1. Ionizable and Cationic Lipids

1-1. SS-cleavable and pH-responsive lipid COATSOME® SS-series

SS-cleavable and pH-responsive lipid-like material for gene, nucleic acids, and small molecule delivery system

We have newly 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 the reductive environment (cytoplasm). These two units synergize for efficient intracellular delivery of encapsulated drugs with enhanced biosafety.

• Proof of concept    

Membrane disruption in the cells

The particle composed COATSOME® SS Series is stable inserum, hence enzymatic degradation of pDNA was prevented by encapsulation. Also the particle composed of COATSOME® SS Series was effectively destabilized in the cytoplasmic environment.