Delivery materials for siRNA therapeutics

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Maximizing the potency of siRNA lipid nanoparticles for hepatic gene silencing in vivo

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Potent and persistent in vivo anti-HBV activity of chemically modified siRNAs

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A combinatorial library of lipid-like materials for delivery of RNAi therapeutics

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Mechanism of DNA Release from Cationic Liposome/DNA Complexes Used in Cell Transfection,

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Recognizing and avoiding siRNA off-target effects for target identification and therapeutic application

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Tumor-Selective Delivery of Macromolecular Drugs via the EPR Effect: Background and Future Prospects

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The First Targeted Delivery of siRNA in Humans via a Self-Assembling, Cyclodextrin Polymer-Based Nanoparticle: From Concept to Clinic

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Mechanisms and optimization of in vivo delivery of lipophilic siRNAs

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Lipid-like materials for low-dose, in vivo gene silencing

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Impact of tumor-specific targeting on the biodistribution and efficacy of siRNA nanoparticles measured by multimodality in vivo imaging

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PEGylation significantly affects cellular uptake and intracellular trafficking of non-viral gene delivery particles

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First-in-Humans Trial of an RNA Interference Therapeutic Targeting VEGF and KSP in Cancer Patients with Liver Involvement

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Microfluidic Synthesis of Highly Potent Limit-size Lipid Nanoparticles for In Vivo Delivery of siRNA

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Dynamic PolyConjugates for targeted in vivo delivery of siRNA to hepatocytes

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Stealth Me. PEG‐PLA Nanoparticles Avoid Uptake by the Mononuclear Phagocytes System

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Resolution of liver cirrhosis using vitamin A–coupled liposomes to deliver siRNA against a collagen-specific chaperone

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Insights into the kinetics of siRNA-mediated gene silencing from live-cell and live-animal bioluminescent imaging

Bartlett, D. W. (2006) · Nucleic Acids Research · doi:10.1093/nar/gkj439 · Cited by 601

On the mechanism whereby cationic lipids promote intracellular delivery of polynucleic acids

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Systemic administration of optimized aptamer-siRNA chimeras promotes regression of PSMA-expressing tumors

Dassie, J. P., Liu, X., Thomas, G. S., Whitaker, R. M., Thiel, K. W., Stockdale, K. R., Meyerholz, D. K., McCaffrey, A. P., McNamara, J. O., & Giangrande, P. H. (2009) · Nature Biotechnology · doi:10.1038/nbt.1560 · Cited by 600

In vivo activity of nuclease-resistant siRNAs

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Sequence-Specific Knockdown of EWS-FLI1 by Targeted, Nonviral Delivery of Small Interfering RNA Inhibits Tumor Growth in a Murine Model of Metastatic Ewing's Sarcoma

Hu‐Lieskovan, S., Heidel, J. D., Bartlett, D. W., Davis, M. E., & Triche, T. J. (2005) · Cancer Research · doi:10.1158/0008-5472.can-05-0565 · Cited by 568

Sheddable Coatings for Long-Circulating Nanoparticles

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Current progress of siRNA/shRNA therapeutics in clinical trials

Burnett, J., Rossi, J. J., & Tiemann, K. (2011) · Biotechnology Journal · doi:10.1002/biot.201100054 · Cited by 452

Folate-targeted therapies for cancer

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Thermodynamically stable RNA three-way junction for constructing multifunctional nanoparticles for delivery of therapeutics

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Administration in non-human primates of escalating intravenous doses of targeted nanoparticles containing ribonucleotide reductase subunit M2 siRNA

Heidel, J. D., Yu, Z., Liu, J. Y.-C., Rele, S. M., Liang, Y., Zeidan, R. K., Kornbrust, D. J., & Davis, M. E. (2007) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0701458104 · Cited by 390

Stimuli-responsive polymers and nanomaterials for gene delivery and imaging applications

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Rapid discovery of potent siRNA-containing lipid nanoparticles enabled by controlled microfluidic formulation.

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Polycation-siRNA nanoparticles can disassemble at the kidney glomerular basement membrane

Zuckerman, J. E., Choi, C. H. J., Han, H., & Davis, M. E. (2012) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1200718109 · Cited by 379

A review of nanocarriers for the delivery of small interfering RNA

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Transferrin-Containing, Cyclodextrin Polymer-Based Particles for Tumor-Targeted Gene Delivery

Bellocq, N. C., Pun, S. H., Jensen, G. S., & Davis, M. E. (2003) · Bioconjugate Chemistry · doi:10.1021/bc034125f · Cited by 350

siRNA Conjugate Delivery Systems

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Efficient In Vivo Delivery of siRNA to the Liver by Conjugation of α-Tocopherol

Nishina, K., Unno, T., Uno, Y., Kubodera, T., Kanouchi, T., Mizusawa, H., & Yokota, T. (2008) · Molecular Therapy · doi:10.1038/mt.2008.14 · Cited by 323

Nephrin strands contribute to a porous slit diaphragm scaffold as revealed by electron tomography

Wartiovaara, J., Öfverstedt, L., Khoshnoodi, J., Zhang, J., Mäkelä, E., Sandin, S., Ruotsalainen, V., Cheng, R. H., Jalanko, H., Skoglund, U., et al. (2004) · Journal of Clinical Investigation · doi:10.1172/jci22562 · Cited by 318

New Class of Polymers for the Delivery of Macromolecular Therapeutics

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A pH-sensitive cationic lipid facilitates the delivery of liposomal siRNA and gene silencing activity in vitro and in vivo

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Cyclodextrin-Modified Polyethylenimine Polymers for Gene Delivery

Pun, S. H., Bellocq, N. C., Liu, A., Jensen, G., Machemer, T., Quijano, E., Schluep, T., Wen, S.-F., Engler, H., Heidel, J. D., et al. (2004) · Bioconjugate Chemistry · doi:10.1021/bc049891g · Cited by 297

ISG15 inhibits Ebola VP40 VLP budding in an L-domain-dependent manner by blocking Nedd4 ligase activity

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Hepatocyte-targeted RNAi Therapeutics for the Treatment of Chronic Hepatitis B Virus Infection

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Action and Reaction: The Biological Response to siRNA and Its Delivery Vehicles

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The size of endothelial fenestrae in human liver sinusoids: implications for hepatocyte-directed gene transfer

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Physicochemical and Biological Characterization of Targeted, Nucleic Acid-Containing Nanoparticles

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Nonbilayer phase of lipoplex–membrane mixture determines endosomal escape of genetic cargo and transfection efficiency

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An Aptamer-siRNA Chimera Suppresses HIV-1 Viral Loads and Protects from Helper CD4 + T Cell Decline in Humanized Mice

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Determination of the Upper Size Limit for Uptake and Processing of Ligands by the Asialoglycoprotein Receptor on Hepatocytesin Vitro and in Vivo

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Development of a Nonviral Gene Delivery Vehicle for Systemic Application

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Effects of Structure of β-Cyclodextrin-Containing Polymers on Gene Delivery

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Polymers in Small-Interfering RNA Delivery

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Silencing or Stimulation? siRNA Delivery and the Immune System

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Targeted Delivery of PLK1-siRNA by ScFv Suppresses Her2 + Breast Cancer Growth and Metastasis

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In vivo pharmacokinetics, tissue distribution and underlying mechanisms of various PEI(–PEG)/siRNA complexes

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Nanovector delivery of siRNA for cancer therapy

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In vivo delivery of RNAi with lipid-based nanoparticles

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Tunable pH-Sensitive Liposomes Composed of Mixtures of Cationic and Anionic Lipids

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Impact of tumor‐specific targeting and dosing schedule on tumor growth inhibition after intravenous administration of siRNA‐containing nanoparticles

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Endosomolysis by Masking of a Membrane-Active Agent (EMMA) for Cytoplasmic Release of Macromolecules

Rozema, D. B., Ekena, K., Lewis, D. L., Loomis, A. G., & Wolff, J. A. (2002) · Bioconjugate Chemistry · doi:10.1021/bc0255945 · Cited by 161

Targeted Delivery Systems for Oligonucleotide Therapeutics

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Elimination Pathways of Systemically Delivered siRNA

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Synthesis of Cluster Galactosides with High Affinity for the Hepatic Asialoglycoprotein Receptor

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Update on the glomerular filtration barrier

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Inhibition of protein kinase C by cationic amphiphiles

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Self-Assembling Nucleic Acid Delivery Vehicles via Linear, Water-Soluble, Cyclodextrin-Containing Polymers

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Structural Effects of Carbohydrate-Containing Polycations on Gene Delivery. 1. Carbohydrate Size and Its Distance from Charge Centers

Reineke, T. M., & Davis, M. E. (2002) · Bioconjugate Chemistry · doi:10.1021/bc025592k · Cited by 119

Imidazole groups on a linear, cyclodextrin-containing polycation produce enhanced gene delivery via multiple processes

Mishra, S., Heidel, J. D., Webster, P. C., & Davis, M. E. (2006) · Journal of Controlled Release · doi:10.1016/j.jconrel.2006.06.018 · Cited by 115

Effect of PEGylation on Biodistribution and Gene Silencing of siRNA/Lipid Nanoparticle Complexes

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Structural Effects of Carbohydrate-Containing Polycations on Gene Delivery. 3. Cyclodextrin Type and Functionalization

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Comparison of Cationic and Amphipathic Cell Penetrating Peptides for siRNA Delivery and Efficacy

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Lipid-derived nanoparticles for immunostimulatory RNA adjuvant delivery

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Co-Injection of a Targeted, Reversibly Masked Endosomolytic Polymer Dramatically Improves the Efficacy of Cholesterol-Conjugated Small Interfering RNAs In Vivo

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Lateral Organization of Liquid-Crystalline Cholesterol-Dimyristoylphosphatidylcholine Bilayers. Evidence for Domains with Hexagonal and Centered Rectangular Cholesterol Superlattices

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Folate-linked lipid-based nanoparticles for synthetic siRNA delivery in KB tumor xenografts

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Ionization Behavior of Amino Lipids for siRNA Delivery: Determination of Ionization Constants, SAR, and the Impact of Lipid pKa on Cationic Lipid−Biomembrane Interactions

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Design and Synthesis of Novel N-Acetylgalactosamine-Terminated Glycolipids for Targeting of Lipoproteins to the Hepatic Asialoglycoprotein Receptor

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