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Open AccessArticle

Novel PEGylated Liposomes Enhance Immunostimulating Activity of isRNA

1
Institute of Chemical Biology and Fundamental Medicine SB RAS, Lavrentieva ave. 8, Novosibirsk 630090, Russia
2
Institute of Fine Chemical Technologies, Moscow Technological University, Vernadskogo ave. 86, Moscow 119571, Russia
*
Author to whom correspondence should be addressed.
Academic Editor: Marina A. Dobrovolskaia
Molecules 2018, 23(12), 3101; https://doi.org/10.3390/molecules23123101
Received: 6 November 2018 / Revised: 23 November 2018 / Accepted: 24 November 2018 / Published: 27 November 2018
(This article belongs to the Special Issue Therapeutic Nucleic Acids: Past, Present, and Future)
The performance of cationic liposomes for delivery of therapeutic nucleic acids in vivo can be improved and specifically tailored to certain types of cargo and target cells by incorporation of PEG-containing lipoconjugates in the cationic liposome’s composition. Here, we report on the synthesis of novel PEG-containing lipoconjugates with molecular masses of PEG 800, 1500 and 2000 Da. PEG-containing lipoconjugates were used as one of the components in liposome preparation with the polycationic amphiphile 1,26-bis(cholest-5-en-3β-yloxycarbonylamino)-7,11,16,20-tetra-azahexacosan tetrahydrochloride (2X3) and the lipid-helper dioleoylphosphatidylethanolamine (DOPE). We demonstrate that increasing the length of the PEG chain reduces the transfection activity of liposomes in vitro, but improves the biodistribution, increases the circulation time in the bloodstream and enhances the interferon-inducing activity of immunostimulating RNA in vivo. View Full-Text
Keywords: cationic liposomes; PEG-containing lipoconjugates; transfection; non-viral delivery system; immunostimulating RNA; biodistribution cationic liposomes; PEG-containing lipoconjugates; transfection; non-viral delivery system; immunostimulating RNA; biodistribution
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Kabilova, T.; Shmendel, E.; Gladkikh, D.; Morozova, N.; Maslov, M.; Chernolovskaya, E.; Vlassov, V.; Zenkova, M. Novel PEGylated Liposomes Enhance Immunostimulating Activity of isRNA. Molecules 2018, 23, 3101.

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