2N12B is a disulfide bond-containing ionizable cationic lipid (pKa = 6.5) that has been used in the generation of lipid nanoparticles (LNPs) for siRNA delivery in vitro and in vivo.[1] LNPs containing 2N12B and encapsulating siRNA targeting VEGFA mRNA reduce VEGFA levels in ARPE-19 retinal pigment cells, as well as reduce migration of human umbilical vein endothelial cells (HUVECs) in a wound healing assay. LNPs containing 2N12B and encapsulating siRNA targeting Vegfa mRNA reduce Vegfa levels in isolated mouse retina, as well as inhibit retinal angiogenesis and decrease fundus vessel leakage, in a mouse model of oxygen-induced retinopathy.
References:
[1].Cao, X., Su, L., and Chen, H.A potent bioreducible ionizable lipid nanoparticle enables siRNA delivery for retinal neovascularization inhibitionEur. J. Pharm. Biopharm.199114296(2024).