ArticleInternational journal of nanomedicine2011
RGD peptide-mediated chitosan-based polymeric micelles targeting delivery for integrin-overexpressing tumor cells.
Article in International journal of nanomedicine, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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Who cites it
27 citing papers in PubMed, 74 citations in OpenAlex.
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- Surfactant-Enabled Nanocarriers in Breast Cancer Therapy: Targeted Delivery and Multidrug Resistance Reversal.Pharmaceutics · 2025Review
- Recent Advances in Peptide-Functionalized Hydrogels for Bone Tissue Engineering.ACS biomaterials science & engineering · 2025Review
- Drug delivery strategy in hepatocellular carcinoma therapy.Cell communication and signaling : CCS · 2022Review
- RGD-Peptide Functionalization Affects theJournal of medicinal chemistry · 2021Article
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- Spontaneous and instant formation of highly stable protein-nanoparticle supraparticle co-assemblies driven by hydrophobic interaction.Nanoscale advances · 2019Article
- A Novel Solubility-Enhanced Rubusoside-Based Micelles for Increased Cancer Therapy.Nanoscale research letters · 2017Article
- Peptide-Mediated Tumor Targeting by a Degradable Nano Gene Delivery Vector Based on Pluronic-Modified Polyethylenimine.Nanoscale research letters · 2016Article
- Endocytosis in gene therapy with non-viral vectors.Wiener medizinische Wochenschrift (1946) · 2016Review
- Nanoparticles for targeted delivery of therapeutics and small interfering RNAs in hepatocellular carcinoma.World journal of gastroenterology · 2015Review
- In Vitro and In Vivo Efficacy of Self-Assembling RGD Peptide Amphiphiles for Targeted Delivery of Paclitaxel.Pharmaceutical research · 2015Article
- Active radar guides missile to its target: receptor-based targeted treatment of hepatocellular carcinoma by nanoparticulate systems.Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine · 2015Review
- Tumor targeting RGD conjugated bio-reducible polymer for VEGF siRNA expressing plasmid delivery.Biomaterials · 2014Article
- αCellular and molecular bioengineering · 2014Article
- Novel tumor-targeting, self-assembling peptide nanofiber as a carrier for effective curcumin delivery.International journal of nanomedicine · 2014Article
- Polysaccharide-based micelles for drug delivery.Pharmaceutics · 2013Article
- An RGD-modified MRI-visible polymeric vector for targeted siRNA delivery to hepatocellular carcinoma in nude mice.PloS one · 2013Article
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundSolid tumors need new blood vessels to feed and nourish them as well as to allow tumor cells to escape into the circulation and lodge in other organs, which is termed "angiogenesis." Some tumor cells within solid tumors can overexpress integrins α(v)β(3) and α(v)β(5), which can specifically recognize the peptide motif Arg-Gly-Asp (RGD). Thus, the targeting of RGD-modified micelles to tumor vasculature is a promising strategy for tumor-targeting treatment.
methodsRGD peptide (GSSSGRGDSPA) was coupled to poly(ethylene glycol)-modified stearic acid-grafted chitosan (PEG-CS-SA) micelles via chemical reaction in the presence of N,N'-Disuccinimidyl carbonate. The critical micelle concentration of the polymeric micelles was determined by measuring the fluorescence intensity of pyrene as a fluorescent probe. The micelle size, size distribution, and zeta potential were measured by light scattering and electrophoretic mobility. Doxorubicin (DOX) was chosen as a model anticancer drug to investigate the drug entrapment efficiency, in vitro drug-release profile, and in vitro antitumor activities of drug-loaded RGD-PEG-CS-SA micelles in cells that overexpress integrins (α(ν)β(3) and α(ν)β(5)) and integrin-deficient cells.
resultsUsing DOX as a model drug, the drug encapsulation efficiency could reach 90%, and the in vitro drug-release profiles suggested that the micelles could be used as a controlled-release carrier for the hydrophobic drug. Qualitative and quantitative analysis of cellular uptake indicated that RGD-modified micelles could significantly increase the DOX concentration in integrin-overexpressing human hepatocellular carcinoma cell line (BEL-7402), but not in human epithelial carcinoma cell line (Hela). The competitive cellular-uptake test showed that the cellular uptake of RGD-modified micelles in BEL-7402 cells was significantly inhibited in the presence of excess free RGD peptides. In vitro cytotoxicity tests demonstrated DOX-loaded RGD-modified micelles could specifically enhance the cytotoxicity against BEL-7402 compared with DOX-loaded PEG-CS-SA and doxorubicin hydrochlorate.
conclusionThis study suggests that RGD-modified PEG-CS-SA micelles are promising drug carriers for integrin-overexpressing tumor active targeting therapy.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.