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. 2020 Oct 28;25(21):5006. doi: 10.3390/molecules25215006

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© 2020 by the authors.

Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).

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Molecular structures of lipids used in gene therapy formulations and discussed throughout the text. (a) Typical zwitterionic (1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC) and 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE)) and neutral lipids (monoolein (MO) and Cholesterol). (b) Typical cationic lipids (1,2-dioleoyl-3-trimethylammonium propane (DOTAP), dimethyldioctadecylammonium bromide (DODAB), didodecyldimethylammonium bromide (DDAB) and cetyltrimethylammonium bromide (CTAB)). (c) PEGylated lipid with DOPE backbone and PEG M_w of ca. 2000 Da. (d) Ionizable cationic lipids (1,2-dilinoleyloxy-3-dimethylaminopropane (DLinDMA), 2,2-dilinoleyl-4-(2-dimethylaminoethyl)-[1,3]-dioxolane (DLinKC2DMA), O-(Z,Z,Z,Z-heptatriaconta-6,9,26,29-tetraen-19-yl)-4-(N,N-dimethylamino)butanoate (DLinMC3DMA) and 2-(dimethylamino)propyl-(12Z,15Z)-3-((9Z,12Z)-octadeca-9,12-dien-1-yl)henicosa-2,12,15-trienoate (YSK13-C3). (e) Multivalent cationic lipid N1-[2-((1S)-1-[(3-aminopropyl)amino]-4-[di(3-amino-propyl)amino]butylcarboxamido)ethyl]-3,4-di[oleyloxy]-benzamide (MVL5, nominal charge of +5) and dendritic headgroup cationic lipid N1-2-[((1S)-1,4-di[(1S)-1,4-di((1S)-1,4-di[(3-aminopropyl)amino]-butylcarboxamido)butyl]carboxamidobutyl)carboxamido]ethyl-3,4-di[(Z)-9-octadecenyloxy]benzamide (MVLBG2, nominal charge of +16).