Office of Technology Transfer – University of Michigan

Synthetic high density lipoproteins for delivery of biologic therapeutics

Technology #6585

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Researchers
James J. Moon
Managed By
Tiefei Dong
Senior Licensing Specialist, Life Sciences 734-763-5332
Patent Protection
US Patent Pending
PCT Patent Application WO 2016/154544

Peptide and nucleic acid-based drugs have tremendous potential as the next generation of therapeutics for devastating diseases like cancer, heart disease and diabetes. These biomolecules could be used to modify gene expression, lower blood cholesterol, treat cardiovascular disease and even vaccinate against and treat cancer amongst many other applications. One of the primary challenges in trying to use these biomolecules for the treatment of human disease lies in the difficulty of delivering them to the appropriate sites of action while also protecting them from degradation after administration.

New modifiable drug delivery systems are needed to improve delivery to target organs and allow for co-delivery of multiple biomolecules or pharmaceuticals while protecting the loaded compounds from degradation in the blood.

Synthetic high density lipoprotein for the delivery of biological therapeutics

This technology is synthetic lipid-replete high density lipoprotein (sHDL) mimetics that can be modified to incorporate biomolecules such as lipids, nucleic acids, proteins and pharmaceutical compounds. This technology protects the loaded compounds and facilitates their delivery to target organs such as liver or lymph nodes. This technology has been tested in vitro and in vivo and found to have broad applicability as a drug delivery system and vaccine platform

  • As a vaccine delivery system, antigen and adjuvant loaded synthetic HDL mimetics were found to induce a robust immune response to the incorporated peptide with antibody production and T cell activation
  • siRNA loaded synthetic HDL mimetics were able to knockdown targeted gene expression in cultured hepatocytes better than an established siRNA delivery system using cholesterol modified RNA molecules
  • In mice, fluorescently labeled synthetic HDL mimetics were found to preferentially accumulate in the liver with little to no accumulation in other organs

How this technology improves on existing therapeutics

This modifiable drug delivery system allows for co-delivery of multiple biomolecules while limiting the degradation and instability that may be found with other delivery platforms. Nucleic acids, proteins and pharmaceutical compounds can all be attached to these synthetic HDL mimetics for delivery to target tissues.

Applications

  • Targeted delivery of nucleic acids, glycolipids, proteins and pharmaceuticals
  • Vaccinations – Both cancer and infectious disease
  • Atherosclerosis therapeutic

Advantages

  • Targeted delivery to specific tissues like liver and lymph nodes
  • Co-delivery of peptides, nucleic acids, glycolipids and pharmaceuticals
  • Protection of loaded compounds from enzymatic digestion
  • Potential for lower dosing and reduced side-effects