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Bile Acid–Histidine Decapeptide Conjugates as Promising Additives in Lipid Nanoparticle Formulation for siRNA Delivery
Bile acid-linked small peptides as helpful additives in lipid nanoparticles for delivering siRNA
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Abstract
The lithocholic acid-histidine decapeptide conjugate reduced ionizable lipids in liposomal nanoparticles while enhancing gene silencing activity.
- The LH conjugate was synthesized and incorporated into liposomal nanoparticles (LiLNPs) with low ionizable lipid content.
- LiLNPs containing the LH conjugate (LiLNP-LH) demonstrated improved gene silencing activity compared to standard LiLNPs.
- LiLNP-LHs showed increased liver accumulation following intravenous injection.
- LiLNP-LHs significantly reduced the release of inflammatory cytokines compared to liposomal nanoparticles with higher ionizable lipid proportions.
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