Highly efficient siRNA delivery carrier using block copolymers and peptides

Enhanced accumulation in cancer tissue, inflammatory sites and posterior eye because of a unique short peptide that improves intracorporeal and intracellular kinetics

Advantage and Core Benefit

  • Transdermal administration in combination with tight junction modulators is also expected
  • Designing the peptide to be placed inside the micelle reduces cytotoxicity.

Background and Technology

For carriers of nucleic acid drugs such as siRNA, it is important to stabilize their pharmacokinetics in the body and facilitate their uptake into cells.
Inventors have developed a unique functional peptide CH2R4H2C that improves cell permeability. Nano-micelles based on a polyethylene glycol-polycaprolactone-peptide conjugated polymer (PEG-PCL-CH2R4H2C) were found to be carriers for enhanced intracellular accumulation of siRNA and to exhibit high silencing efficacy (doi.org/10.1016/j.ijpharm.2017.07.077, doi:10.3390/molecules21101279).

Furthermore, the block copolymer (PEG-PCL) and stearinated peptide (STR-CH2R4H2C) were mixed without linkage, and the peptide was placed inside the micelle by electrical interaction to solve the cytotoxicity issue. Using the improved nano-micelles as carriers of anti-NF-κB siRNA (siRelA), we confirmed that the therapeutic efficacy was comparable to conventional ones in rheumatoid arthritis mice and pancreatic cancer subcutaneous transplantation models.

 

Data

  • Therapeutic effect of Anti-NF-kB (siRelA)-loaded nano-micelle in collagen-induced arthritis (CIA) model mice. Intravenous administration of siRelA-loaded nano-micelles (siRNA: 20 µg, MTX: 6 mg/kg) to CIA model mice suppressed inflammatory cytokines to the same level as normal mice and improved clinical scores of arthritis.

Patent

WO2019-013255

Researcher

Dr. Yuki Takashima (Tokyo University of Pharmacy and Life Sciences)
Dr. Takanori Kanazawa (University of Shizuoka)

Expectations

We hope to collaborate with companies developing nucleic acid drugs to promote drug discovery and development using the nano micelles we have developed. For companies interested in delivery targeting ophthalmology, tumors, etc., this is expected to be a good collaboration, as many tools can be combined and devised. We can provide materials in MTA and micelle prototypes with payloads.

 

Project No: WL-04356

 

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