DOPE-PEG2000-GALA

DOPE-PEG2000-GALA: surface modification of liposomes and nanoparticles for pH-responsive intracellular delivery of drugs, nucleic acids, and macromolecules, specifically to overcome the endosomal escape barrier.
Structural composition:
(1) DOPE; a fusogenic phospholipid with two oleoyl chains that anchors into lipid bilayers and promotes membrane fusion and destabilization under acidic conditions;
(2) PEG2000; a hydrophilic polymer that provides steric stabilization and prolongs circulation half-life;
(3) GALA peptide; a synthetic pH-responsive peptide (sequence: WEAALAEALAEALAEHLAEALAEALEALAA) that adopts a random coil conformation at neutral pH (blood, pH 7.4) but transitions to an amphipathic alpha helix upon protonation of glutamic acid residues in acidic endosomes (pH 5.0-6.5), inserting into and destabilizing endosomal membranes to trigger cargo release into the cytoplasm, significantly enhancing endosomal escape efficiency.

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