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Review
. 2019 Feb 12;10(3):369-377.
doi: 10.1039/c8md00515j. eCollection 2019 Mar 1.

Diversity of PEGylation methods of liposomes and their influence on RNA delivery

A S Nosova  1 , O O Koloskova  1 , A A Nikonova  1   2 , V A Simonova  3 , V V Smirnov  1   3 , D Kudlay  1 , M R Khaitov  1
Affiliations
Review

Diversity of PEGylation methods of liposomes and their influence on RNA delivery

A S Nosova et al. Medchemcomm. .

Abstract

Gene therapy is a promising approach for personalized medicine, but its application in humans requires development of efficient and safe vehicles. PEGylated liposomes are some of the most suitable delivery systems for nucleic acids because of their stability under physiological conditions and prolonged circulation time, compared to conventional and other types of "stealth" liposomes. In vitro/in vivo activity of PEGylated liposomes is highly dependent on PEG motif abundance. The process of "stealth" coverage formation is a very important parameter for efficient transfection assays and further fate determination of the PEG layer after tissue penetration. In this review, we discuss the latest methods of PEGylated liposome preparation.

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Figures

Fig. 1
Fig. 1. PEGylation density – coverage type dependency.
Fig. 2
Fig. 2. Scheme of PEGylated lipoplex preparation by the pre-insertion method.
Fig. 3
Fig. 3. mPEG-PE lipids: N-(methylpolyoxyethylene oxycarbonyl)-1,2-distearoyl-sn-glycero-3-phosphoethanolamine (DSPE-mPEG), N-(methylpolyoxyethylene oxycarbonyl)-1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine (DPPE-mPEG), and N-(methylpolyoxyethylene oxycarbonyl)-1,2-dioleoyl-sn-glycero-3-phosphoethanolamine-poly(ethylene glycol) (DOPE-mPEG). N – number of oxyethylene –CH2CH2O– units.
Fig. 4
Fig. 4. Non-PE PEGylated lipids: mPEG2k-Glu(C16)2 and mPEG-Chol. N – number of oxyethylene –CH2CH2O– units.
Fig. 5
Fig. 5. Scheme of PEGylated lipoplex preparation by the post-insertion method.
Fig. 6
Fig. 6. Non-PE PEGylated lipids applied in the post-insertion method: mPEG2k-tz-Glu(C16)2, N-(methylpolyoxyethylene oxyethyl)-2-hexadecylcarbamoylmethyl hexadecanoic amide (mPEG-HDAS), and mPEG-Cer-Cx. N – number of oxyethylene –CH2CH2O– units, x – number of homologous –CH2– groups.
Fig. 7
Fig. 7. PEG cleavage after tumor tissue penetration.
Fig. 8
Fig. 8. Cleavable PEGylated lipids: mPEG-S-S-DSPE, mPEG-S-S-POPE, mPEG-hz-CHEMS. N – number of oxyethylene –CH2CH2O– units.
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