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Nanomaterials 2018, 8(3), 131;

Enhanced Delivery of Therapeutic siRNA into Glioblastoma Cells Using Dendrimer-Entrapped Gold Nanoparticles Conjugated with β-Cyclodextrin

Department of Radiology, Shanghai Tenth People’s Hospital, Tongji University School of Medicine, Shanghai 200072, China
College of Chemistry, Chemical Engineering and Biotechnology, Donghua University, Shanghai 201620, China
Université Paris Descartes, PRES Sorbonne Paris Cité, CNRS UMR 860, Laboratoire de Chimie et de Biochimie Pharmacologiques et Toxicologique, 45, rue des Saints Peres, 75006 Paris, France
CQM—Centro de Química da Madeira, MMRG, Universidade da Madeira, Campus da Penteada, 9020-105 Funchal, Portugal
Laboratoire de Chimie de Coordination du CNRS, 205 Route de Narbonne, BP 44099, 31077 Toulouse CEDEX 4, France
Université de Toulouse, UPS, INPT, 31077 Toulouse CEDEX 4, France
Authors to whom correspondence should be addressed.
Received: 8 January 2018 / Revised: 28 January 2018 / Accepted: 29 January 2018 / Published: 27 February 2018
(This article belongs to the Special Issue Nanocolloids for Nanomedicine and Drug Delivery)
Full-Text   |   PDF [5449 KB, uploaded 27 February 2018]   |  


We describe a safe and highly effective non-viral vector system based on β-cyclodextrin (β-CD)-modified dendrimer-entrapped gold nanoparticles (Au DENPs) for improved delivery small interfering RNA (siRNA) to glioblastoma cells. In our approach, we utilized amine-terminated generation 5 poly(amidoamine) dendrimers partially grafted with β-CD as a nanoreactor to entrap Au NPs. The acquired β-CD-modified Au DENPs (Au DENPs-β-CD) were complexed with two different types of therapeutic siRNA (B-cell lymphoma/leukemia-2 (Bcl-2) siRNA and vascular endothelial growth factor (VEGF) siRNA). The siRNA compression ability of the Au DENPs-β-CD was evaluated by various methods. The cytocompatibility of the vector/siRNA polyplexes was assessed by viability assay of cells. The siRNA transfection capability of the formed Au DENPs-β-CD vector was evaluated by flow cytometric assay of the cellular uptake of the polyplexes and Western blot assays of the Bcl-2 and VEGF protein expression. Our data reveals that the formed Au DENPs-β-CD carrier enables efficiently delivery of siRNA to glioma cells, has good cytocompatibility once complexed with the siRNA, and enables enhanced gene silencing to inhibit the expression of Bcl-2 and VEGF proteins. The developed Au DENPs-β-CD vector may be used for efficient siRNA delivery to different biosystems for therapeutic purposes. View Full-Text
Keywords: PAMAM dendrimers; β-CD; gold nanoparticles; gene silencing; siRNA PAMAM dendrimers; β-CD; gold nanoparticles; gene silencing; siRNA

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Qiu, J.; Kong, L.; Cao, X.; Li, A.; Wei, P.; Wang, L.; Mignani, S.; Caminade, A.-M.; Majoral, J.-P.; Shi, X. Enhanced Delivery of Therapeutic siRNA into Glioblastoma Cells Using Dendrimer-Entrapped Gold Nanoparticles Conjugated with β-Cyclodextrin. Nanomaterials 2018, 8, 131.

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