PEG lipids
PEG lipids are found in the exterior shell of the LNP and serve a couple of key functions including:1 providing steric hindrance to prevent aggregation and 2 promoting a small particle size. PEG-lipids are also used to prevent proteins from binding to LNPs and increase systemic circulation times and mediate indirect targeting capabilities of LNPs. The ability of LNPs formulated with PEG-lipids to bypass the reticulo-endothelial clearance system and stay in systemic circulation gives them their nickname - “stealth agents”.
Explore our cGMP PEG offering:
While PEG-lipids have long been the standard for LNP formulations, they also present a few challenges including:
- Steric hindrance of long PEG chains hinders the ability of a cell to uptake the therapeutic
- PEGylation also hinders endosomal escape of nanoparticles, leading to decreased activity of the delivery system
- Repeated administration of PEGylated systems can result in a phenomenon called accelerated blood clearance (ABC).
Other alternatives to PEG-lipids in LNPs are being explored, and recent work has identified polysarcosine (pSar)-lipids as a promising alternative. pSar-lipids, a polymer-lipid conjugate based on the amino acid sarcosine, have demonstrated similar stealth properties to PEG-lipids. Previous studies have also shown polysarcosine lipids to induce a lower immunogenic response than PEG-lipids when administered to rabbits, zebrafish embryos, and mice. And most recently, pSar-lipids were evaluated in mRNA-LNPs and displayed high RNA transfection ability and an improved safety profile. Avanti is now offering pSar-lipids with varying polymeric chain lengths and lipid chain lengths for your PEG-free mRNA delivery research! Discover polysarcosine lipids as an alternative to PEG-lipids today!
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Lipídios inovadores: Permitindo a entrega e estabilidade de vacinas baseadas em ácido nucleico e tecnologias terapêuticas e de edição genética.
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Serviços de suporte lipídico
1. Hald Albertsen C, Kulkarni JA, Witzigmann D, Lind M, Petersson K, Simonsen JB. The role of lipid components in lipid nanoparticles for vaccines and gene therapy.
2. Adv Drug Deliv Rev. 2022 Sep;188:114416. doi: 10.1016/j.addr.2022.114416. Epub 2022 Jul 3.