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Nanomaterials 2018, 8(5), 270; https://doi.org/10.3390/nano8050270

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

1
Laboratory of Pharmaceutical Technology and Biopharmacy, CIRM, University of Liège, CHU Bat B36 Tour 4, +2, 1 avenue de l’Hopital, 4000 Liège, Belgium
2
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)
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Abstract

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
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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.

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