Next Article in Journal
Fabrication and Adsorption Behavior of Magnesium Silicate Hydrate Nanoparticles towards Methylene Blue
Next Article in Special Issue
Drug Delivery System for Emodin Based on Mesoporous Silica SBA-15
Previous Article in Journal
Photoinduced Glycerol Oxidation over Plasmonic Au and AuM (M = Pt, Pd and Bi) Nanoparticle-Decorated TiO2 Photocatalysts
Previous Article in Special Issue
Development and Characterization of Solid Lipid Nanoparticles Loaded with a Highly Active Doxorubicin Derivative
Article Menu
Issue 5 (May) cover image

Export Article

Open AccessFeature PaperArticle
Nanomaterials 2018, 8(5), 270;

Cationic Liposomes Carrying siRNA: Impact of Lipid Composition on Physicochemical Properties, Cytotoxicity and Endosomal Escape

Laboratory of Pharmaceutical Technology and Biopharmacy, CIRM, University of Liège, CHU Bat B36 Tour 4, +2, 1 avenue de l’Hopital, 4000 Liège, Belgium
Laboratory of Protein Signaling and Interactions, GIGA-Molecular Biology of Diseases, University of Liège, 4000 Liège, Belgium
Author to whom correspondence should be addressed.
Received: 13 April 2018 / Revised: 18 April 2018 / Accepted: 21 April 2018 / Published: 24 April 2018
(This article belongs to the Special Issue Pharmaceutical Nanotechnology)
Full-Text   |   PDF [1053 KB, uploaded 3 May 2018]   |  


In recent year, cationic liposomes have gained a lot of attention for siRNA delivery. Despite this, intracellular barriers as endosomal escape and cytosolic delivery of siRNA still represent a challeng, as well as the cytotoxicity due to cationic lipids. To address these issues, we developed four liposomal formulations, composed of two different cationic lipids (DOTAP and DC-Cholesterol) and different ratio of co-lipids (cholesterol and DOPE). The objective is to dissect these impacts on siRNA efficacy and cytotoxicity. Liposomes were complexed to siRNA at six different N/P molar ratios, physico-chemical properties were characterized, and consequently, N/P 2.5, 5 and 10 were selected for in vitro experiments. We have shown that cytotoxicity is influenced by the N/P ratio, the concentration of cationic lipid, as well as the nature of the cationic lipid. For instance, cell viability decreased by 70% with liposomes composed of DOTAP/Cholesterol/DOPE 1/0.75/0.5 at a N/P ratio 10, whereas the same formulation at a N/P ratio of 2.5 was safe. Interestingly, we have observed differences in terms of mRNA knock-down efficiency, whereas the transfection rate was quite similar for each formulation. Liposomes containing 50% of DOPE induced a mRNA silencing of around 80%. This study allowed us to highlight crucial parameters in order to develop lipoplexes which are safe, and which induce an efficient intracytoplasmic release of siRNA. View Full-Text
Keywords: liposome; siRNA; Cellular uptake: lipids; cytoxiciy liposome; siRNA; Cellular uptake: lipids; cytoxiciy

Figure 1

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

Supplementary material


Share & Cite This Article

MDPI and ACS Style

Lechanteur, A.; Sanna, V.; Duchemin, A.; Evrard, B.; Mottet, D.; Piel, G. Cationic Liposomes Carrying siRNA: Impact of Lipid Composition on Physicochemical Properties, Cytotoxicity and Endosomal Escape. Nanomaterials 2018, 8, 270.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics



[Return to top]
Nanomaterials EISSN 2079-4991 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top