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Synthesis of new zinc (II) phthalocyanine conjugates with block copolymers for cancer therapy
摘要： Synthetic routes towards new conjugates of hydrophilic zinc(II) phthalocyanine (ZnPc) with poly(ethylene oxide)-b-poly(propylene oxide)-b-poly(ethylene oxide) (Pluronic P123) and poly(L-lactide) (PLLA), are described. The main semiproduct ZnPc was obtained by heating 4-nitrophthalimide with urea and zinc chloride, followed by the reduction step. Steglich esterification was used to synthesize two ZnPc-conjugated block copolymers, further utilized in fabrication of polymeric micelles (PMs) - functionalized with the zinc(II) phthalocyanine-type moiety. Biological evaluation of the PMs indicated an acceptable biocompatibility level in accord with requirements in the field of nanotheranostics and nanomedicine.
关键词： fluorescent polymeric micelles,cyclotetramerization,Steglich esterification,in vitro biological evaluation,ZnPc-conjugated block copolymers,diagnostic marker
更新于2025-09-23 15:22:29
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Dual-responsive doxorubicin-conjugated polymeric micelles with aggregation-induced emission active bioimaging and charge conversion for cancer therapy
摘要： In recent years, intelligent polymeric micelles with multi-functions are in urgent demand for cancer diagnosis and therapy. Herein, pH and redox dual-responsive prodrug micelles with aggregation-induced emission (AIE) active cellular imaging and charge conversion have been prepared for combined chemotherapy and bioimaging based on a novel doxorubicin-conjugated amphiphilic PMPC-PAEMA-P (TPE-co-HD)-ss-P (TPE-co-HD)-PAEMA-PMPC copolymer. The doxorubicin is conjugated via a pH cleavable imine linkage and can be packed in the hydrophobic core along with the glutathione (GSH)-sensitive disulfide bond. The DOX-conjugated inner core is sealed with a pH-responsive PAEMA as the “gate”, which would rapidly open in the acidic condition, following the drug release and charge conversion-mediated acceleration of endocytosis. After an efficient internalization, the disulfide bond can be cleaved by the high concentration of GSH causing the further accelerated drug release. Meanwhile, intracellular drug delivery can be traced due to the AIE behavior of micelles. Moreover, great tumor inhibition in vitro and in vivo has been demonstrated for these DOX-conjugated micelles. This smart prodrug micelle system would be a desirable drug carrier for cancer therapy and bioimaging.
关键词： polymeric micelles,charge conversion,aggregation-induced emission,dual-responsive,cancer therapy
更新于2025-09-23 15:21:21
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Synthesis and analysis of 64Cu-labeled GE11-modified polymeric micellar nanoparticles for EGFR-targeted molecular imaging in a colorectal cancer model
摘要： Polymeric micellar nanoparticles represent versatile and biocompatible platforms for targeted drug delivery. However, tracking their biodistribution, stability, and clearance profile in vivo is challenging. The goal of this study was to prepare surface-modified micelles with peptide GE11 for targeting the epidermal growth factor receptor (EGFR). In vitro fluorescence studies demonstrated significantly higher internalization of GE11-micelles into EGFR-expressing HCT116 colon cancer cells versus EGFR-negative SW620 cells. Azo coupling chemistry of tyrosine residues in the peptide backbone with aryl diazonium salts was used to label the micelles with radionuclide 64Cu for positron emission tomography (PET) imaging. In vivo analysis of 64Cu-labeled micelles showed prolonged blood circulation and predominant hepatobiliary clearance. The biodistribution profile of EGFR-targeting GE11-micelles was compared with non-targeting HW12-micelles in HCT116 tumor-bearing mice. PET revealed increasing tumor-to-muscle ratios for both micelles over 48 h. Accumulation of GE11-containing micelles in HCT116 tumors was higher compared to HW12-decorated micelles. Our data suggest that the efficacy of image-guided therapies with micellar nanoparticles could be enhanced by active targeting, as demonstrated with cancer biomarker EGFR.
关键词： polymeric micelles,epidermal growth factor receptor (EGFR),64Cu,GE11 peptide,Colorectal cancer,positron emission tomography (PET)
更新于2025-09-23 15:21:01
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Preliminary Study of MR and Fluorescence Dual-mode Imaging: Combined Macrophage-Targeted and Superparamagnetic Polymeric Micelles
摘要： Purpose: To establish small-sized superparamagnetic polymeric micelles for magnetic resonance and fluorescent dual-modal imaging (MRI) and investigated the macrophage-targeted in vitro. Methods: A new class of superparamagnetic iron oxide nanoparticles (SPIONs) and Nile red-co-loaded mPEG-Lys3-CA4-NR/SPION polymeric micelles was synthesized to label Raw264.7 cells. The physical characteristics of the polymeric micelles were assessed, the T2 relaxation rate was calculated, and the effect of labeling on the cell viability and cytotoxicity was also determined in vitro. In addition, further evaluation of the application potential of the micelles was conducted via in vitro MRI. Results: The diameter of the mPEG-Lys3-CA4-NR/SPION polymeric micelles was 33.8 ± 5.8 nm on average. Compared with the hydrophilic SPIO, mPEG-Lys3-CA4-NR/SPION micelles increased transversely (r2), leading to a notably high r2 from 1.908 μg/mL-1S-1 up to 5.032 μg/mL-1S-1, making the mPEG-Lys3-CA4-NR/SPION micelles a highly sensitive MRI T2 contrast agent, as further demonstrated by in vitro MRI. The results of Confocal Laser Scanning Microscopy (CLSM) and Prussian blue staining of Raw264.7 after incubation with micelle-containing medium indicated that the cellular uptake efficiency is high. Conclusion: We successfully synthesized dual-modal MR and fluorescence imaging mPEG-Lys3-CA4-NR/SPION polymeric micelles with an ultra-small size and high MRI sensitivity, which were effectively and quickly uptaken into Raw 264.7 cells. mPEG-Lys3-CA4-NR/SPION polymeric micelles might become a new MR lymphography contrast agent, with high effectiveness and high MRI sensitivity.
关键词： macrophage-targeted,polymeric micelles,MRI,SPIONs,fluorescence imaging
更新于2025-09-23 15:21:01
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ICGa??Conjugated and <sup>125</sup> Ia??Labeled Polymeric Micelles with High Biosafety for Multimodality Imaginga??Guided Photothermal Therapy of Tumors
摘要： Noninvasive multimodality imaging-guided precision photothermal therapy (PTT) is proven to be an effective strategy for tumor theranostics by integrating diagnostics and therapeutics in one nanoplatform. In this study, indocyanine green (ICG)-conjugated and radionuclide iodine-125 (125I)-labeled polymeric micelles (PEG-PTyr(125I)-ICG PMs) are strategically prepared by the self-assembly of the ICG-decorated amphiphilic diblock polymer poly(ethylene glycol)–poly(l-tyrosine-125I)–(indocyanine green) (PEG-PTyr(125I)-ICG). The as-prepared polymeric micelles exhibit favorable biocompatibility, excellent size/photo/radiolabel stability, a high-photothermal conversion efficiency, a passive tumor-targeting ability, and a fluorescence (FL)/photoacoustic (PA)/single photon emission computed tomography (SPECT) imaging property. After tail intravenous injection, the polymeric micelles can efficiently accumulate at the tumor site and present comprehensive FL/PA/SPECT images with a high sensitivity, excellent spatial resolution, and unlimited tissue penetration under near-infrared (NIR) irradiation. Upon 808 nm laser irradiation, the subsequent precision PTT of tumors can be achieved with minimal cumulative side effects. Thus, this capable multifunctional nanoplatform with simple components and preparation procedures for FL/PA/SPECT multimodality imaging-guided PTT can be a potential candidate for clinical tumor theranostics.
关键词： biosafety,multimodality imaging,photothermal therapy,polymeric micelles,tumor theranostics
更新于2025-09-16 10:30:52
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Cyclic-Arginine-Glycine-Aspartic (c-RGD) Conjugated Polymeric Micelles for SPECT/NIRF Dual-Modality Tumor Imaging
摘要： The purpose of this research was to develop a dual modality nanoparticle probe for nuclear and near-infrared fluorescence tomography (NIRF) imaging of tumor integrin αvβ3 expression. c-RGD was conjugated to polyethylene glycol-coated, core-crosslinked polymeric micelles (CCPM) dually labeled with both near-infrared fluorescence fluorophores (Cy7) and a radioisotope (111In). In vitro, CCPM-RGD was selectively bound to αvβ3 positive human glioma U87 cells, and this uptake could be blocked by an excess amount of c-RGD. In vivo, subcutaneously U87 xenograft tumors were clearly visible by both SPECT and NIRF after intravenous administration of 18.5 MBq111In labeled CCPM-RGD. The accumulation of 111In-CCPM-RGD in the U87 tumor could be significantly reduced after co-injection with an excess amount of c-RGD peptide (>95% inhibition). At 72 hrs post injection, the tumor uptake was 5.21 ± 0.46% of the injected dose per gram of tissue (%ID/g). 111In-labeled CCPM-RGD allowed visualization of cancer cells over expressing αvβ3 by both nuclear and optical techniques.
关键词： SPECT Imaging,c-RGD,Fluorescence Optical Imaging,Polymeric Micelles
更新于2025-09-10 09:29:36
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Aggregation-Induced Emission (AIE) Polymeric Micelles for Imaging-Guided Photodynamic Cancer Therapy
摘要： Photodynamic therapy (PDT) is a noninvasive treatment for selectively killing malignant tumor cells. The photosensitizer is a necessary component of photodynamic nanomedicine. Many efforts have been made to develop new photosensitizers for efficient cancer photodynamic therapy. In this work, we report a novel nano photosensitizer, polymeric micelles (AIE-M) with aggregation induced emission characteristic, for photodynamic cancer therapy. AIE-M with sub-20 nm particle size is prepared by the self-assembly of salicylaldazine-incorporated amphiphilic polymer (AIE-1), which can produce reactive oxygen species (ROS) with light irradiation in solution. After uptake by cancer cells, AIE-M can specially sojourn in plasma membranes of cancer cells at the early stage and predominantly accumulate in the mitochondria of cancer cell at the late stage. The phototoxicity of AIE-M, resulting from the generation of intracellular ROS with light irradiation, can efficiently cause cancer cells death by apoptosis and necrosis. The advantages of AIE-M as a nano photosensitizer include the small size, highly colloidal stability in the process of preparation and storage, and high cell penetration. The ultra-low Critical Micelle Concentration (CMC) of AIE-1, negligible dark toxicity and super phototoxicity of AIE-M suggest its promising potential for image-guided PDT.
关键词： polymeric micelles,imaging,photodynamic,aggregation induced emission,cancer therapy
更新于2025-09-09 09:28:46