DOPE-PEG2000-R6H4

DOPE-PEG2000-R6H4: surface modification of liposomes and nanoparticles for enhanced intracellular drug and nucleic acid delivery, with pH-responsive endosomal escape capability.
Structural composition:
(1) DOPE; a fusogenic phospholipid with two oleoyl chains that anchors into lipid bilayers and promotes membrane destabilization under acidic conditions;
(2) PEG2000; a hydrophilic polymer that provides steric stabilization and prolongs circulation half-life by reducing immune clearance;
(3) R6H4 peptide; a cell-penetrating peptide rich in arginine (for membrane interaction and cellular uptake via electrostatic interactions with negatively charged cell membranes) and histidine (for pH-responsive endosomal escape through the proton sponge effect, where histidine imidazole groups protonate in acidic endosomes causing osmotic swelling and membrane rupture), enabling efficient cytosolic release of cargo.

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