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”.
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).
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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.