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Updated: Apr 27, 2026
Delivery of Therapeutic siRNA to the CNS Using Cationic and Anionic Liposomes
Published on: July 23, 2016
Anginex lipoplexes for delivery of anti-angiogenic siRNA
Afrouz Yousefi1, Meriem Bourajjaj1, Negar Babae1
1Department of Pharmaceutics, Utrecht Institute for Pharmaceutical Sciences, Faculty of Science, Utrecht University, Universiteitsweg 99, 3584 CG Utrecht, The Netherlands.
Abstract:
Angiogenesis is one of the hallmarks of cancer which renders it an attractive target for therapy of malignancies. Tumor growth suppression can be achieved by inhibiting angiogenesis since it would deprive tumor cells of oxygen and vital nutrients. Activation of endothelial cells of tumor vasculature is the first step in angiogenesis which is mediated by various factors. One of the major triggers in this process is vascular endothelial growth factor (VEGF) which binds to VEGF receptors on endothelial cells of tumor vessels. This induces a series of signaling cascades leading to activation of cellular processes involved in angiogenesis, and therefore down-regulation of VEGF receptor-2 (VEGFR-2) expression seems a viable option to inhibit angiogenesis. In our investigations, this aim has been pursued by using siRNA interfering with the expression of VEGFR-2. Since the discovery of RNA interference (RNAi) as a gene regulation process, successful delivery of small non-coding RNA has presented itself as a major challenge. In the current study, we have characterized a galectin-1 targeted anginex-coupled lipoplex (Angiplex) containing siRNA against the gene of VEGFR-2 as an angiostatic therapeutic. Angiplex particles had a size of approximately 120 nm with a net negative charge and were stable in vitro. These particles were internalized in a specific manner by HUVECs compared to a non-targeted lipoplex system, and their uptake was higher than Lipofectamine 2000. Gene silencing efficiency of Angiplex was shown to be 61%.
Insights
Researchers developed a targeted lipoplex (Angiplex) delivering siRNA to inhibit vascular endothelial growth factor receptor-2 (VEGFR-2) expression, a key driver of tumor angiogenesis. This novel therapeutic approach showed significant gene silencing efficiency, offering a promising strategy for cancer therapy.
Area of Science:
- Oncology
- Molecular Biology
- Nanotechnology
Background:
- Angiogenesis, the formation of new blood vessels, is crucial for tumor growth and metastasis.
- Vascular Endothelial Growth Factor Receptor-2 (VEGFR-2) plays a pivotal role in mediating tumor angiogenesis.
- Inhibiting VEGFR-2 is a promising therapeutic strategy for cancer treatment.
Purpose of the Study:
- To develop and characterize a novel targeted lipoplex system (Angiplex) for delivering small interfering RNA (siRNA) against VEGFR-2.
- To evaluate the efficacy of Angiplex in gene silencing and cellular uptake in human umbilical vein endothelial cells (HUVECs).
Main Methods:
- siRNA targeting VEGFR-2 was encapsulated in galectin-1 targeted anginex-coupled lipoplexes (Angiplex).
- Physicochemical properties of Angiplex, including size and charge, were characterized.
- Cellular uptake of Angiplex in HUVECs was compared to non-targeted lipoplexes and Lipofectamine 2000.
- Gene silencing efficiency of VEGFR-2 by Angiplex was quantified.
Main Results:
- Angiplex particles were approximately 120 nm with a negative charge and demonstrated in vitro stability.
- Angiplex exhibited specific cellular internalization in HUVECs with higher uptake compared to control systems.
- A gene silencing efficiency of 61% for VEGFR-2 was achieved using Angiplex.
Conclusions:
- Angiplex represents a potentially effective targeted delivery system for siRNA-based cancer therapy.
- The targeted delivery and efficient gene silencing by Angiplex offer a promising approach to inhibit tumor angiogenesis.
- Further studies are warranted to evaluate the therapeutic potential of Angiplex in preclinical cancer models.
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