Shrirang, K. have previously demonstrated that using a longer carbon tail length of 22 carbons and unsaturation in the form of 1,2-dierucoyl-sn-glycero-3-phosphoethanolamine (DEPE) as a helper lipid provides dramatic improvement in mRNA delivery, compared to LNPs incorporating the DOPE helper lipid.
Product name | DEPE |
Chemical name | 1,2-Dierucoyl-sn-glycero-3-phosphoethanolamine |
CAS no. | 904304-57-0 |
NMPA CDE registration no. | N/A |
USFDA DMF no. | N/A |
Quality grade | reagent grade |
Quality standards | N/A |
Molecular formula | C49H94NO8P |
| Applications and examples | |
Product code | |
Package sizes | 1kg |
Storage condition | N/A |
[1] WO2021007278 - IMPROVED MRNA-LOADED LIPID NANOPARTICLES AND PROCESSES OF MAKING THE SAME
The inventors have surprisingly found that delivery and/or expression of mRNA in vivo can be improved dramatically by optimizing the helper lipid component of multicomponent liposomes encapsulating the mRNA. In particular, the present invention is based on the discovery that the presence of 1,2-Dierucoyl-sn-glycero-3-phosphoethanolamine (DEPE) as a helper lipid in mRNA-encapsulating lipid nanoparticle formulations comprising one or more cationic lipids, one or more PEG-modified lipids and one or more helper lipids can increase delivery and/or expression of mRNA in vivo by more than two-fold relative to conventional liposomes comprising dioleoylphosphatidylethanolamine (DOPE) as one of the helper lipids. DEPE-containing lipid nanoparticles were comparable DOPE-containing lipid nanoparticles in terms of safety and tolerability (as assessed by liver toxicity markers such as ALT and AST).
Accordingly, it is an aspect of the invention to provide a lipid nanoparticle for the delivery of mRNA to a subject in need thereof, wherein the lipid nanoparticle comprises one or more cationic lipids, one or more PEG-modified lipids and one or more helper lipids encapsulating the mRNA, wherein the one or more helper lipids comprises 1,2-Dierucoyl-sn-glycero-3-phosphoethanolamine (DEPE). The DEPE in the lipid nanoparticle provides for the enhanced expression of the mRNA when administered to a subject.
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