Rational design and combinatorial chemistry of ionizable lipids for RNA delivery
In 2018, LNPs enabled the first FDA approval of a siRNA drug (Onpattro); two years later, two SARS-CoV-2 vaccines (Comirnaty, Spikevax) based on LNPs containing mRNA also arrived at the clinic, saving millions of lives during the COVID-19 pandemic. Notably, each of the three FDA-approved LNP formula...
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| Veröffentlicht in: | Journal of materials chemistry. B, Materials for biology and medicine Materials for biology and medicine, 2023-07, Vol.11 (28), p.6527-6539 |
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| container_title | Journal of materials chemistry. B, Materials for biology and medicine |
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| creator | Xu, Yue Golubovic, Alex Xu, Shufen Pan, Anni Li, Bowen |
| description | In 2018, LNPs enabled the first FDA approval of a siRNA drug (Onpattro); two years later, two SARS-CoV-2 vaccines (Comirnaty, Spikevax) based on LNPs containing mRNA also arrived at the clinic, saving millions of lives during the COVID-19 pandemic. Notably, each of the three FDA-approved LNP formulations uses a unique ionizable lipid while the other three components,
i.e.
, cholesterol, helper lipid, and PEGylated lipid, are almost identical. Therefore, ionizable lipids are critical to the delivery efficiency of mRNA. This review covers recent advances in ionizable lipids used in RNA delivery over the past several decades. We will discuss chemical structures, synthetic routes, and structure-activity relationships of ionizable lipids.
This review will delve into the crucial role of ionizable lipids in the development of lipid nanoparticles (LNPs) for efficient RNA delivery. |
| doi_str_mv | 10.1039/d3tb00649b |
| format | Article |
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i.e.
, cholesterol, helper lipid, and PEGylated lipid, are almost identical. Therefore, ionizable lipids are critical to the delivery efficiency of mRNA. This review covers recent advances in ionizable lipids used in RNA delivery over the past several decades. We will discuss chemical structures, synthetic routes, and structure-activity relationships of ionizable lipids.
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i.e.
, cholesterol, helper lipid, and PEGylated lipid, are almost identical. Therefore, ionizable lipids are critical to the delivery efficiency of mRNA. This review covers recent advances in ionizable lipids used in RNA delivery over the past several decades. We will discuss chemical structures, synthetic routes, and structure-activity relationships of ionizable lipids.
This review will delve into the crucial role of ionizable lipids in the development of lipid nanoparticles (LNPs) for efficient RNA delivery.</description><subject>Cholesterol</subject><subject>Combinatorial analysis</subject><subject>Combinatorial chemistry</subject><subject>COVID-19</subject><subject>COVID-19 Vaccines</subject><subject>Humans</subject><subject>Lipids</subject><subject>Lipids - chemistry</subject><subject>mRNA</subject><subject>Nanoparticles - chemistry</subject><subject>Pandemics</subject><subject>RNA, Messenger - genetics</subject><subject>SARS-CoV-2 - genetics</subject><subject>Severe acute respiratory syndrome coronavirus 2</subject><subject>siRNA</subject><subject>Vaccines</subject><issn>2050-750X</issn><issn>2050-7518</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2023</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpdkd9LwzAQx4Mobsy9-K4UfBGhmjRJ2zxu8ycMlTHBt5KkiWa0zUxaYf71Zm5O8F7u4D735e57ABwjeIkgZlclbgWEKWFiD_QTSGGcUZTv72r42gND7xcwRI7SHJND0MMZJpRg2AfPM94a2_AqKpU3b03EmzKStham4a11JjTku6qNb90qsjoKrPniolJRZZam9JG2Lpo9jsJ4ZT6VWx2BA80rr4bbPAAvtzfzyX08fbp7mIymscQ4a2OUZ5wzJLUsCc2VTGRaMs25ThHVeZYhwrhIISO05IppBpkWhHDBhBAplQQPwPlGd-nsR6d8W4Qlpaoq3ijb-SLJkyCDUUYDevYPXdjOhZvXFGYJTbN0LXixoaSz3juli6UzNXerAsFibXVxjefjH6vHAT7dSnaiVuUO_TU2ACcbwHm56_79Cn8DwRGC4A</recordid><startdate>20230719</startdate><enddate>20230719</enddate><creator>Xu, Yue</creator><creator>Golubovic, Alex</creator><creator>Xu, Shufen</creator><creator>Pan, Anni</creator><creator>Li, Bowen</creator><general>Royal Society of Chemistry</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7QF</scope><scope>7QO</scope><scope>7QQ</scope><scope>7SC</scope><scope>7SE</scope><scope>7SP</scope><scope>7SR</scope><scope>7TA</scope><scope>7TB</scope><scope>7U5</scope><scope>8BQ</scope><scope>8FD</scope><scope>F28</scope><scope>FR3</scope><scope>H8D</scope><scope>H8G</scope><scope>JG9</scope><scope>JQ2</scope><scope>KR7</scope><scope>L7M</scope><scope>L~C</scope><scope>L~D</scope><scope>P64</scope><scope>7X8</scope><orcidid>https://orcid.org/0000-0001-5006-9143</orcidid><orcidid>https://orcid.org/0000-0002-7695-1115</orcidid><orcidid>https://orcid.org/0000-0001-7672-9170</orcidid><orcidid>https://orcid.org/0009-0003-1557-6694</orcidid><orcidid>https://orcid.org/0000-0001-5151-5686</orcidid></search><sort><creationdate>20230719</creationdate><title>Rational design and combinatorial chemistry of ionizable lipids for RNA delivery</title><author>Xu, Yue ; 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Notably, each of the three FDA-approved LNP formulations uses a unique ionizable lipid while the other three components,
i.e.
, cholesterol, helper lipid, and PEGylated lipid, are almost identical. Therefore, ionizable lipids are critical to the delivery efficiency of mRNA. This review covers recent advances in ionizable lipids used in RNA delivery over the past several decades. We will discuss chemical structures, synthetic routes, and structure-activity relationships of ionizable lipids.
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| source | MEDLINE; Royal Society Of Chemistry Journals 2008- |
| subjects | Cholesterol Combinatorial analysis Combinatorial chemistry COVID-19 COVID-19 Vaccines Humans Lipids Lipids - chemistry mRNA Nanoparticles - chemistry Pandemics RNA, Messenger - genetics SARS-CoV-2 - genetics Severe acute respiratory syndrome coronavirus 2 siRNA Vaccines |
| title | Rational design and combinatorial chemistry of ionizable lipids for RNA delivery |
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