WARF: P110315US02

Improving Drug Delivery with Boronic Acids


Ronald Raines, Gregory Ellis, Michael Palte

The Wisconsin Alumni Research Foundation (WARF) is seeking commercial partners interested in developing methods of boronating cargo molecules like proteins and drugs to enhance their uptake in cells.
OVERVIEWThe utility of many biologic drugs is limited by inefficient delivery into cells. Strategies to overcome this limitation have included enhancing the attraction between positively charged drug agents and the negatively charged cell surface. Other efforts have focused on natural ligands to target and bind agents to specific receptors on the cell surface.

Such methods have been used to deliver pharmaceuticals, proteins, peptides, nucleic acids and other particles into cells. While this has yielded some success, there remains a need for additional delivery strategies.

One promising approach takes advantage of the dense forest of polysaccharides, known as the glycocalyx, found on the surface of many cells. Targeting therapeutic agents to the glycocalyx could boost their cellular uptake.
THE INVENTIONUW–Madison researchers have developed methods for boronating cargo molecules to mediate their entry into mammalian cells via the glycocalyx. ‘Cargo’ molecules include drugs, proteins, labels, amino acids or any other desired molecule.

Boronation methods include ligating, crosslinking or otherwise bonding phenylboronic acids/oligopeptides to the cargo molecule. It is believed that the boronates undergo complexation with glycans on the cell surface. This facilitates the molecule’s entry into cell endosomes, where the cargo is released by enzyme action.
BUSINESS OPPORTUNITYThis invention provides a new means of delivering molecules into mammalian cells. Presently, the most common method in use is LipofectamineTM (Invitrogen Inc.), which has annual sales near half a billion dollars. However, LipofectamineTM can only be used in vitro and not to deliver drugs. Also, its reagent is retained in the cell membrane. The new approach has neither of these limitations.
  • Boronate-mediated delivery of drugs, proteins, nucleic acids and other molecules
  • Cellular uptake of molecules is enhanced significantly.
  • Delivery could take place in vivo or in vitro.
  • Method is straightforward.
For More Information About the Inventors
Contact Information
For current licensing status, please contact Jennifer Gottwald at or 608-960-9854.
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UW–Madison has the integrative capabilities to complete many key components of the drug development cycle, from discovery through clinical trials. As one of the top research universities in the world, and one of the two best-funded universities for research in the country, UW–Madison offers state-of-the-art facilities unmatched by most public universities.

These include the Small Molecule Screening Facility at the UW Comprehensive Cancer Center; the Zeeh Pharmaceutical Experiment Station, which provides consulting and laboratory services for developing formulations and studying solubility, stability and more; the Waisman Clinical Biomanufacturing Facility; the Wisconsin Institute for Medical Research, which provides UW–Madison with a complete translational research facility; and the innovative, interdisciplinary Wisconsin Institutes for Discovery, home to the private, nonprofit Morgridge Institute for Research and its public twin, WID, part of the university's graduate school. The highly qualified experts at these facilities are ready to work with you to create a library of candidates for drug development.