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Impact of the Structure of Biocompatible Aliphatic Polycarbonates on siRNA Transfection Ability.
Abstract RNAi therapeutics are promising therapeutic tools that have sparked the interest of many researchers. In an effort to provide a safe alternative to PEI, we have designed a series of new guanidinium and/or morpholino functionalized biocompatible and biodegradable polycarbonate vectors. The impact of different functions (morpholino-, guanidinium-, hydrophobic groups), of the architecture (linear homopolymer to dumbbell-shape) and of the molecular weight of these copolymers on their capacity to form polyplexes and to decrease the expression of two epigenetic regulators of gene expression, HDAC7 and HDAC5 was...
Source: Biomacromolecules - January 20, 2015 Category: Biochemistry Authors: Frère A, Kawalec M, Tempelaar S, Peixoto P, Hendrick E, Peulen O, Evrard B, Dubois P, Mespouille L, Mottet D, Piel G Tags: Biomacromolecules Source Type: research

Synthesis of Poly(meth)acrylates with Thioether and Tertiary Sulfonium Groups by ARGET ATRP and Their Use as siRNA Delivery Agents.
Abstract The field of RNA interference depends on the development of safe and efficient carriers for short interfering ribonucleic acid (siRNA) delivery. Conventional cationic monomers for siRNA delivery have utilized the nitrogen heteroatom to produce cationic charges. Here, we polymerized cationic sulfonium (meth)acrylate by activators regenerated by electron transfer (ARGET) atom transfer radical polymerization (ATRP) to form polymers with narrow molecular weight distributions for siRNA delivery. The tertiary sulfonium species was stable toward dealkylation in water but less stable in the polar aprotic solvent ...
Source: Biomacromolecules - December 17, 2014 Category: Biochemistry Authors: Mackenzie MC, Shrivats AR, Konkolewicz D, Averick SE, McDermott MC, Hollinger JO, Matyjaszewski K Tags: Biomacromolecules Source Type: research

Dual MMP7-Proximity-Activated and Folate Receptor-Targeted Nanoparticles for siRNA Delivery.
Abstract A dual-targeted siRNA nanocarrier has been synthesized and validated that is selectively activated in environments where there is colocalization of two breast cancer hallmarks, elevated matrix metalloproteinase (MMP) activity and folate receptor overexpression. This siRNA nanocarrier is self-assembled from two polymers containing the same pH-responsive, endosomolytic core-forming block but varying hydrophilic, corona-forming blocks. The corona block of one polymer consists of a 2 kDa PEG attached to a distal folic acid (FA); the second polymer contains a larger (Y-shaped, 20 kDa) PEG attached to the core ...
Source: Biomacromolecules - November 21, 2014 Category: Biochemistry Authors: Li H, Miteva M, Kirkbride KC, Cheng MJ, Nelson CE, Simpson EM, Gupta MK, Duvall CL, Giorgio TD Tags: Biomacromolecules Source Type: research

Size-Dependent Knockdown Potential of siRNA-Loaded Cationic Nanohydrogel Particles.
Abstract To overcome the poor pharmacokinetic conditions of short double-stranded RNA molecules in RNA interference therapies, cationic nanohydrogel particles can be considered as alternative safe and stable carriers for oligonucleotide delivery. For understanding key parameters during this process, two different types of well-defined cationic nanohydrogel particles were synthesized, which provided nearly identical physicochemical properties with regards to their material composition and resulting siRNA loading characteristics. Yet, according to the manufacturing process using amphiphilic reactive ester block copo...
Source: Biomacromolecules - October 22, 2014 Category: Biochemistry Authors: Nuhn L, Tomcin S, Miyata K, Mailänder V, Landfester K, Kataoka K, Zentel R Tags: Biomacromolecules Source Type: research

Amphipathic Homopolymers for siRNA Delivery: Probing Impact of Bifunctional Polymer Composition on Transfection.
In this study, we systematically explore the influence of the lipophilic group on the siRNA transfection properties of the polycationic-based delivery vectors. For this, a novel and modular synthetic strategy was developed for the preparation of polymers carrying a cationic site and a lipophilic group at each polymer repeat unit. These bifunctional polymers could form a complex with siRNA and deliver it to human colon carcinoma cells (HT-29-luc). In general, transfection capability increased with an increase in the chain length of the lipophilic moiety. The best transfection agent, a polymer containing ammonium groups and ...
Source: Biomacromolecules - April 22, 2014 Category: Biochemistry Authors: Buerkli C, Lee SH, Moroz E, Stuparu MC, Leroux JC, Khan A Tags: Biomacromolecules Source Type: research

Aggregation Behavior of Cationic Nanohydrogel Particles in Human Blood Serum.
Abstract For systemic siRNA delivery applications, well-defined drug carriers are required that guarantee stability for both carrier and cargo. Among various concepts progressing in market or final development, cationic nanohydrogel particles may serve as novel transport media especially designed for siRNA-in vivo experiments. In this work, the interaction of nanohydrogel particles with proteins and serum components was studied via dynamic light scattering in human blood serum as novel screening method prior to applications in vivo. The formation of larger aggregates mostly caused by charge interaction with albumi...
Source: Biomacromolecules - April 3, 2014 Category: Biochemistry Authors: Nuhn L, Gietzen S, Mohr K, Fischer K, Toh K, Miyata K, Matsumoto Y, Kataoka K, Schmidt M, Zentel R Tags: Biomacromolecules Source Type: research

Smurf1 knocked-down, mesenchymal stem cells and BMP-2 in an electrospun system for bone regeneration.
Abstract A sandwich-like system, fabricated with electrospun, poly (lactic-co-glycolic-acid) (PLGA) membranes incorporating either human recombinant bone morphogenetic protein 2 (BMP-2) enriched microspheres, rat bone marrow mesenchymal stem cells (rMSC), or rMSC with their Smurf1 (Smad Ubiquitin Regulatory Factor-1) expression knocked down by means of siRNA (rMSC573) at varying densities was evaluated in a rat calvarial, critical-size defect. The behavior of four membrane varieties, fabricated with different PLGA copolymers, was initially studied in rMSC cultures to decide on optimal membrane degradation and cell...
Source: Biomacromolecules - February 22, 2014 Category: Biochemistry Authors: Rodriguez-Evora M, García-Pizarro E, Del Rosario C, Perez-Lopez J, Reyes R, Delgado A, Rodriguez-Rey JC, Evora C Tags: Biomacromolecules Source Type: research

The influence of oligospermine architecture on their suitability for siRNA delivery.
Abstract Spermines are naturally abundant polyamines, which partially condense nucleic acids and exhibit the "proton-sponge effect" in an acidic environment. However, spermine shows limited transfection efficiency of nucleic acids due to its low molecular weight. Therefore, spermines need to be modified to be used as non-viral vectors for nucleic acids. Here, we synthesized linear bisspermine, and linear and dendritic tetraspermine with different molecular architecture. These oligospermines have been self-assembled into polyplexes with siRNA. The structure-activity relationship of the oligospermines was evaluated ...
Source: Biomacromolecules - February 19, 2014 Category: Biochemistry Authors: Elsayed M, Corrand V, Kolhatkar V, Xie Y, Kim NH, Kolhatkar R, Merkel OM Tags: Biomacromolecules Source Type: research

RVG peptide-linked trimethylated chitosan for delivery of siRNA to the brain.
Abstract In this work, a peptide derived from the rabies virus glycoprotein (RVG) was linked to siRNA/trimethylated chitosan (TMC) complexes through bifunctional PEG for efficient brain-targeted delivery of siRNA. The physiochemical properties of the complexes, such as siRNA complexing ability, size and zeta potential, morphology, serum stability and cytotoxicity, were investigated prior to studying the cellular uptake, in vitro gene silencing efficiency and in vivo biodistribution. The RVG peptide-linked siRNA/TMC-PEG complexes showed increased serum stability, negligible cytotoxicity and higher cellular uptake t...
Source: Biomacromolecules - February 18, 2014 Category: Biochemistry Authors: Gao Y, Wang Z, Zhang J, Zhang Y, Huo H, Wang T, Jiang T, Wang S Tags: Biomacromolecules Source Type: research

Cationic Dendron-Bearing Lipids: Investigating Structure-Activity Relationships for Small Interfering RNA Delivery.
Abstract A new family of cationic dendron-bearing lipids (CDLs) with poly(amidoamine) dendrons of first to third generation (named as A1, A2 and A3, respectively) was synthesized through a synthesis approach that permits facile variation of chemical structures. All the CDLs could effectively bind small interfering RNA (siRNA) to form complexes confirmed by gel retardation analysis. In in vitro transfection experiments, A1/siRNA complexes exhibited significant gene silencing efficiency close to LipofectamineTM 2000/siRNA complexes and much higher than A2/siRNA and A3/siRNA complexes. To reveal the underlying reason...
Source: Biomacromolecules - October 21, 2013 Category: Biochemistry Authors: Zhang Y, Chen J, Xiao C, Li M, Tian H, Chen X Tags: Biomacromolecules Source Type: research

Assessment of Cholesterol-Derived Ionic Copolymers as Potential Vectors for Gene Delivery.
Abstract A library of cholesterol-derived ionic copolymers were synthesized via reversible addition fragmentation chain transfer (RAFT) polymerization as 'smart' gene delivery vehicles holding diverse surface charges. Polyplex systems formed with anionic poly(methacrylic acid-co-cholesteryl methacrylate P(MAA-co-CMA) and cationic poly(dimethylamino ethyl methacrylate-co-cholesteryl methacrylate Q-P(DMAEMA-co-CMA) copolymer series were evaluated for their therapeutic efficiency. Cell viability assays, conducted on SHEP, HepG2, H460 and MRC5 cell lines, revealed that alterations in the copolymer composition (CMA mol...
Source: Biomacromolecules - October 14, 2013 Category: Biochemistry Authors: Sevimli S, Sagnella SM, Kavallaris M, Bulmus V, Davis TP Tags: Biomacromolecules Source Type: research

Monodispersed Brush-like Conjugated Polyelectrolyte Nanoparticles with Efficient and Visualized SiRNA Delivery for Gene Silencing.
Abstract RNA interference is supposed to be one of the most powerful technologies for suppression of genes and treatment of diverse human diseases while the safely delivery and visualization of siRNA were still challenging. In this text, a novel type of monodispersed conjugated polymer nanoparticles PFNBr with brush-like molecular structure was introduced into siRNA delivery system. The nanoparticles in the delivery system simply and conveniently acquired dual functions which can not only carry high amount of siRNA to penetrate intracellularly for knockdown targeted mRNA but also act as signal agents for siRNA tra...
Source: Biomacromolecules - September 16, 2013 Category: Biochemistry Authors: Jiang R, Lu XM, Yang M, Deng W, Fan Q, Huang W Tags: Biomacromolecules Source Type: research

Highlighting the Role of Polymer Length, Carbohydrate Size, and Nucleic Acid Type in Potency of Glycopolycation Agents for pDNA and siRNA Delivery.
Abstract While nucleic acids such as small interfering RNA (siRNA) and plasmid DNA (pDNA) are promising research tools and therapeutic modalities, their potential in medical applications is limited by a fundamental mechanistic understanding and inadequate efficiency. Herein, two series of carbohydrate-based polycations were synthesized and examined that varied in the degree of polymerization (n)-one containing trehalose [Tr4(n) series: Tr4(23), Tr4(55), Tr4(77)] and the other containing beta-cyclodextrin [CD4(n) series: CD4(10), CD4(26), CD4(39), CD4(143), CD4(239)]. In addition, two monosaccharide models were exa...
Source: Biomacromolecules - September 13, 2013 Category: Biochemistry Authors: Xue L, Ingle NP, Reineke TM Tags: Biomacromolecules Source Type: research

Polymer Nanocarrier System for Endosome Escape and Timed Release of siRNA with Complete Gene Silencing and Cell Death in Cancer Cells.
Abstract An influenza virus-inspired polymer mimic nanocarrier was used to deliver siRNA for specific and near complete gene knockdown of an osteoscarcom cell line (U-2SO). The polymer was synthesized by single-electron transfer living radical polymerization (SET-LRP) at room temperature to avoid complexities of transfer to monomer or polymer. It was the only LRP method that allowed good block copolymer formation with a narrow molecular weight distribution. At nitrogen to phosphorus (N/P) ratios of equal to or greater than 20 (greater than a polymer concentration of 13.8 μg/mL) with polo-like kinase 1 (PLK1) siRN...
Source: Biomacromolecules - September 4, 2013 Category: Biochemistry Authors: Gu W, Jia Z, Truong NP, Prasadam I, Xiao Y, Monteiro MJ Tags: Biomacromolecules Source Type: research

Surface modified HK:siRNA nanoplexes with enhanced pharmacokinetics and tumor growth inhibition.
Abstract We characterized in this study the pharmacokinetics and antitumor efficacy of histidine-lysine (HK):siRNA nanoplexes modified with PEG and a cyclic RGD (cRGD) ligand targeting αvβ3 and αvβ5 integrins. With non-invasive imaging, systemically administered surface modified HK:siRNA nanoplexes showed nearly 4-fold greater blood levels, 40% higher accumulation in tumor tissue, and 60% lower luciferase activity than unmodified HK:siRNA nanoplexes. We then determined whether the surface modified HK:siRNA nanoplex carrier was more effective in reducing MDA-MB-435 tumor growth with an siRNA targeting Raf-1. Re...
Source: Biomacromolecules - January 29, 2013 Category: Biochemistry Authors: Chou ST, Leng Q, Scaria P, Kahn JD, Tricoli LJ, Woodle M, Mixson AJ Tags: Biomacromolecules Source Type: research

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