Related Experiment Video

Updated: Feb 16, 2026

Porous Silicon Microparticles for Delivery of siRNA Therapeutics
08:31

Porous Silicon Microparticles for Delivery of siRNA Therapeutics

Published on: January 15, 2015

11.5K

Fluorination Enhances Serum Stability of Bioreducible Poly(amido amine) Polyplexes and Enables Efficient Intravenous

Gang Chen1, Kaikai Wang1, Yixin Wang1

  • 1State Key Laboratory of Natural Medicines, Department of Pharmaceutics, China Pharmaceutical University, Nanjing, 210009, China.

Advanced Healthcare Materials
|December 28, 2017
PubMed

Insights

New siRNA delivery systems enhance cancer treatment by combining fluorination, bioreducibility, and PEGylation for improved stability and targeted tumor delivery, overcoming previous limitations in systemic administration.

Area of Science:

  • Biomaterials Science
  • Nanotechnology
  • Cancer Therapeutics

Background:

  • Systemic delivery of small interfering RNA (siRNA) for cancer treatment is hindered by poor stability and inefficient delivery of polycation/siRNA polyplexes.
  • Existing delivery methods often face challenges in balancing stability, cellular uptake, and intracellular release of siRNA.

Purpose of the Study:

  • To develop and test a novel modular siRNA delivery system (PEG-PCD-F) combining fluorination, bioreducibility, and PEGylation.
  • To overcome the limitations of current siRNA delivery systems for effective systemic delivery to distant tumors.

Main Methods:

  • Synthesis of PEGylated, fluorinated, and bioreducible copolymers (PEG-PCD-F) with varying degrees of fluorination.
  • Formation of polyplexes with siRNA and evaluation of their stability, cellular uptake, and gene silencing efficacy in vitro.
  • Assessment of in vivo tumor growth inhibition following systemic administration of PEG-PCD-F/siRNA polyplexes in a breast cancer model.

Main Results:

  • Fluorinated copolymers formed stable polyplexes with siRNA, demonstrating enhanced gene silencing in vitro compared to non-fluorinated controls.
  • Fluorination improved polyplex stability, cellular uptake, and endosomal escape, while maintaining efficient siRNA release in the intracellular environment.
  • Systemic intravenous administration of PEG-PCD-F/siRNA targeting Bcl2 significantly inhibited breast tumor growth in vivo.

Conclusions:

  • The combination of bioreducibility, fluorination, and PEGylation in a modular design offers a promising strategy for effective systemic siRNA delivery.
  • The developed PEG-PCD-F system successfully addresses the conflicting demands of siRNA delivery for enhanced cancer therapy.
  • This approach provides strong evidence for overcoming previous barriers in achieving stable and efficient systemic siRNA delivery to tumors.
Keywords:
bioreducible poly(amido amine)sfluorinationpolyplexestumor siRNA delivery

More Related Videos

Delivery of Therapeutic siRNA to the CNS Using Cationic and Anionic Liposomes10:33

Delivery of Therapeutic siRNA to the CNS Using Cationic and Anionic Liposomes

Published on: July 23, 2016

11.2K
Preparation of Exosomes for siRNA Delivery to Cancer Cells09:59

Preparation of Exosomes for siRNA Delivery to Cancer Cells

Published on: December 5, 2018

26.1K

Related Concept Videos

siRNA - Small Interfering RNAs02:30

siRNA - Small Interfering RNAs

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.
In the cytoplasm, siRNA is processed from a double-stranded RNA, which comes from either endogenous DNA transcription or exogenous sources like a virus. This double-stranded RNA is then cleaved by the...
18.8K
Bioavailability Enhancement: Drug Stability Enhancement and GI Retention01:05

Bioavailability Enhancement: Drug Stability Enhancement and GI Retention

Body:Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
227
RNA Stability01:53

RNA Stability

Intact DNA strands can be found in fossils, while scientists sometimes struggle to keep RNA intact under laboratory conditions. The structural variations between RNA and DNA underlie the differences in their stability and longevity. Because DNA is double-stranded, it is inherently more stable. The single-stranded structure of RNA is less stable but also more flexible and can form weak internal bonds. Additionally, most RNAs in the cell are relatively short, while DNA can be up to 250 million...
35.8K
mRNA Stability and Gene Expression02:51

mRNA Stability and Gene Expression

The structure and stability of mRNA molecules regulates gene expression, as mRNAs are a key step in the pathway from gene to protein. In eukaryotes, the half-life of mRNA varies from a few minutes up to several days. mRNA stability is essential in growth and development. The absence of the proteins regulating its stability, such as tristetraprolin in mice, can cause systemic issues, including bone marrow overgrowth, inflammation, and autoimmunity.
Cis-acting Elements involved in mRNA stability
6.7K
Amines to Amides: Acylation of Amines01:19

Amines to Amides: Acylation of Amines

Various carboxylic acid derivatives (such as acid chlorides, esters, and anhydrides) can be used for the acylation of amines to yield amides. The reaction requires two equivalents of amines. The first amine molecule functions as a nucleophile and attacks the carbonyl carbon to produce a tetrahedral intermediate. This is followed by the loss of the leaving group and restoration of the C=O bond.
Next, the second equivalent of amine serves as a Brønsted base and deprotonates the quaternary...
3.5K
Nuclear Stability03:18

Nuclear Stability

Protons and neutrons, collectively called nucleons, are packed together tightly in a nucleus. With a radius of about 10−15 meters, a nucleus is quite small compared to the radius of the entire atom, which is about 10−10 meters. Nuclei are extremely dense compared to bulk matter, averaging 1.8 × 1014 grams per cubic centimeter. If the earth’s density were equal to the average nuclear density, the earth’s radius would be only about 200 meters.
To hold positively charged protons together...
23.4K