ArticlePharmaceutical research2004
Evaluation of generation 2 and 3 poly(propylenimine) dendrimers for the potential cellular delivery of antisense oligonucleotides targeting the epidermal growth factor receptor.
Article in Pharmaceutical research, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 83 citations in OpenAlex.
- Synthetic-polymer-assisted antisense oligonucleotide delivery: targeted approaches for precision disease treatment.Beilstein journal of nanotechnology · 2025Review
- Stimuli-responsive chitosan-based nanocarriers for cancer therapy.BioImpacts : BI · 2017Review
- Network of nanomedicine researches: impact of Iranian scientists.BioImpacts : BI · 2015Article
- Nanotoxicity: a key obstacle to clinical translation of siRNA-based nanomedicine.Nanomedicine (London, England) · 2014Review
- Intrinsic bio-signature of gene delivery nanocarriers may impair gene therapy goals.BioImpacts : BI · 2013Article
- Translational Approaches towards Cancer Gene Therapy: Hurdles and Hopes.BioImpacts : BI · 2012Article
- Radiolabeled oligonucleotides for antisense imaging.Current organic synthesis · 2011Article
- Lipid and polymeric carrier-mediated nucleic acid delivery.Expert opinion on drug delivery · 2010Review
- Release profile and stability evaluation of optimized chitosan/alginate nanoparticles as EGFR antisense vector.International journal of nanomedicine · 2010Article
- Physicochemical and biological properties of self-assembled antisense/poly(amidoamine) dendrimer nanoparticles: the effect of dendrimer generation and charge ratio.International journal of nanomedicine · 2010Article
- Triazine dendrimers as nonviral gene delivery systems: effects of molecular structure on biological activity.Bioconjugate chemistry · 2009Article
- Interactive Design Strategy for a Multi-Functional PAMAM Dendrimer-Based Nano-Therapeutic Using Computational Models and Experimental Analysis.Journal of computational and theoretical nanoscience · 2009Article
- Toxicogenomics to improve comprehension of the mechanisms underlying responses of in vitro and in vivo systems to nanomaterials: a review.Current genomics · 2008Article
- RNAi for treating hepatitis B viral infection.Pharmaceutical research · 2008Review
- Hydrophobization and bioconjugation for enhanced siRNA delivery and targeting.RNA (New York, N.Y.) · 2007Review
- Encapsulation of nucleic acids and opportunities for cancer treatment.Pharmaceutical research · 2007Review
- Understanding specific and nonspecific toxicities: a requirement for the development of dendrimer-based pharmaceuticals.Wiley interdisciplinary reviews. Nanomedicine and nanobiotechnologyReview
Corrections and comments
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Authors and funding
7 authors at 6 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTo evaluate low generation, G2 and G3, poly(propylenimine) dendrimers for the potential cellular delivery of antisense oligonucleotides (ODNs) targeting the epidermal growth factor receptor (EGFR) in A431 epidermoid carcinoma cells.
methodsCell cytotoxicity of the dendrimers was evaluated using trypan blue exclusion assays. Cellular uptake studies of fluorescently labeled ODNs were performed using fluorescence-activated cell sorting analysis. Intracellular fate of dendrimer-delivered ODNs was assessed in both fixed and live cells using fluorescent microscopy. Antisense ODN activity was assessed in terms of cancer cell growth, inhibition of target EGFR protein, and reduction in mRNA levels.
resultsG2 dendrimer (DAB-8) was less toxic than G3 (DAB-16) dendrimer in A431 cells, with IC50 of >175 and approximately 30 microg/ml, respectively. Uptake of fluorescently labeled ODN:dendrimer complexes was increased by up to 100-fold compared to a marker of fluid-phase endocytosis and up to 9-fold over free ODN at the optimal dendrimer:ODN (w/w) ratio of 5:1. Uptake of dendrimer:ODN complexes was significantly reduced at 4 degrees C (p < 0.05). Live cell fluorescent microscopy resulted in an intracellular distribution of dendrimer:ODN complexes that was suggestive of endocytic uptake; in contrast, cell fixation resulted in an artefactual nuclear localization. Treatment of A431 cells with anti-EGFR antisense ODN:dendrimer complexes inhibited cell growth, protein, and mRNA expression to levels comparable to Oligofectamine-mediated delivery.
conclusionsG2 and G3 poly(propylenimine) dendrimers markedly improved the delivery and activity of ODNs and thus may represent general reagents for the delivery of ODNs to cells in culture.
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