JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2026
·
IF 4.9
Guolong Shi,Minglin Ji,Sedrati Manar,Jing Chen,Guohua Jiang
Antithrombotic medications, including antiplatelet drugs, anticoagulants, and thrombolytics, remain fundamental to the clinical management of thrombosis, as they are widely used in the treatment of cardiovascular diseases and other conditions to prevent and treat thrombotic events. Thrombolytic agents, such as urokinase and streptokinase, are pivotal in the treatment of acute thrombotic diseases by activating the fibrinolytic system to dissolve blood clots. However, these agents face challenges due to their limited targeting specificity, short half-life, and varying efficiency, which can result in suboptimal therapeutic outcomes. In this study, we developed cyclic RGD (cRGD)-functionalized liposomes (IR/LK@cLip) to encapsulate IR-780 and lumbrokinase (LK). Leveraging the affinity of the RGD sequence for activated platelet membrane glycoprotein IIb/IIIa receptors, we aimed to improve the targeted chemo-photothermal combined therapy for thrombi. The cRGD can specifically target GPIIb-IIIa receptors, which are overexpressed on activated platelets, enabling the fabricated liposomes to actively recognize thrombi. When exposed to near-infrared (NIR) laser irradiation, IR-780, acting as a photosensitizer, can induce the disintegration of liposomes and promote the release of LK, which enhances drug penetration efficiency by increasing thrombus porosity. In vivo studies have confirmed that IR/LK@cLip exhibits effective accumulation at the site of thrombus formation. Moreover, the IR/LK@cLip has demonstrated the ability to rapidly restore blood circulation at thrombosed locations, suggesting its potential as a powerful antithrombotic treatment.
✓ 已验证
产品关联
DOI
高影响因子
Polymer Chemistry
·
2018
·Vol. 9
·期 14
·1780-1786
·
IF 4.927
Chao Chen,San H. Thang
Synthetic peptides containing the arginine–glycine–aspartate (RGD) motif have been used extensively as inhibitors of integrin–ligand interactions in studies of cell adhesion and cell target moiety. MARGD (sequences: Phe-Gly-Arg-Gly-Asp-Ser), a methacrylamide monomer containing a pending RGD peptide, was synthesized and obtained in high purity (≥90%) via an automated peptide synthesizer followed by a simple precipitation in diethyl ether. MARGD can be polymerised by reversible addition–fragmentation chain transfer (RAFT) polymerization to afford well-defined polymers containing a RGD peptide group with controlled molecular weight, low dispersity (Đ < 1.25), and a precise chain end structure. In this study, linear pseudo-first-order kinetics and number average molecular weight dependence on conversion were observed during the RAFT polymerization. Diblock peptide-polymer conjugates were prepared using PMARGD as a macro-chain transfer agent or using MARGD as a monomer, and the resulting diblock conjugates all showed low dispersities. The cytotoxicity study using mouse fibroblast cells (L929) revealed that the bioconjugates are non-toxic up to high concentration. Furthermore, enhanced cell adhesion was observed when the bioconjugates immobilized on the glass slide surfaces. This study provides a novel and efficient strategy to access well-defined peptide-polymer conjugates with diversity for both peptides and polymers.
研究领域:
聚合物化学
·
生物材料
·
细胞生物学
✓ 已验证
DOI
高影响因子
JOURNAL OF BIOMATERIALS SCIENCE-POLYMER EDITION
·
2015
·
IF 1.648
Ju Liang,Wenlan Wu,Danyu Lai,Junbo Li,Cailin Fang
A lipopeptide (LP)-containing KKGRGDS as the hydrophilic heads and lauric acid (C12) as the hydrophobic tails has been designed and prepared by standard solid-phase peptide synthesis technique. LP can self-assemble into spherical micelles with the size of ~30 nm in PBS (phosphate buffer saline) (pH 7.4). Curcumin-loaded LP micelles were prepared in order to increase the water solubility, sustain the releasing rate, and improve the tumor targeted delivery of curcumin. Water solubility, cytotoxicity, in vitro release behavior, and intracellular uptake of curcumin-loaded LP micelles were investigated. The results showed that LP micelles can increase the water solubility of curcumin 1.1 × 103 times and sustain the release of curcumin in a low rate. Curcumin-loaded LP micelles showed much higher cell inhibition than free curcumin on human cervix carcinoma (HeLa) and HepG2 cells. When incubating these curcumin-loaded micelles with HeLa and COS7 cells, due to the over-expression of integrins on cancer cells, the micelles can efficiently use the tumor-targeting function of RGD (functionalized peptide sequences: Arg-Gly-Asp) sequence to deliver the drug into HeLa cells, and better efficiency of the self-assembled LP micelles for curcumin delivery than crude curcumin was also confirmed by LCSM (laser confocal scanning microscope) assays. Combined with the enhanced solubility and higher cell inhibition, LP micelles reported in this study may be promising in clinical application for targeted curcumin delivery.
研究领域:
药剂学
·
肿瘤学
·
生物材料
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INORGANIC CHEMISTRY COMMUNICATIONS
·
2025
·
IF 5.4
Peijian Yang,Ying Li,Haiyun Zhai,Xiulan Cai
The aim of this study is to develop a novel molybdenum oxide nanocomposite with good dispersion and targeting tumor cells and investigate their DOX delivery performance. Briefly, molybdenum oxide (MoO x ) nanocomposite prepared by hydrothermal method were grafted with polyglycerol (MoO x -PG), followed by stepwise organic coupling with RGD peptide (MoO x -PG-RGD), and finally loaded with DOX. The physicochemical properties of MoO x -PG-RGD nanocomplexes were characterized by FTIR, SEM, XPS and TGA. The results showed that the grafted PG layer largely enhanced the dispersibility and biocompatibility of MoO x nanocomposite in physiological media. The obtained MoO x -PG-RGD/DOX exhibited drug-loading efficiency of 18.67 %. Drug release experiments indicated that MoO x -PG-RGD/DOX exhibited a faster release rate under acidic conditions in tumors. In addition, MTT cytotoxicity assay and cell uptake experiments indicated that MoO x -PG-RGD/DOX efficiently delivered DOX into targeted cells by integrin α v β 3 receptor-mediated endocytosis, which leading to an enhanced therapeutic efficacy of DOX. These results suggested that MoO x -PG-RGD, as a novel anticancer drug delivery vector, had great potential for application in tumor therapy.
研究领域:
纳米医学
·
药物递送
·
癌症治疗
·
材料科学
·
生物医学工程
✓ 已验证
产品关联
DOI
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
·
2016
·
IF 3.902
Yi Zhang,Zhongbing Huang,Zhi Wu,Guangfu Yin,Lei Wang,Fabao Gao
Absence of efficient targeting limits the application of magnetic nanochains (NCs) in the diagnosis of early brain cancer. Herein, dextran-coated NCs (more than 100 nm length and ∼10 nm cores diameter), which were modified by cyclic pentapeptide c(RGDyC) or chlorotoxin (CTX) as the targeting molecules, were fabricated via carbodiimide chemistry and thiol technique. The analysis results revealed that the obtained slender NCs exhibited good biocompatibility, superparamagnetic property, high transverse relaxivity ( R 2 ) and longer blood circulation time. The test results of human umbilical vein endothelial cells and U251 human glioma cells indicated that the conjugation of c(RGDyC) could obviously increase the cyto-internalization of c(RGDyC)-NCs, however, CTX modification could significantly enhance accumulation of CTX-NCs in U251 cells, leading to cellular apoptosis. The results of in vivo biodistribution tests and in vivo magnetic resonance (MR) imaging indicated that, although the c(RGDyC)-NCs could target early glioma to some extent and obviously enhance the contrast of MR imaging, CTX-NCs possessed higher tumor-targeting ability and good inhibition effect than the c(RGDyC)-NCs, suggesting that CTX-NCs are promising candidates for the diagnosis and therapy of early glioma.
研究领域:
生物医学工程
·
肿瘤学
·
分子影像学
✓ 已验证
DOI
PubMed
高影响因子
BIOMATERIALS
·
2014
·
IF 8.312
Wantong Song,Zhaohui Tang,Dawei Zhang,Ying Zhang,Haiyang Yu,Mingqiang Li,Shixian Lv,Hai Sun,Mingxiao Deng,Xuesi Chen
There are two important obstacles for the currently applied anti-cancer drug delivery systems. One is the conflict between long-circulation and cellular uptake while the other one is the achievement of ideal anti-cancer efficacy. To solve these problems, we designed a polypeptide-based micelle system that combined the advantages of receptor mediated endocytosis and multi-drug delivery. Firstly, an amphiphilic PLG- g -Ve/PEG graft copolymer was prepared by grafting α-tocopherol (Ve) and polyethylene glycol (PEG) to poly( l -glutamic acid) (PLG). Then docetaxel (DTX) and cisplatin (CDDP) were co-loaded into the PLG- g -Ve/PEG micelles via hydrophobic and chelation effect. After that, the surface of the dual-drug-loaded micelles was decorated with an α v β 3 integrin targeting peptide c(RGDfK). The targeted dual-drug-loaded micelles showed synergistic cytotoxicity and enhanced internalization rate in mouse melanoma (B16F1) cells. In vivo tests demonstrated that remarkable long circulation, anti-tumor and anti-metastasis efficacy could be achieved using this drug delivery system. This work revealed a strategy for the design and preparation of anti-cancer drug delivery systems with reduced side effect, enhanced anti-tumor and anti-metastasis efficacy.
研究领域:
药学
·
肿瘤学
·
生物材料
✓ 已验证
DOI
高影响因子
RSC Advances
·
2016
·Vol. 6
·期 48
·42109-42119
·
IF 3.289
Gang Pan,Yi-jie Bao,Jie Xu,Tao Liu,Cheng Liu,Yan-yan Qiu,Xiao-jing Shi,Hui Yu,Ting-ting Jia,Xia Yuan,Ze-ting Yuan,Pei-hao Yin,Yi-jun Cao
We report on the fabrication of a multifunctional polymeric prodrug covalently linked with an anticancer drug (bufalin, BUF) and tumor-targeting peptide (RGD) and investigate its anticancer performance against colon cancer in mice. The polymerizable monomer, 3-((2-(methacryloyloxy)ethyl) thio)propanoic acid (BSMA), was synthesized first. Atom radical transfer polymerization (ATRP) of BSMA and oligo(ethylene glycol) monomethyl ether methacrylate (OEGMA) afforded random copolymers, P(OEGMA-co-BSMA). The polymeric prodrug of BUF, P(OEGMA-co-BUF), was obtained by an esterification reaction between the carboxyl groups of P(OEGMA-co-BSMA) and the hydroxyl group of BUF. Finally, a tumor-targeting polymeric prodrug, P(OEGMA-co-BUF-co-RGD), was obtained via an aminolysis reaction of P(OEGMA-co-BUF) in the presence of RGD and the final drug content was determined to be ∼32.9 wt%. In aqueous media, P(OEGMA-co-BUF-co-RGD) self-assembles into micelles and the hydrodynamic diameter (Dh) of the micelles was determined to be ∼33.0 (±2.5) nm by dynamic laser light scattering (LLS). It was demonstrated that the tumor-targeting polymeric prodrug showed improved anticancer performance both in vitro and in vivo in comparison with that of free BUF.
研究领域:
药学
·
肿瘤学
·
生物材料
✓ 已验证
产品关联
DOI
高影响因子
DYES AND PIGMENTS
·
2017
·
IF 3.473
Yanhua Lai,Ping Zhao,Zhan Zhang,Bai Li,Junchen Wu
The self-assembled peptide cargo carrier with the ability of probe offered an effective strategy to deliver and track the anticancer drug, cisplatin (DDP) in ovarian cancer cells. This simple peptide system containing a pyrene fluorogen and arginine-glycine-aspartic acid (RGD) sequence could be utilized to release DDP in situ by the specific recognition between an RGD motif and α v β 3 integrin that was over-expressed on ovarian cancer cells. Importantly, we found that the disassembly-triggered peptide nanofibers , PA1, could effectively combine with DDP and release DDP in the cytoplasm with the pyrene fluorescence restoring. Moreover, the peptide cargo carrier efficiently penetrated tumour cells for enhancing therapeutic efficacy. Our system could open the door for the delivery of anticancer drug in cancer-related therapy.
研究领域:
生物化学
·
肿瘤学
·
药物递送系统
✓ 已验证
产品关联
DOI
高影响因子
ACS Applied Materials & Interfaces
·
2019
·
IF 8.456
Renuka Khatik,Zhengyun Wang,Debo Zhi,Sonia Kiran,Pankaj Dwivedi,Gaolin Liang,Bensheng Qiu,Qing Yang
Multifunctional nanomaterials with targeted imaging and chemotherapy have high demand with great challenge. Herein, we rationally aimed to design multifunctional drug delivery systems by RGD-modified chitosan (CH)-coated nanoneedles (NDs) of gadolinium arsenate (RGD-CH-Gd-AsNDs). These NDs have multifunctionality for imaging and targeted therapy. NDs on intravenous administration demonstrated significant accumulation of As ions/species in tumor tissues, which was monitored by the change in T1-weighted magnetic resonance (MR) imaging. Moreover, NDs were well opsonized in cells with high specificity, subsequently inducing apoptosis to the HepG2 cells. Consequent to this, the in vivo results demonstrated biosafety, enhanced tumor targeting, and tumor regression in a subcutaneously transplanted xenograft model in nude mice. These RGD-CH-Gd-AsNDs have great potential, and we anticipate that they could serve as a novel platform for real-time T1-weighted MR diagnosis and chemotherapy.
研究领域:
医学影像学
·
药物递送系统
·
肿瘤学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BIOMATERIALS
·
2020
·
IF 10.317
Jichun Yang,Shuojiong Pan,Shiqian Gao,Yiheng Dai,Huaping Xu
Thioredoxin reductase (TrxR) is an essential mammalian enzyme that possesses a selenocysteine active site. TrxR is overexpressed in many malignant tumors and has a close relationship with apoptosis, drug resistance, recurrence and metastasis of tumors. Recently, TrxR has emerged as a promising target for anticancer therapy. Herein, we developed a TrxR-interfering drug delivery system (DDS) based on RGD-PEG-PUSeSe-PEG-RGD self-assembling micelles for imaging-guided gemcitabine (GEM) chemosensitization and anti-recurrence/metastasis therapy. The diselenide-containing micelles were degraded in response to TrxR stimuli for GEM releasing. In the meantime, the dissociated polymers’ chain segments targeted the active site of TrxR via Se–Se/Se–S dynamic reactions for activity inhibition. This inhibition by the micelles not only provided chemosensitization, but reduced tumor recurrence/metastasis risk via the induction of residual tumor cell apoptosis by triggering ROS production post-chemotherapy. In this work, we took the transformation between Se-containing dynamic covalent bonds developed by our group from in vitro to in vivo , which furthered the knowledge on the biochemistry of selenium and provided aspects to develop new TrxR inhibitors. Overall, the TrxR-interfering DDS combined excellent antitumor effects for primary solid tumors with the inhibition of tumor recurrence/metastasis during post-treatment care, providing new perspectives for efficient cancer therapy.
研究领域:
癌症治疗
·
药学
·
生物化学
·
材料科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
MATERIALS & DESIGN
·
2021
·
IF 7.991
Yufei Liu,Long Yang,Guijing Chen,Zhentao Liu,Tao Lu,Yong Yang,Jia Yu,Dongdong Kang,Wei Yan,Min He,Shuhao Qin,Jie Yu,Chuan Ye,Heng Luo
Although microfiber (MF) loaded polypeptides have been widely studied in the field of medicine, load control and slow release remain significant challenges. Herein, polybutylene adipate terephthalate (PBAT) hollow porous MFs (HPMFs) were prepared by improving and regulating the groups and structures of the MFs to address these challenges. The capacity of the HPMFs for the loading of polypeptide can be improved. Measurements involving the use of X-ray photoelectron, energy-dispersive, and ultraviolet (UV) spectroscopies in conjunction with scanning electron microscopy measurements showed that the amount of polypeptide (arginylglycylaspartic acid, RGD) loaded on the HPMFs was significantly higher than that loaded on the MFs. Animal cell experiments revealed that PBAT grafted MAH has good bioactivity. By loading RGD onto HPMFs and MFs, RGD@HPMFs and RGD@MFs were obtained. A study on HeLa and A549 cancer cells showed that the inhibition rates of RGD@HPMFs were higher than that of RGD@MFs by 14.1% and 6.9%, respectively. The results obtained herein show that HPMF scaffold preparation by improving the material groups and regulating the structure of MFs can address the challenges associated with control of the load and sustained release of polypeptides and other drugs.
研究领域:
生物医学工程
·
材料科学
·
药物递送系统
✓ 已验证
DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2025
·
IF 5.2
Jing Wang,Congcong Lin,Xiaoyang Li,Junyao Wei,Yihua Wang,Rongtao Li,Yan Ming,Jingling Tang,Jiaxin Liu,Manjie Zhang,Hongyu Ji
Myocardial infarction (MI) is a leading cause of heart failure and death in cardiovascular diseases. Most drug trials currently fail due to inadequate local drug activity and side effects. In this study, we developed a novel polydopamine (PDA) nano delivery system that carries sodium ferulate (SF) and is modified with RGD peptides (SF/RGD-PDA NPs) for precise targeted delivery. SF is a clinical adjuvant for cardiovascular and cerebrovascular diseases but lacks targeting and has a short half-life. PDA, known for its excellent biocompatibility and surface modifiability, serves as an effective carrier. SF was loaded onto PDA through π-π stacking, while RGD was attached via a Michael addition reaction, resulting in stable SF/RGD-PDA NPs with an average particle size of 206.13 nm. In vitro and in vivo studies indicate that this targeted formulation has good safety. Targeting studies showed a 2.19-fold increase in nanoparticle accumulation in the heart and a 5.94-fold increase in cellular uptake efficiency. Pharmacodynamic studies revealed a 1.45-fold increase in endothelial cell proliferation, a 1.46-fold increase in angiogenesis rate, and a significant reduction in MI area. These findings suggest that SF/RGD-PDA NPs can improve endothelial cell function and reduce MI area through targeted delivery.
研究领域:
药学
·
心血管病学
·
纳米医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）