SS-cleavable and pH-responsive Lipids

COATSOME® SS-Series – for gene, nucleic acids and small molecule drug 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.

Features

Encapsulation: siRNA, mRNA, pDNA

Efficient drug delivery into the cytoplasm of cells

Biodegradability and low toxicity

Controlled targeting of organs: liver, spleen, or lymph nodes

3 responsive units

Proof of concept – Particle formation

Serum resistance

Membrane disruption in the cells

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

Blue: nucleus (Hoechst33342), Green: Lipid membrane (NBD), Red: pDNA (Rhodamine)

COATSOME® SS Series

COATSOME SS-E

SS-cleavable and pH-responsive Lipids, MW=1322.0
Chemical name: Bis{2-[N-methyl-N-(α-D-tocopherolhemisuccinatepropyl)amino]ethyl}disulfide
CAS#: 1436860-64-8
Package size: 0.1g / 1g / 10g

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COATSOME SS-EC

SS-cleavable and pH-responsive Lipids, MW=1402.2
Chemical name: Bis{2-[4-(α-D-tocopherolhemisuccinateethyl)piperidyl]ethyl} disulfide
CAS#: Not available
Package size: 0.1g / 1g / 10g

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COATSOME SS-OC

SS-cleavable and pH-responsive Lipids, MW=905.5
Chemical name: Bis{2-[4-(cis-9-octadecenoateethyl)-1-piperidinyl]ethyl}disulfide
CAS#: Not available
Package size: 0.1g / 1g / 10g

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COATSOME SS-OP

SS-cleavable and pH-responsive Lipids, MW=1173.8
Chemical name: Bis[2-(4-{2-[4-(cis-9-octadecenoyloxy)phenylacetoxy]ethyl}piperidinyl)ethyl] disulfide
CAS#: 2377474-67-2
Package size: 0.1g / 1g / 10g

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