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RSC Advances · 2018 ·Vol. 8 ·期 54 ·30887-30893 · IF 2.936

Novel oligopeptide nanoprobe for targeted cancer cell imaging

Wen-Qiang Ding,Si-Yong Qin,Yin-Jia Cheng,Yi-Han Ma,Ai-Qing Zhang

Here we designed and constructed a tryptophan-phenylalanine-phenylalanine-tryptophan (WFFW) tetrapeptide, which generated photostable and tunable fluorescence emission signals from 340 nm to 500 nm. The WFFW tetrapeptide could self-assemble into a spherical nanostructure with enhanced fluorescence intensity. Driven by π–π stacking and hydrogen bond interaction, WFFW co-assembled with arginine-glycine-aspartic acid (RGD) modified WFFW to form a cancer-targeted fluorescent nanoprobe, which could selectively image the cancer cells.

研究领域: 生物化学 · 医学影像 · 纳米医学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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BIOCONJUGATE CHEMISTRY · 2019 · IF 4.349

Theranostic Quercetin Nanoparticle for Treatment of Hepatic Fibrosis

Qiang Zhang,Dan Xu,Qiuyan Guo,Wenjun Shan,Jun Yang,Tongtong Lin,Shefang Ye,Xi Zhou,Yunlong Ge,Shengli Bi,Lei Ren

The progression of hepatic fibrosis can lead to cirrhosis and hepatic failure, but the development of antifibrotic drugs have faced the challenges of poor effectiveness and targeted specificity. Herein, a theranostic strategy was carried to encapsulate a natural medicine (Quercetin, QR) into hepatitis B core (HBc) protein nanocages (NCs) for imaging and targeted treatment of hepatic fibrosis. It was noted that nanoparticles (RGD-HBc/QR) with surface-displayed RGD targeting ligand exhibit a rather high selectivity toward activated HSCs via the binding affinity with integrin αvβ3, and an efficient inhibition of proliferation and activation of hepatic stellate cells (HSCs) in vitro and in vivo. Once encapsulated in quercetin–gadolinium complex and/or labeled with the NIR fluorescent probes (Cy5.5), the resulting nanoparticles (RGD-HBc/QGd) show great potential as NIR fluorescent and magnetic resonance imaging contrast agents for hepatic fibrosis in vivo. Therefore, the multifunctional integrin-targeted nanoparticles could selectively deliver QR to the activated HSCs, and may provide an effective antifibrotic theranostic strategy.

CAS / MDL: 367-93-1
研究领域: 医学 · 药学 · 生物技术
✓ 已验证 产品关联 DOI PubMed 高影响因子
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BIOMATERIALS · 2026 · IF 13.6

Ready-to-use, in situ formed collagen/RGD/hyaluronic acid hydrogel: accelerating full-thickness wound healing

Tiemei Zheng,Siqi Li,Yusen Li,Jin Song,Pengyu Huang,Xiaosong Gu,Kuo Yang,Xiuyun Liu,Xiaoli Wang

A robust strategy was developed to customize the hydrogel's composition, concentration, and crosslink density, thereby providing a method for the screening and optimization of skin repair hydrogels. Specifically, methyltetrazine-modified collagen (Col-T), norbornene-modified RGD peptide, and norbornene-modified hyaluronic acid with varying degrees of modification (HA-N low , HA-N med , and HA-N high ), were synthesized. Upon mixing Col-T, RGD-N, and one of the HA-N derivatives, a bioorthogonal reaction was immediately initiated, thereby forming an in situ crosslinked, shape-adaptable hydrogel. An extracellular matrix-mimetic hydrogel composed of collagen, RGD peptide, and hyaluronic acid was optimized using human epidermal stem cells (hEpdSCs), human dermal fibroblasts (HDFs), and human umbilical vein endothelial cells (HUVECs). The optimized hydrogel effectively promoted the hEpdSCs proliferation, the proliferation and migration of HDFs, and the migration and tubular formation of HUVECs. In comparison, GelMA exhibited significant cytotoxicity against hEpdSCs due to the use of photoinitiator LAP. The hydrogel exhibited anti-hemolytic, pro-coagulant, and tissue-adhesive properties, and significantly accelerated the healing of 15 mm × 15 mm full-thickness wound after a single application without any additives. This hydrogel was associated with enhanced hair follicle-like structure formation and reduced inflammation-related responses in the wound area. Furthermore, its ready-to-use and biodegradable nature made it highly suitable for clinical applications.

✓ 已验证 DOI PubMed 高影响因子
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Materials Today Bio · 2025 · IF 10.2

Two-dimensional graphene nanomaterials for combined photothermal and chemotherapy-enhanced targeted therapy of breast cancer

Xiongjie Zhu,Juanjuan Lei,Chao Jiang,Zhaobi Fang,Wenkai Zhang,Zhe Yang,Rui Guo,Rui Xu,Xiaoshan Hu

Breast cancer is one of the most common malignant tumors in women, accounting for 7–10 % of all malignant tumors in the body. Second only to uterine cancer, it poses a significant threat to women's health. In this study, a two-dimensional material based on GO nanoparticles was designed to combine photothermal therapy (PTT) with chemotherapy for targeted treatment of breast cancer. Firstly, HPAA was grafted onto GO through an amide reaction after EDC/NHS activation. Secondly, RGD was attached to the amino group of HPAA. Finally, the chemotherapeutic drug doxorubicin was loaded through intermolecular interactions. In vitro results showed that the HPAA/GO-RGD@DOX exhibited a good photothermal effect and drug release profile, with greater drug release in acidic environments compared to neutral ones. Additionally, it accelerated the apoptosis of tumor cells under laser irradiation. Importantly, in vivo experiments demonstrated that HPAA/GO-RGD@DOX, when combined with laser irradiation, effectively targeted the tumor site and inhibited tumor growth. In conclusion, HPAA/GO-RGD@DOX exhibits high tumor targeting efficiency and a strong photothermal effect. This study suggests that the HPAA/GO-RGD@DOX composite holds great promise as a new type of functional 2D nanoparticle with photothermal capabilities for breast cancer therapy.

研究领域: 肿瘤学 · 纳米医学 · 生物材料学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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POLYMER DEGRADATION AND STABILITY · 2020 · IF 4.032

A chitosan based scaffold with enhanced mechanical and biocompatible performance for biomedical applications

Xianzhen Dong,Qiao Cheng,Yanpiao Long,Chao Xu,Honglin Fang,Yuzhe Chen,Honglian Dai

Chitosan exhibiting excellent functional properties was found to be potential in a wide variety of industrial and biomedical applications. The lack of biological activities and the poor mechanical properties somewhat limit its applications. To address these limitations, chemical modification has been proved to be an efficient method. Here, we immobilized arginine-glycine-aspartic acid (RGD) on chitosan molecules and incorporated the chitosan with Poly(L-lactide-co-glycolide)-Poly(ethylene glycol) (PLGA-PEG) and β-tricalcium phosphate (β-TCP) nanoparticles to obtain a chitosan-based scaffold with enhanced mechanical and biocompatible performance. XPS and FT-IR confirmed the successful grafting of RGD peptides onto the chitosan chain. The mechanical properties, hydrophilicity and degradation behaviors of the membrane were characterized by stress-strain, water contact angle, and weight loss, respectively. Cytotoxicity, cellular adhesion, and cellular viability of the scaffolds were studied by MTT assay, cell adhesion, and cell survival experiments, respectively. The advantageous mechanical properties and the hydrophilic surface of the chitosan-based scaffold were achieved by blending with PLGA-PEG. The preliminary biocompatibility studies revealed that all the scaffolds were cell compatible, and the hydrophilic surface was more suitable for cell adhesion. The scaffolds grafted with RGD exhibited high cell adhesion rate than the pure chitosan. The results suggested that the surface hydrophilicity and biocompatibility of the chitosan-based scaffolds play an important role in enhancing cell adhesion and growth.

研究领域: 生物医学工程 · 材料科学 · 细胞生物学
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Science of Advanced Materials · 2019 ·Vol. 11 ·期 7 ·1008-1018 · IF 1.158

Application of New Fluorescent Carbon Point Material in Digital Image Detection of Skin Tumors

Pan Hongtao,Zhang Yanjie,Zhao Xiangkun,Zhou Hongsuo

In this study, glutamic acid and sugar are selected as raw materials to produce glutamic acid-sucrose fluorescent carbon dot material (CDs-N) according to a certain proportion. In order to prolong the time of biological detection, CDs-N-PEG is modified by PEG. Considering that melanoma will enter the brain, Angiopep-2 ligand and RGD circulating ligand are selected to further obtain CDs-N-PEG-ANG and CDs-N-PEG-RGD. The material is characterized, the fluorescence spectrum is tested, the tyrosinase detection test is designed, the B16F10 cells in vivo are selected for the biotoxicity test, and the tyrosinase and melanoma detection are extended to the organism. In this study, mice and zebrafish are selected as the research objects. The experimental results show that the fluorescent carbon dots designed in this study can detect tyrosinase well. With the increase of concentration and reaction time, the fluorescent carbon dots fluorescence intensity corresponding to the site will continue to increase. In the toxicity test of B16F10 cells, the fluorescent carbon dot material shows little toxicity, indicating that the material has good biocompatibility. Tyrosinase activity is well detected in zebrafish. By comparing B16F10 cells and Hela cells expressed with different tyrosinases, melanoma in mice is preliminarily detected. In this study, tyrosinase is used to detect melanoma and tyrosinase-based biomarkers are used to provide a feasible method for the preliminary diagnosis of melanoma.

研究领域: 生物医学 · 材料科学 · 肿瘤学
✓ 已验证 DOI 高影响因子
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BIOMEDICINE & PHARMACOTHERAPY · 2019 · IF 3.743

Improving breast cancer therapy using doxorubicin loaded solid lipid nanoparticles: Synthesis of a novel arginine-glycine-aspartic tripeptide conjugated, pH sensitive lipid and evaluation of the nanomedicine in vitro and in vivo

Gang Zheng,Meizhu Zheng,Ben Yang,Hui Fu,Yongqing Li

Breast cancer is the leading cause of cancer mortality in women worldwide. To overcome the toxic side effects and multidrug resistance (MDR) during doxorubicin (DOX) chemotherapy, an arginine-glycine-aspartic (RGD) tripeptide modified, pH-sensitive solid lipid nanoparticles (SLNs) is employed in this study. In this study, a RGD conjugated, pH sensitive lipid was synthesized using glycerin monostearate (GMS) and adipic acid dihydrazide (HZ) as lipid materials and named RGD-HZ-GMS. RGD-HZ-GMS was applied to encapsulate DOX to construct a RGD modified, DOX loaded SLNs (RGD-DOX-SLNs). To evaluate the anticancer effect of RGD-DOX-SLNs, breast cancer cell line (MCF-7 cells) and DOX resistant cell line (MCF-7/ADR cells) were used. in vivo tumor suspension and toxicity effects were evaluated on mice bearing MCF-7/ADR cells breast cancer model. RGD-DOX-SLNs had a uniformly spherical shape. The mean particle size and zeta potential of the RGD-DOX-SLNs was 96.3 nm and 35.6 mV, respectively. RGD-DOX-SLNs showed 5.58 fold higher area under the plasma concentration – time curve (AUC) compared with DOX solution. Terminal half life (T 1/2 ) and peak concentration (C max ) of RGD-DOX-SLNs was 10.85 h and 39.12 ± 2.71 L/kg/h. in vitro and in vivo antitumor results indicate that RGD-DOX-SLNs might be a promising novel lipid carrier which could improve breast cancer therapy.

研究领域: 肿瘤学 · 药剂学 · 生物医学工程
✓ 已验证 DOI PubMed 高影响因子
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CARBOHYDRATE POLYMERS · 2016 · IF 4.219

One-pot synthesis of dextran decorated reduced graphene oxide nanoparticles for targeted photo-chemotherapy

Yanfang Hu,Liang He,Jianxun Ding,Diankui Sun,Li Chen,Xuesi Chen

Graphene-based nanocarriers show great potential in photo-chemotherapy, however, to prepare desired reduced graphene oxide (rGO) nanoparticles in a facile way is still a challenge. Herein, a novel strategy has been presented to prepare rGO nanoparticle using dextran (Dex) as a reducing agent. In this strategy, Dex was directly conjugated on rGO by hydrogen bond and then self-assemble to form rGO/Dex nanoparticles. After decorated by dextran, rGO-based nanoparticles not only show excellent biocompatibility but also can load anticancer drug for photo-chemotherapy. The data of fourier transform infrared (FT-IR) analysis, Raman spectrum analysis, thermos-gravimetric analysis (TGA), X-ray photoelectron spectroscopy (XPS), the transmission electron microscope (TEM) image and dynamic light scattering (DLS) measurements powerfully proved that the stable rGO-based nanoparticles with desired nanosize have been successfully prepared. To verify the photo-chemotherapy, anticancer drug, doxorubicin (DOX), has been loaded on rGO/Dex nanoparticles (rGO/DOX/Dex). And RGD, a kind of oligopeptide which can improve the intracellular uptake by α v β 3 recognition, also has been introduced (rGO/DOX/RDex). Compared with single chemotherapy, rGO/DOX/Dex and rGO/DOX/RDex combining the local specific chemotherapy and external near-infrared (NIR) photo-thermal therapy show higher therapeutic efficacy, endowing the desired rGO-based nanoparticle with great potential for cancer treatments.

CAS / MDL: 9048-71-9 9004-54-0
研究领域: 纳米医学 · 肿瘤学 · 生物材料
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF CONTROLLED RELEASE · 2014 · IF 7.261

Efficient, dual-stimuli responsive cytosolic gene delivery using a RGD modified disulfide-linked polyethylenimine functionalized gold nanorod

Feihu Wang,Yuanyuan Shen,Wenjun Zhang,Min Li,Yun Wang,Dejian Zhou,Shengrong Guo

Controlled-release systems capable of responding to external stimuli and/or unique internal environments have received great interests in site-specific gene and/or drug delivery. In this work, a functionalized gene nanocarrier for dual-stimuli triggered cytosolic gene delivery is developed and showing high gene delivery efficacy with low cytotoxicity. The nanocarrier is prepared by conjugating gold nanorod (GNR) with multiple disulfide cross-linked short PEIs to harness the advantageous properties of GNR based near infrared (NIR) laser induced photothermal heating and intracellular stimuli-triggered degradability of disulfide cross-linked short PEIs (DSPEI). The DSPEI is further grafted with a poly(ethylene glycol) (PEG) section to afford high carrier stability in cell cultures and a terminal RGD peptide for specific targeting of cancer cells. The nanocarrier is found to effectively condense plasmid DNA to form a highly stable GNR-DSPEI-PEG-RGD/DNA complex with tumor cell-targeting ability that can be efficiently uptaken by cancer cells. Moreover, the loaded genes can be effectively released from the complex triggered by the high intracellular glutathione content and/or by photothermal effect of NIR irradiation at 808   nm. Interestingly, the GNRs-based complex can easily escape from intracellular endo-/lyso-somal compartments and release the gene load into the cytosol upon exposure to NIR irradiation, resulting in significantly improved gene transfection efficiency. Our new gene carrier exhibits high gene transfection efficiency, comparable to or even better than that of high MW PEIs, but with a much lower cytotoxicity. Additionally, neither the GNR-based carrier nor the laser treatment shows any significant evidence of cytotoxicity. This work demonstrates a promising strategy for intracellular stimuli triggered, photothermal controllable gene delivery system, which can be further applied to many other nanomedicine fields.

研究领域: 生物医学工程 · 分子生物学 · 纳米医学
✓ 已验证 DOI PubMed 高影响因子
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JOURNAL OF NANOBIOTECHNOLOGY · 2020 ·Vol. 18 ·期 1 ·1-11 · IF 6.518

Co-delivery of miR-29b and germacrone based on cyclic RGD-modified nanoparticles for liver fibrosis therapy

Ji De,Wang Qiaohan,Zhao Qi,Tong Huangjin,Yu Mengting,Wang Meng,Lu Tulin,Jiang Chengxi

Hepatic stellate cells (HSCs) were activated and secreted excessive amounts of extracellular matrix (ECM) proteins during pathogenetic progress of liver fibrosis. Germacrone (GMO) and miR-29b can play an important role in inhibiting growth of HSCs and production of type I collagen. GMO and miR-29b were co-encapsulated into nanoparticles (NPs) based on poly(ethylene glycol)-block-poly(lactide-co-glycolide) (PEG-PLGA). Then, NPs were modified with cyclic RGD peptides (cRGDfK). cRGDfK is an effective ligand to bind integrin αvβ3 and increase the targeting ability for fibrotic liver. GMO- and miR-29b-loaded NPs exhibited great cytotoxicity to activated HSCs and significantly inhibited production of type I collagen. Liver fibrosis model of mice was induced by administration of carbon tetrachloride. Great targeting ability was achieved in liver fibrotic mice treated with cRGD-modified NPs. Significant ant-fibrotic effects have been presented based on hematoxylin and eosin (H&E), Masson and Sirius Red staining results of liver tissues collected from mice treated with drug-loaded NPs. All these results indicate GMO- and miR-29b-loaded cRGD-modified NPs have the potential for clinical use to treat liver fibrosis.

研究领域: 药理学 · 分子生物学 · 纳米医学
✓ 已验证 DOI PubMed 高影响因子
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International Journal of Nanomedicine · 2023 · IF 8

Topical ocular delivery to laser-induced choroidal neovascularization by dual internalizing RGD and TAT peptide-modified nanoparticles

Yongchao Chu,Ning Chen,Huajun Yu,Hongjie Mu,Bin He,Hongchen Hua,Aiping Wang,Kaoxiang Sun

A nanoparticle (NP) was developed to target choroidal neovascularization (CNV) via topical ocular administration. The NPs were prepared through conjugation of internalizing arginine-glycine-aspartic acid RGD (iRGD; Ac-CCRGDKGPDC) and transactivated transcription (TAT) (RKKRRQRRRC) peptide to polymerized ethylene glycol and lactic-co-glycolic acid. The iRGD sequence can specifically bind with integrin αvβ3, while TAT facilitates penetration through the ocular barrier. 1H nuclear magnetic resonance and high-performance liquid chromatography demonstrated that up to 80% of iRGD and TAT were conjugated to poly(ethylene glycol)– poly(lactic-co-glycolic acid). The resulting particle size was 67.0±1.7 nm, and the zeta potential of the particles was −6.63±0.43 mV. The corneal permeation of iRGD and TAT NPs increased by 5.50- and 4.56-fold compared to that of bare and iRGD-modified NPs, respectively. Cellular uptake showed that the red fluorescence intensity of iRGD and TAT NPs was highest among primary NPs and iRGD- or TAT-modified NPs. CNV was fully formed 14 days after photocoagulation in Brown Norway (BN) rats as shown by optical coherence tomography and fundus fluorescein angiography analyses. Choroidal flat mounts in BN rats showed that the red fluorescence intensity of NPs followed the order of iRGD and TAT NPs > TAT-modified NPs > iRGD-modified NPs > primary NPs. iRGD and TAT dual-modified NPs thus displayed significant targeting and penetration ability both in vitro and in vivo, indicating that it is a promising drug delivery system for managing CNV via topical ocular administration.

研究领域: 药剂学 · 眼科 · 分子生物学
✓ 已验证 DOI PubMed 高影响因子
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Contrast Media & Molecular Imaging · 2017 · IF 3.307

Synthesis and Bioevaluation of Iodine-131 Directly Labeled Cyclic RGD-PEGylated Gold Nanorods for Tumor-Targeted Imaging

Yingying Zhang,Yongxue Zhang,Lianglan Yin,Xiaotian Xia,Fan Hu,QingYao Liu,Chunxia Qin,Xiaoli Lan

Introduction. Radiolabeled gold nanoparticles play an important role in biomedical application. The aim of this study was to prepare iodine-131 (131I)-labeled gold nanorods (GNRs) conjugated with cyclic RGD and evaluate its biological characteristics for targeted imaging of integrin β3-expressing tumors. Methods. HS-PEG(5000)-COOH molecules were applied to replace CTAB covering the surface of bare GNRs for better biocompatibility, and c(RGDfK) peptides were conjugated onto the carboxyl terminal of GNR-PEG-COOH via EDC/NHS coupling reactions. The nanoconjugate was characterized, and 131I was directly tagged on the surface of GNRs via AuI bonds for SPECT/CT imaging. We preliminarily studied the characteristics of the probe and its feasibility for tumor-targeting SPECT/CT imaging. Results. The 131IGNR-PEG-cRGD probe was prepared in a simple and rapid manner and was stable in both PBS and fetal bovine serum. It targeted selectively and could be taken up by tumor cells mainly via integrin β3-receptor-mediated endocytosis. In vivo imaging, biodistribution, and autoradiography results showed evident tumor uptake in integrin β3-expressing tumors. Conclusions. These promising results showed that this smart nanoprobe can be used for angiogenesis-targeted SPECT/CT imaging. Furthermore, the nanoprobe possesses a remarkable capacity for highly efficient photothermal conversion in the near-infrared region, suggesting its potential as a multifunctional theranostic agent.

研究领域: 纳米技术 · 放射学 · 分子生物学 · 癌症研究 · 生物医学工程
✓ 已验证 DOI PubMed 高影响因子
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