2016
DOI: 10.1021/acs.molpharmaceut.5b00608
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Abstract: Small interfering RNA (siRNA) therapeutics have potential advantages over traditional small molecule drugs such as high specificity and the ability to inhibit otherwise "undruggable" targets. However, siRNAs have short plasma half-lives in vivo, can induce a cytokine response, and show poor cellular uptake. Formulating siRNA into nanoparticles offers two advantages: enhanced siRNA stability against nuclease degradation beyond what chemical modification alone can provide; and improved site-specific delivery tha… Show more

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Cited by 21 publications
(21 citation statements)
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“…Another interesting approach is to react polyamines or positively charged dendrimers with some of the carboxyl groups of PLGA in order to generate additional positive charges that can be used for electrostatic binding 134. In addition, siRNAs may also be covalently linked to PLGA via intracellular cleavable disulfide linkers 136…”
Section: Delivery Systemsmentioning
confidence: 99%
“…Another interesting approach is to react polyamines or positively charged dendrimers with some of the carboxyl groups of PLGA in order to generate additional positive charges that can be used for electrostatic binding 134. In addition, siRNAs may also be covalently linked to PLGA via intracellular cleavable disulfide linkers 136…”
Section: Delivery Systemsmentioning
confidence: 99%
“…Common strategies to stabilize siRNA polyplexes include bioreducible crosslinking and hydrophobic stabilization of the polycations or covalent attachment of the siRNA to the carrier . In our previous work, we investigated the influence of cysteines for bioreducible disulfide‐linkage and hydrophobic domains such as tyrosine trimers and fatty acids on the properties of polyplexes formed with siRNA and sequence‐defined cationic oligoamino amide oligomers .…”
Section: Nucleic Acid Binding—the Polyplex Formation Processmentioning
confidence: 99%
“…Nanoparticles prepared with PLGA are often used as an siRNA delivery system. 18 , 27 , 28 , 29 , 30 , 31 , 32 , 33 When preparing siRNA-incorporated PLGA nanoparticles using the double emulsion method, poly (vinyl alcohol) (PVA) is usually used as the emulsifying agent to create stable and homogenous emulsions. 18 , 27 , 28 , 29 , 30 , 31 , 34 In order to PEGylate the PLGA nanoparticles, copolymers synthesized by conjugating PEG molecules with PLGA or PLA are regularly used.…”
Section: Resultsmentioning
confidence: 99%
“… 18 , 27 , 28 , 29 , 30 , 31 , 34 In order to PEGylate the PLGA nanoparticles, copolymers synthesized by conjugating PEG molecules with PLGA or PLA are regularly used. 31 , 32 , 33 In the present study, we used the acid-sensitive PEG-hydrazone-C18 (PHC) previously synthesized in our laboratory as an emulsifying agent in the second water phase to prepare siRNA-incorporated PLGA nanoparticles using the double emulsion method ( i.e. , AS-siRNA-NPs, where AS indicates that the nanoparticles are PEGylated with the acid-sensitive sheddable PEG).…”
Section: Resultsmentioning
confidence: 99%