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Updated: Jun 13, 2026

Preparation of Neutrally-charged, pH-responsive Polymeric Nanoparticles for Cytosolic siRNA Delivery
Published on: May 2, 2019
What are the key targeted delivery technologies of siRNA now?
1Department of Immunology, Institute for Cancer Research, Radiumhospitalet-Rikshopitalet Universtity Hospital, Oslo, Norway.
Abstract:
Whilst significant advances have been made in the delivery of nucleic acids to mammalian cells, most of the used strategies do not distinguish between normal and cancer cells. The same challenge is also facing radioactive- and chemo-therapies which are highly toxic and poorly tolerated due to limited tumor specificity. Regardless of the nature of the drug, there is a need for developing a technology platform which targets drugs only to tumors cells, leaving normal cells undamaged. Among the targeting strategies, receptor-targeted delivery provides an innovative strategy to selectively direct therapeutics to cancer cells. Receptor-binding ligands (e.g., peptides, antibodies, aptamers) can be incorporated into gene delivery vesicles or directly conjugated to siRNA in the hope in promoting their localization in target cell expressing the cognate receptors. The present chapter discusses the current progress made in the specific delivery of siRNAs.
Insights
Targeted delivery of nucleic acid therapies, like small interfering RNAs (siRNAs), to cancer cells remains a challenge. Receptor-targeted delivery offers a promising strategy to improve therapeutic specificity and minimize damage to healthy cells.
Area of Science:
- Biomedical Engineering
- Molecular Biology
- Oncology
Background:
- Current nucleic acid delivery methods lack specificity, affecting both normal and cancer cells.
- Conventional cancer therapies (chemo- and radiotherapy) exhibit toxicity and poor tumor specificity.
- A critical need exists for targeted drug delivery platforms to spare healthy tissues.
Purpose of the Study:
- To review advancements in the specific delivery of small interfering RNAs (siRNAs).
- To highlight receptor-targeted delivery as an innovative strategy for cancer therapeutics.
- To discuss methods for directing therapeutics selectively to tumor cells.
Main Methods:
- Exploration of receptor-targeted delivery strategies for therapeutics.
- Incorporation of receptor-binding ligands (peptides, antibodies, aptamers) into delivery systems.
- Conjugation of ligands directly to small interfering RNA (siRNA).
Main Results:
- Receptor-targeted delivery enhances localization of therapeutics to cancer cells expressing cognate receptors.
- Ligand incorporation into gene delivery vesicles improves targeting efficiency.
- Direct conjugation of ligands to siRNA facilitates selective cellular uptake.
Conclusions:
- Receptor-targeted delivery represents a significant advancement in achieving tumor-specific nucleic acid therapy.
- This approach holds potential for developing more effective and less toxic cancer treatments.
- Further research in this area is crucial for clinical translation.
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