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Experimental RNAi02:15

Experimental RNAi

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RNA interference (RNAi) is a cellular mechanism that inhibits gene expression by suppressing its transcription or activating the RNA degradation process. The mechanism was discovered by Andrew Fire and Craig Mello in 1998 in plants. Today, it is observed in almost all eukaryotes, including protozoa, flies, nematodes, insects, parasites, and mammals. This precise cellular mechanism of gene silencing has been developed into a technique that provides an efficient way to identify and determine the...
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The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
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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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siRNA - Small Interfering RNAs02:30

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Small interfering RNAs, or siRNAs, are short regulatory RNA molecules that can silence genes post-transcriptionally, as well as the transcriptional level in some cases. siRNAs are important for protecting cells against viral infections and silencing transposable genetic elements.
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RNA Interference01:23

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RNA interference (RNAi) is a process in which a small non-coding RNA molecule blocks the post-transcriptional expression of a gene by binding to its messenger RNA (mRNA) and preventing the protein from being translated.
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Related Experiment Video

Updated: May 6, 2026

Preparation of Neutrally-charged, pH-responsive Polymeric Nanoparticles for Cytosolic siRNA Delivery
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Polycation-based nanoparticles for RNAi-mediated cancer treatment.

Borja Ballarín-González1, Morten Frendø Ebbesen1, Kenneth Alan Howard1

  • 1Interdisciplinary Nanoscience Center (iNANO), Department of Molecular Biology and Genetics, University of Aarhus, Aarhus, Denmark.

Cancer Letters
|October 22, 2013
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Summary

RNA interference (RNAi) therapeutics offer a promising, targeted approach to cancer treatment by silencing specific genes. Polycation-based nanoparticles (polyplexes) are being developed for effective delivery of these RNAi agents, showing potential in clinical trials.

Keywords:
CancerClinical translationEPR effectNanoparticlesRNAisiRNA

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Area of Science:

  • Oncology
  • Nanotechnology
  • Molecular Biology

Background:

  • Cancer incidence is rising globally, driven by aging populations and significant socio-economic impact.
  • Gene expression deregulation is a hallmark of cancer development.
  • RNA interference (RNAi) pathway, modulated by microRNAs and small interfering RNAs (siRNAs), presents a novel therapeutic avenue.

Purpose of the Study:

  • To review pre-clinical and clinical studies on polycation-based nanoparticles (polyplexes) for RNAi-mediated anti-cancer interventions.
  • To highlight potential RNAi targets and discuss the enhanced permeability and retention (EPR) effect in systemic delivery.
  • To assess the clinical translation potential of polyplex-based RNAi therapeutics.

Main Methods:

  • Review of pre-clinical and clinical studies involving polycation-based nanocarriers for RNAi delivery.
  • Analysis of intratumoural and intravenous administration routes.
  • Focus on nanoparticle design for overcoming biological barriers and leveraging the EPR effect.

Main Results:

  • Polycation-based nanoparticles (polyplexes) demonstrate versatility in overcoming extracellular and intracellular barriers for RNAi delivery.
  • The enhanced permeability and retention (EPR) effect is a key factor in systemic delivery of RNAi therapeutics.
  • A cyclodextrin polymer-based nanocarrier system is currently in clinical trials, indicating progress.

Conclusions:

  • RNAi therapeutics, delivered via polyplexes, represent a potentially more effective and safer anti-cancer strategy.
  • Personalized cancer treatment may be achievable through microRNA-based tumor profiling combined with targeted RNAi.
  • Clinical translation of polyplex-based RNAi therapies is progressing, with promising results from ongoing trials.