PEG lipids, also known as PEGylated lipids are a class of PEG derivatives that are attached to a lipid moiety such as DMG or DSPE. PEG lipid has been used extensively to improve circulation times for liposome encapsulated (LNP) drugs and reduce non-specific uptakes.
PEG lipids such as PEG2000-DMG (Figure 1) can have multiple effects on the properties of lipid nanoparticles. The amount of PEG lipids can affect particle size. PEG lipids can further contribute to particle stability by decreasing particle aggregation, and the optimization of PEG can prolong the blood circulation time of nanoparticles by reducing clearance mediated by the kidneys and the mononuclear phagocyte system. Finally, PEG lipids can also be used to conjugate specific ligands to the particle for targeted delivery. The extent of these effects depend on the proportions and properties of the PEG lipids (such as PEG molar mass and lipid length). Lipid nanoparticle-siRNA formulations containing PEG2000-DMG have shorter circulation times and higher delivery efficacy in vivo than formulations containing PEG2000-DSG. This difference may be attributed to the faster dissociation of PEG2000-DMG from lipid nanoparticles, compared with PEG2000-DSG, which may benefit cellular uptake and endosomal escape of lipid nanoparticles.
Figure 1: Structures of PEG2000-DMG and PEG2000-DSG
PEG-lipid micelles, primarily conjugates of polyethylene glycol (PEG) and distearyl phosphatidylethanolamine (DSPE) or PEG-DSPE, have emerged as promising drug-delivery carriers to address the shortcomings associated with new molecular entities with suboptimal biopharmaceutical attributes. The flexibility in PEG-DSPE design coupled with the simplicity of physical drug entrapment have distinguished PEG-lipid micelles as versatile and effective drug carriers for cancer therapy. They were shown to overcome several limitations of poorly soluble drugs such as non-specific biodistribution and targeting, lack of water solubility and poor oral bioavailability. PEG lipids is used as an excipient in both the Moderna vaccine and the Pfizer-BioNTech COVID-19 vaccine.
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