ArticleBioconjugate chemistry2013
Neutral polymeric micelles for RNA delivery.
Article in Bioconjugate chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 47 citations in OpenAlex.
- Covalent Polymer-RNA Conjugates for Potent Activation of the RIG-I Pathway.Advanced healthcare materials · 2025Article
- Article
- Nonviral delivery systems for antisense oligonucleotide therapeutics.Biomaterials research · 2022Review
- Charge-Conversion Strategies for Nucleic Acid Delivery.Advanced functional materials · 2021Article
- pH-Responsive Amphiphilic Carboxylate Polymers: Design and Potential for Endosomal Escape.Frontiers in chemistry · 2021Review
- Structural Optimization of Polymeric Carriers to Enhance the Immunostimulatory Activity of Molecularly Defined RIG-I Agonists.ACS central science · 2020Article
- Let-7 miRNA and CDK4 siRNA co-encapsulated in Herceptin-conjugated liposome for breast cancer stem cells.Asian journal of pharmaceutical sciences · 2020Article
- Highly efficient gene release in spatiotemporal precision approached by light and pH dual responsive copolymers.Chemical science · 2019Article
- Targeted mRNA Therapy for Ornithine Transcarbamylase Deficiency.Molecular therapy : the journal of the American Society of Gene Therapy · 2018Article
- Enzyme-Cleavable Polymeric Micelles for the Intracellular Delivery of Proapoptotic Peptides.Molecular pharmaceutics · 2017Article
- Covalent nano delivery systems for selective imaging and treatment of brain tumors.Advanced drug delivery reviews · 2017Review
- Design of smart HPMA copolymer-based nanomedicines.Journal of controlled release : official journal of the Controlled Release Society · 2016Review
- Antibody targeting facilitates effective intratumoral siRNA nanoparticle delivery to HER2-overexpressing cancer cells.Oncotarget · 2016Article
- Dynamic intracellular delivery of antibiotics via pH-responsive polymersomes.Polymer chemistry · 2015Article
- Neutral polymer micelle carriers with pH-responsive, endosome-releasing activity modulate antigen trafficking to enhance CD8(+) T cell responses.Journal of controlled release : official journal of the Controlled Release Society · 2014Article
- Macromolecular therapeutics.Journal of controlled release : official journal of the Controlled Release Society · 2014Review
- Translating materials design to the clinic.Nature materials · 2013Article
- Advancing polymeric delivery systems amidst a nucleic acid therapy renaissance.ACS macro letters · 2013Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
RNA interference (RNAi) drugs have significant therapeutic potential, but delivery systems with appropriate efficacy and toxicity profiles are still needed. Here, we describe a neutral, ampholytic polymeric delivery system based on conjugatable diblock polymer micelles. The diblock copolymer contains a hydrophilic poly[N-(2-hydroxypropyl)methacrylamide-co-N-(2-(pyridin-2-yldisulfanyl)ethyl)methacrylamide) (poly[HPMA-co-PDSMA]) segment to promote aqueous stability and facilitate thiol-disulfide exchange reactions and a second ampholytic block composed of propylacrylic acid (PAA), dimethylaminoethyl methacrylate (DMAEMA), and butyl methacrylate (BMA). The poly[(HPMA-co-PDSMA)-b-(PAA-co-DMAEMA-co-BMA)] was synthesized using reversible addition-fragmentation chain transfer (RAFT) polymerization with an overall molecular weight of 22 000 g/mol and a PDI of 1.88. Dynamic light scattering and fluorescence measurements indicated that the diblock copolymers self-assemble under aqueous conditions to form polymeric micelles with a hydrodynamic radius and critical micelle concentration of 25 nm and 25 μg/mL, respectively. Red blood cell hemolysis experiments show that the neutral hydrophilic micelles have potent membrane destabilizing activity at endosomal pH values. Thiolated siRNA targeting glyceraldehyde 3-phosphate dehydrogenase (GAPDH) was directly conjugated to the polymeric micelles via thiol exchange reactions with the pyridal disulfide groups present in the micelle corona. Maximum silencing activity in HeLa cells was observed at a 1:10 molar ratio of siRNA to polymer following a 48 h incubation period. Under these conditions 90% mRNA knockdown and 65% protein knockdown at 48 h was achieved with negligible toxicity. In contrast the polymeric micelles lacking a pH-responsive endosomalytic segment demonstrated negligible mRNA and protein knockdown under these conditions. The potent mRNA knockdown and excellent biocompatibility of the neutral siRNA conjugates demonstrate the potential utility of this carrier design for delivering therapeutic siRNA drugs.
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Registered trials
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.