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Related Concept Videos

Site-Targeted Drug Delivery Systems: Polymeric Carriers01:24

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Polymeric carriers enhance targeted drug delivery by increasing efficacy while minimizing off-target effects. These carriers comprise a biodegradable polymeric backbone integrated with functional elements that enable targeting, improve physicochemical properties, and regulate drug release.Targeting MechanismsThe targeting ability of polymeric carriers is mediated by a homing device, which is a molecular recognition component designed to selectively bind to specific tissues or cells. Monoclonal...
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Related Experiment Video

Updated: Apr 21, 2026

Preparation of Neutrally-charged, pH-responsive Polymeric Nanoparticles for Cytosolic siRNA Delivery
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Targeted decationized polyplexes for siRNA delivery.

Luís Novo1, Kaori M Takeda, Tamara Petteta

  • 1Department of Pharmaceutics, Utrecht Institute for Pharmaceutical Sciences, Utrecht University , 3584, CG Utrecht, The Netherlands.

Molecular Pharmaceutics
|November 11, 2014
PubMed
Summary

Folate-targeted decationized polyplexes show promise as safe and stable carriers for small interfering RNA (siRNA) delivery. These systems efficiently deliver siRNA to target cells, enabling sequence-specific gene silencing with rapid intracellular release.

Keywords:
biocompatibilitynanoparticlepolymersiRNA deliverytargeting

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Area of Science:

  • Biotechnology
  • Nanomedicine
  • Molecular Biology

Background:

  • Small interfering RNA (siRNA) therapeutics require safe and efficient delivery systems.
  • Previous work demonstrated the potential of decationized polyplexes for DNA delivery, showing safety and triggered release.
  • Targeted decationized polyplexes feature a disulfide cross-linked pHPMA core for nucleic acid entrapment and a PEG-folate shell for targeting.

Purpose of the Study:

  • To investigate the suitability of folate-targeted decationized polyplexes for delivering small interfering RNA (siRNA).
  • To optimize the carrier system, focusing on the cross-linking density of the polyplex core for enhanced siRNA delivery.

Main Methods:

  • Preparation of stable, nanosized siRNA-loaded decationized polyplexes by optimizing core cross-linking density.
  • Assessment of siRNA stability within polyplexes in human plasma using fluorescence correlation spectroscopy (FCS).
  • Evaluation of gene silencing efficacy and cellular effects in a folate receptor-overexpressing cell line (Skov3-luc) using luciferase expression and XTT assays.

Main Results:

  • Optimized cross-linking density yielded stable, nanosized siRNA decationized polyplexes.
  • Significant siRNA entrapment within polyplexes was observed in human plasma.
  • Sequence-specific gene silencing was achieved in Skov3-luc cells, with no observed interference with intrinsic luciferase expression or cell metabolic activity.

Conclusions:

  • Folate-targeted decationized polyplexes are safe and stable carriers for siRNA.
  • These polyplexes effectively interact with target cells and rapidly disassemble upon cellular entry.
  • The optimized system demonstrates potential as a promising delivery vehicle for siRNA-based therapies.