tumor cells, resulting in synergistic treatment of cancer, which is attributed to a combination of the anticancer effect of Zn2+ and DOX.
关键词： Zinc oxide quantum dots (ZnO QDs),poly(2-(dimethylamino) ethyl methacrylate) (PDMAEMA),drug delivery,poly(carboxybetaine methacrylate) (PCBMA)
更新于2025-09-10 09:29:36
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Doxorubicin-loaded protease-activated near-infrared fluorescent polymeric nanoparticles for imaging and therapy of cancer
摘要： Despite significant progress in the field of oncology, cancer remains one of the leading causes of death. Chemotherapy is one of the most common treatment options for cancer patients but is well known to result in off-target toxicity. Theranostic nanomedicines that integrate diagnostic and therapeutic functions within an all-in-one platform can increase tumor selectivity for more effective chemotherapy and aid in diagnosis and monitoring of therapeutic responses. Material and methods: In this work, theranostic nanoparticles were synthesized with commonly used biocompatible and biodegradable polymers and used as cancer contrast and therapeutic agents for optical imaging and treatment of breast cancer. These core–shell nanoparticles were prepared by nanoprecipitation of blends of the biodegradable and biocompatible amphiphilic copolymers poly(lactic-co-glycolic acid)-b-poly-l-lysine and poly(lactic acid)-b-poly(ethylene glycol). Poly-l-lysine in the first copolymer was covalently decorated with near-infrared fluorescent Alexa Fluor 750 molecules. Results: The spherical nanoparticles had an average size of 60–80 nm. The chemotherapeutic drug doxorubicin was encapsulated in the core of nanoparticles at a loading of 3% (w:w) and controllably released over a period of 30 days. A 33-fold increase in near-infrared fluorescence, mediated by protease-mediated cleavage of the Alexa Fluor 750-labeled poly-l-lysine on the surface of the nanoparticles, was observed upon interaction with the model protease trypsin. The cytocompatibility of drug-free nanoparticles and growth inhibition of drug-loaded nanoparticles on MDA-MB-231 breast cancer cells were investigated with a luminescence cell-viability assay. Drug-free nanoparticles were found to cause minimal toxicity, even at high concentrations (0.2–2,000 μg/mL), while doxorubicin-loaded nanoparticles significantly reduced cell viability at drug concentrations .10 μM. Finally, the interaction of the nanoparticles with breast cancer cells was studied utilizing fluorescence microscopy, demonstrating the potential of the nanoparticles to act as near-infrared fluorescence optical imaging agents and drug-delivery carriers. Conclusion: Doxorubicin-loaded, enzymatically activatable nanoparticles of less than 100 nm were prepared successfully by nanoprecipitation of copolymer blends. These nanoparticles were found to be suitable as controlled drug delivery systems and contrast agents for imaging of cancer cells.
关键词： enzymatic activation,nanoprecipitation,theranostics,PEG,poly-l-lysine,PLGA,block copolymers,nanomedicine,fluorescence imaging,drug delivery,nanoparticles,PLA
更新于2025-09-10 09:29:36
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Redox Responsive Fluorescent nanoparticles based on Diselenide-containing AIEgens for Cell imaging and Selective Cancer Therapy
摘要： A fluorescent molecule diselenide-containing 9, 10-distyrylanthracene (DSA) derivative (SeDSA) with aggregation induced emission (AIE) characteristic was successfully synthesized and SeDSA nanoparticles (NPs) were prepared through nanoprecipitation method. SeDSA could coassemble with the antitumor prodrug, diselenide-containing paclitaxel (SePTX) which could be obtained by precipitation, to form SeDSA-SePTX Co-NPs (Co-NPs). Molecular dynamics (MD) simulations reveal that the driving forces for the self-assembly behaviors of SeDSA NPs and SePTX NPs are π-π interactions and hydrophobic interactions, respectively. While the driving forces for Co-NPs include hydrophobic interactions between SeDSA and SePTX, π-π interactions between SeDSA molecules and hydrophobic interactions between SePTX molecules. Meanwhile, Se-Se bonds play a crucial role in balancing the intramolecular forces. These diselenide-containing nanoparticles (SeDSA NPs, SePTX NPs and Co-NPs) exhibit high stability in physiological conditions and excellent reduction-sensitivity under redox agent glutathione (GSH) because of the selenium-sulfur exchange reaction between diselenide and GSH. Both SeDSA NPs and Co-NPs show strong orange fluorescence emissions on the account of the AIE feature of SeDSA and they were easily internalized by HeLa and HepG2 cells. Distinctively, the Co-NPs combine the advantage of SeDSA and SePTX for cell imaging and antineoplastic activity and exhibit selectivity of cytotoxicities between neoplasia cells and normal cells. It highlights developing diselenide-containing AIEgens as a unique approach to prepare uniform and stable fluorescent nanoparticles for the application in cell imaging and tumor treatment.
关键词： AIEgens,drug delivery,diselenide bond,self-assembly,bioimaging
更新于2025-09-10 09:29:36
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Hybrid Nanostructures for Cancer Theranostics || Nanostructures for Externally Triggered Chemo/Thermal Therapies
摘要： Cancer is the most common cause of death globally despite improvement in early detection, life-style changes, and advances in radiotherapy, immunotherapy, chemotherapy, and molecular medicine. The American Cancer Society estimated 1,688,780 cases of cancer and 600,920 deaths in the USA in 2017 alone. Problems with current therapies include: invasive procedures, systemic side effects from the nonspecific nature of chemotherapy drugs, and drug-resistant tumors. In addition to limited efficacy, the side effects of current treatments include anemia, bleeding or clotting, loss of bone density, bowel dysfunction, fatigue, hair loss, damage to the heart, immune suppression, infertility, lung dysfunction, lymphedema, mental deficits, nausea, pain, sexual dysfunction, skin changes, weight loss or gain, and urinary and bladder problems. Radiation and chemotherapies comprise the bulk of cancer treatment methods in current practice, and the off-target effects are primarily due to the nonspecific toxicity of these methods. Obviously, limiting nonspecific toxicity will improve patients’ quality of life, while not affecting tumor directed dose—this provides the motivation to pursue tumor-targeted nanomedicine. Further, many current therapy methods do not adequately address the individual patient differences resulting from inter and intra-tumor heterogeneity. Ideal disease treatment would noninvasively deliver therapy to only the target, limiting side effects due to the nonspecific drug action, and expose the tumor to a sufficient amount of drug, or other therapy such as heat or radiation. Multifunctional nanoparticles (NPs), which aid in the diagnosis (generally by acting as a contrast agent for traditional diagnostic imaging modalities), possibly targeted to the specific molecular phenotype of tumors, and which also deliver therapy (nanotheranostics) offer benefits not possible with other therapies. Only about 1% of current therapeutic agents deposit in tumors; thus, the vast majority of injected drugs are either excreted or end up in undesired tissues. In addition to not effectively treating the disease, exposing the tumors to such low concentrations of chemotherapeutic agents also artificially selects for cells that can tolerate the drug, leading to resistance. Incorporating drugs into nanoconstructs that can be noninvasively tracked for delivery to the tumor and activated at the disease site, offers a potential solution to both the drug-delivery and toxicity/efficacy problems of current chemotherapies. Besides drug delivery, NPs can also be designed and used to thermally ablate the tumor using energy from an external source, thereby avoiding invasive surgical procedures. The subcellular size (in the tens to hundreds of nanometers, similar in size to organelles) of NPs makes them exceptionally well suited for use in drug delivery and/or as absorbers for certain wavelengths of light. They can circulate for a relatively long period because they avoid rapid filtration by the spleen and can pass through Kupffer cell sieve plates. A long circulation time gives them a greater percentage of injected dose accumulating in the desired location. Tumors generally exhibit a more porous vasculature and poorer lymphatic circulation than normal tissue, allowing more and larger particles to cross over between the blood vessels and intercellular space and build up there. This is called enhanced permeability and retention (EPR), and can cause NPs to build up in the tumor, provided they can circulate long enough.
关键词： Drug delivery,Cancer,Thermal ablation,Enhanced permeability and retention (EPR),Externally triggered NPs,Nanotheranostics,Nanomedicine
更新于2025-09-10 09:29:36
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Synthesis, characterization, swelling-deswelling properties of Novel nanoparticle-hydrogel containing core chitosan and their cyclohexanone-crosslinked counterparts
摘要： Novel Chitosan-cyclohexanone Mannich based hydrogel nanoparticles (CCMb1-4) were prepare via the reaction of chitosan with different concentration of 2, 6-bis (piperidin-1-ylmethyl) cyclohexanone. 2HCl (1%, 5%, 10% and 15% wt/wt) at 70–80°C for 7 h. These hydrogels were subjected to equilibrium swelling studies at room temperature in solutions of pH 2, 4, 6 and 8. The (CCMb1-4) showed maximum percent swellability at pH = 2.0. Furthermore, the swelling of the (CCMb1-4) followed Fickian diffusion. This preliminary investigation of chitosan-based interpolymeric hydrogels showed that they may be exploited to expand the utilization of these systems in drug delivery applications.
关键词： Chitosan,mannish base,hydrogels,drug delivery,swellability
更新于2025-09-10 09:29:36
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Aggregation-induced emission (AIE) fluorophores as imaging tools to trace the biological fate of nano-based drug delivery systems
摘要： The vigorous development of nanotechnology has been accompanied by an equally strong interest and research efforts in nano-based drug delivery systems (NDDSs). However, only a few NDDSs have been translated into clinic thus far. One of the important hurdles is the lack of tools to comprehensively and directly trace the biological fate of NDDSs. Recently, aggregation-induced emission (AIE) fluorophores have emerged as attractive bioimaging tools due to flexible controllability, negligible toxicity and superior photostability. Herein, we recapitulate the current advances in the application of AIE fluorophores to monitor NDDSs both in vitro and in vivo. Particularly, we discuss the cellular fates of self- indicating and stimuli-responsive NDDSs with AIE fluorophores. Moreover, we highlight the in vivo application of AIE agents on the long-term tracking of therapeutics and the multi- modal monitoring of diagnostics in NDDSs. Challenges and opportunities in AIE-guided exploration of NDDSs are also discussed in detail.
关键词： aggregation-induced emission,bioimaging tools,nano-based drug delivery system,in vitro and in vivo
更新于2025-09-10 09:29:36
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Designing luminescent ruthenium prodrug for precise cancer therapy and rapid clinical diagnosis
摘要： The effective design of a targeted drug delivery system could improve the therapeutic efficacy of anticancer drugs by reducing their undesirable adsorption and toxic side effects. Here, an RGD-peptide functionalized and bioresponsive ruthenium prodrug (Ru-RGD) was designed for both cancer therapy and clinical diagnosis. This prodrug can be selectively delivered to cervical tumor sites to enhance theranostic efficacy. The benzimidazole-based ligand of the complex is susceptible to acidic conditions so, after reaching the tumor microenvironment, ligand substitution occurs and the therapeutic drug is released. The deep-red emissions produced by both one-photon and two-photon excitation increases the potential of Ru-RGD for use in the deep tissue imaging of 3D tumor spheroids. The specific accumulation of the Ru prodrug in tumor sites allows for precise tumor diagnosis and therapy in vivo. Luminescence staining of 38 clinical patient specimens shows that Ru-RGD exhibits differences in binding capability between cervical cancer and normal tissue, with a sensitivity of 95% and a specificity of 100%. This study thus provides an approach for the effective design and application of targeted metal complexes in cancer therapy and clinical diagnosis.
关键词： targeted drug delivery,cancer theranosis,rapid clinical diagnosis,two-photon imaging,tumor microenvironment
更新于2025-09-10 09:29:36
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Rare earth-functionalized nanodiamonds for dual-modal imaging and drug delivery
摘要： Nanodiamonds (NDs) have attracted much attention in biomedical research for their high chemical stability, low toxicity and good biocompatibility. However, the insufficient fluorescence of NDs largely inhibit their multi-functional bio-applications ， such as simultaneous diagnosis and chemotherapy. Herein, a multifunctional NDs-based nanoparticles(ND-TTA:RE) with excellent fluorescence and paramagnetic properties has been fabricated by covalently functionalizing NDs with rare-earth (RE=Eu3+, Gd3+) 2-Thenoyltrifluoroacetone (TTA) complexes. The NDs-based nanoparticles exhibit intense red emission and could enhance the T1-weighted MR image due to the coordinated RE ions. The in vitro/in vivo experiments demonstrate its large potential for optical and MR imaging. In addition, the ND-TTA:RE also shows good drug storage capability that reach to 375 ug/mg toward anticancer drug doxorubicin (Dox) and exhibits significant pH-dependent drug-release behavior. The MTT assays shows that the as-synthesized ND-TTA:RE have low toxicity in a concentration range from 0 to 150 mg/mL, while the Dox-loaded ND-TTA:RE (ND-TTA:RE-Dox) shows effective chemotherapy towards gastric cancer cells. The dual-mode imaging and drug delivery abilities make ND-TTA:RE a promising nanomaterial for multifunctional applications. In addition, this work may also provide a new strategy for the design of multi-functional nanoplatform.
关键词： Dual-modal imaging,Nanodiamond,Rare earth,Drug delivery.
更新于2025-09-10 09:29:36
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Hollow CuS nanocube as nanocarrier for synergetic chemo/photothermal/photodynamic therapy
摘要： Here, hollow CuS nanocubes about 250-300 nm in size were synthesized based on the Kirkendall effect by using CuO nanocubeas precursor and template. The reactant concentration and reaction time could be adopted to adjust the final composition and hollow structure. The as-synthetic CuS nanocube was assembled by a great deal of nanoparticles (15-20 nm), making abundant porous structure in the shell layer. The localized surface plasmon resonance and the novel porous hollow structure (improve light reflex) further make sure the enhanced Near-infrared (NIR) light absorption as well as photothermal conversion efficiency (30.3 %). Moreover, the mechanism of reactive oxygen species (ROS) generation was investigated in detail, revealing that the released Cu+ ion and the oxygen are the determined factors. To further improve the monodispersity and biocompatibility, PEG-NH2 modified nanostructure (CuS@PEG) was prepared and it possessed high loading efficiency to doxorubicin hydrochloride (DOX). Moreover, DOX-CuS@PEG reveals the acid and NIR sensitive-release performance. The synergistic effect of chemotherapy associated with photothermal therapy (PTT) and photodynamic therapy (PDT) display the enhanced specific cytotoxicity to cancer cells.
关键词： Drug delivery,Hollow CuS,Photothermal therapy,Photodynamic therapy,NIR
更新于2025-09-10 09:29:36
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DOX/ICG-carrying γ-PGA-g-PLGA-based polymeric nanoassemblies for acid-triggered rapid DOX release combined with NIR-activated photothermal effect
摘要： To boost the efficacy of chemo-photothermal cancer treatment by the intracellular rapid release of doxorubicin (DOX) combined with near-infrared (NIR)-triggered photothermal effect of indocyanine green (ICG), the poly(γ-glutamic acid)-g-poly(lactic-co-glycolic acid) (γ-PGA-g-PLGA)-based polymeric nanoassemblies (PNAs) with simultaneous incorporation of DOX and ICG were developed in this work by simple one-step nanoprecipitation. The obtained DOX/ICG-loaded PNAs were characterized by a compact γ-PGA/DOX complexes-encapsulated PLGA-rich core covered with the co-assembly of amphiphilic D-α-tocopheryl polyethylene glycol succinate (TPGS), 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[amino(polyethylene glycol)] (DSPE-PEG) and ICG molecules. The robust cargo-loaded PNAs not only promoted the photo-stability of ICG in PBS, but also reduced ICG leakage from PNAs. With the milieu pH being altered from 7.4 to 5.0, the massive disruption of ionic DOX/γ-GA complexes and PLGA degradation considerably accelerated DOX release from payload-containing PNAs. The results of in vitro cellular uptake revealed that the DOX/ICG-loaded PNAs appreciably enhanced the cellular uptake of payloads by HeLa cells. Notably, through the intracellular acid-triggered rapid DOX release combined with the ICG-based NIR-activated hyperthermia and singlet oxygen generation, the combination therapy of DOX/ICG-loaded PNAs can use lower dosage of drugs to effectively inhibit proliferation of HeLa cells compared to the chemo or photothermal treatment alone, thus showing the great potential to improve efficacy of cancer treatment.
关键词： polymeric nanoassemblies,pH-triggered DOX release,NIR-activated photothermal treatment,amphiphilic graft copolymers,intracellular drug delivery
更新于2025-09-09 09:28:46