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Updated: Feb 6, 2026
Delivery of Therapeutic siRNA to the CNS Using Cationic and Anionic Liposomes
Published on: July 23, 2016
Targeted Liposomes for siRNA Delivery to Cancer
Josimar O Eloy1, Raquel Petrilli2, Giovanni Loureiro Raspantini2
1School of Pharmacy, Odontology and Nursing, Federal University of Ceara, Rua Capitão Francisco Pedro, 1210, 60430-372, Fortaleza, CE, Brazil.
Background:
RNA interference is a promising therapeutic tool for the treatment of a variety of diseases, with great potential for cancer therapy. Small interfering RNA (siRNA), however, presents several drawbacks that hamper its therapeutic application. Lipid nanoparticles, including liposomes, are delivery systems with great potential for siRNA delivery, protecting it from degradation, enhancing its cell uptake with the ability of controlled release. However, non-specific delivery and side effects could potentially limit the in vivo application. Therefore, targeting lipid nanoparticles to overexpressed receptors of cancer cells represents a strategy for better therapeutic outcome, with improved efficacy and reduced toxicity. For this purpose, lipid nanoparticles could be functionalized with several moieties that can be recognized by cancer cells more than by normal cells. These ligands include folate, transferrin, peptides, oligosaccharides, monoclonal antibodies and aptamers.
Methods:
In this paper, we reviewed functionalization strategies and addressed the major in vitro and in vivo findings in the field of cancer treatment with siRNA.
Results:
Many papers showed enhanced siRNA delivery by targeted liposomes, resulting in enhanced drug uptake and better cytotoxicity, with consequent better tumor growth control in xenograft studies.
Conclusion:
siRNA delivery mediated by functionalized liposomes is promising, but clinical trials need to be conducted.
Insights
Targeted lipid nanoparticles enhance small interfering RNA (siRNA) delivery for cancer therapy. Functionalized liposomes improve efficacy and reduce toxicity, showing promise for clinical trials.
Area of Science:
- Biotechnology
- Nanomedicine
- Cancer Therapeutics
Background:
- RNA interference (RNAi) using small interfering RNA (siRNA) shows therapeutic potential for diseases, especially cancer.
- Lipid nanoparticles (LNPs), such as liposomes, protect siRNA from degradation and enhance cell uptake, but face challenges with non-specific delivery and side effects.
- Targeting LNPs to cancer cell receptors via functionalization with ligands like folate or antibodies improves therapeutic outcomes by enhancing efficacy and reducing toxicity.
Purpose of the Study:
- To review functionalization strategies for lipid nanoparticles in siRNA delivery for cancer treatment.
- To address in vitro and in vivo findings related to targeted siRNA delivery in cancer therapy.
Main Methods:
- Review of literature on functionalization strategies for lipid nanoparticles.
- Analysis of in vitro and in vivo studies on siRNA delivery using targeted liposomes for cancer treatment.
Main Results:
- Targeted liposomes demonstrate enhanced siRNA delivery, leading to increased drug uptake and cytotoxicity in cancer cells.
- Studies in xenograft models show improved tumor growth control with targeted siRNA-loaded liposomes.
Conclusions:
- Functionalized liposomes represent a promising strategy for siRNA delivery in cancer therapy.
- Further clinical trials are necessary to validate the therapeutic potential of siRNA delivery mediated by functionalized liposomes.
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