7. SS-cleavable and pH-responsive Lipid Like Material (COATSOME® SS-Series)

COATSOME® SS-series New

SS-cleavable and pH-responsive lipid-like material for gene delivery and nucleic acid delivery system

We have developed COATSOME® SS-series lipids for effective intracellular delivery and lower toxicity. COATSOME® SS-series contains dual sensing motifs that can respond to the intracellular environment; tertiary amines respond to an acidic compartment (endosome/lysosome) for membrane destabilization, and disulfide bond that can cleave in reductive environment (cytoplasm). These two units synergize for efficient intracellular delivery of encapsulated drugs with enhanced biosafety.

SSLipids1

 SS-OP2

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• Proof of concept

   Particle formation

   Serum resistance

   Particle disruption in the cytoplasm

Using the non-cleavable lipid as a component of membrane, pDNA dominantly colocalizes with lipid membrane. In contrast, using SS-Cleavable lipid instead of the non-cleavable lipid, the pDNA does not colocalize with membrane and can be found prominently. These show that cleavage of the disulfide bonding accelerates particle disruption.