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Related Experiment Video

Updated: Oct 15, 2025

Sequence-specific and Selective Recognition of Double-stranded RNAs over Single-stranded RNAs by Chemically Modified Peptide Nucleic Acids

Sequence-specific and Selective Recognition of Double-stranded RNAs over Single-stranded RNAs by Chemically Modified Peptide Nucleic Acids

Published on: September 21, 2017

Transferrin Receptor Targeted Polyplexes Completely Comprised of Sequence-Defined Components.

Teoman Benli-Hoppe¹, Şurhan Göl Öztürk¹, Özgür Öztürk¹

¹Pharmaceutical Biotechnology, Center for Drug Research, and Center for Nanoscience, Ludwig-Maximilians-Universität Munich, Butenandtstrasse 5-13, Munich, 81377, Germany.

Macromolecular Rapid Communications

|October 29, 2021

Summary

Synthetic polyplexes targeting the transferrin receptor (TfR) offer a novel approach for gene delivery. These fully synthetic nanoparticles demonstrate efficient gene silencing and delivery in cancer cells.

Keywords:

gene silencing gene transfer nanoparticles pDNA siRNA transferrin receptors

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Published on: June 13, 2014

Area of Science:

Biotechnology
Nanomedicine
Drug Delivery

Background:

Transferrin (Tf) modified polyplexes show promise for tumor-targeted nucleic acid delivery.
Challenges exist in pharmaceutical production due to blood-derived proteins and polydisperse subunits.

Purpose of the Study:

To design fully synthetic, monodisperse polyplexes for Tf receptor (TfR)-mediated gene delivery.
To overcome limitations of current Tf-based delivery systems.

Main Methods:

Solid-phase synthesis of cationizable lipo-oligoaminoamide (lipo-OAA) for siRNA polyplex core.
Attachment of a retro-enantio peptide (reTfR) via PEG spacer and click chemistry for TfR targeting.
Evaluation of six lipo-OAAs with varying lipidic domains and redox-sensitive linkages.

Main Results:

Demonstrated improved gene silencing in TfR-expressing KB and DU145 cells using siRNA polyplexes.
Successfully utilized analogous plasmid DNA (pDNA) polyplexes for receptor-mediated gene delivery in K562 and Neuro2a cells.
Assessed the impact of core polyplex stability on receptor-dependent gene transfer.

Conclusions:

Fully synthetic, TfR-targeted polyplexes offer a viable alternative for nucleic acid delivery.
The synthetic approach facilitates pharmaceutical-grade production.
Optimized lipo-OAAs enhance the efficiency of receptor-mediated gene transfer.