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Internally Cationic Polyamidoamine PAMAM-OH Dendrimers for siRNA Delivery: Effect of the Degree of Quaternization and Cancer Targeting
Open accessAbstract
A novel cancer targeted, internally cationic and surface neutral polyamidoamine (PAMAM) dendrimer, was designed, synthesized, and evaluated as a nanocarrier for the targeted intracellular delivery of siRNA. The dendrimer contained a synthetic analog of Luteinizing hormone-releasing hormone as cancer targeting moiety. The proposed delivery system possesses the following advantages: (1) internal cationic charges for complexation with siRNA and enhanced siRNA protection; (2) low cytotoxicity; (3) lesser degree of quaternization offering free tertiary amines for potential proton sponge effect; and (4) targeting specifically to cancer cells for enhancing siRNA uptake and efficiency and potential limitation of adverse side effects of chemotherapy on healthy organs. Both nontargeted and targeted dendrimer-siRNA complexes formed compact nanometer size spherical particles, exhibited very low cytotoxicity even at the higher concentration, and efficiently penetrated cancer cells in vitro. However, only the targeted dendrimer-siRNA complex was able to substantially decrease the expression of a targeted BCL2 gene.
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Stoscheck, C. M. (1990) · Methods in Enzymology · doi:10.1016/0076-6879(90)82008-p · Cited by 1,438
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Canton, I., & Battaglia, G. (2012) · Chemical Society Reviews · doi:10.1039/c2cs15309b · Cited by 936
Dendrimers as Nanocarriers for Nucleic Acid and Drug Delivery in Cancer Therapy
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Surface-Engineered Dendrimers in Gene Delivery
Yang, J., Zhang, Q., Chang, H., & Cheng, Y. (2015) · Chemical Reviews · doi:10.1021/cr500542t · Cited by 429
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Metadata
- Authors
- Patil, M. L., Zhang, M., Taratula, O., Garbuzenko, O. B., He, H., & Minko, T.
- Venue
- Biomacromolecules
- Publisher
- American Chemical Society (ACS)
- Published
- 2009-01-21
- Volume
- 10
- Issue
- 2
- Pages
- 258-266
- ISSN
- 1525-7797 (ISSN-L)
- 1526-4602
- OpenAlex
- W1995953743
- Cited by
- 213
- References
- 1
- FWCI
- 18.95
- Type
- journal article
- Language
- en
- Open access
- green
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- Patil, M. L., Zhang, M., Taratula, O., Garbuzenko, O. B., He, H., & Minko, T. (2009). Internally Cationic Polyamidoamine PAMAM-OH Dendrimers for siRNA Delivery: Effect of the Degree of Quaternization and Cancer Targeting. Biomacromolecules. https://doi.org/10.1021/bm8009973
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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