| WARF: P05226US |  |
| Micelle Composition with Enhacing Drug Loading Capacity and Stability |
| INVENTORS | • | Glen Kwon, Marcus Forrest |
The Wisconsin Alumni Research Foundation (WARF) is seeking commercial partners interested in developing a micelle composition that can be used to deliver relatively insoluble therapeutic compounds.
OVERVIEW
Many powerful drugs have only limited usefulness because they are relatively insoluble in aqueous solutions. For example, the anti-cancer and immunomodulatory compound rapamycin exhibits impressive activity against many tumor models but is difficult to deliver to tumor sites in vivo because of its low solubility. Current methods of delivering such compounds often involve highly toxic solubilization agents, which limit how much of the active compound can be administered. Polymeric micelles, which circulate in the blood for prolonged periods, can serve as vehicles for the targeted delivery of such compounds. Micelles are unique among drug carrier systems because of their biocompatibility, nanoscopic dimensions, hydrophilic shell and hydrophobic core. Some of these micelles are FDA approved, while others are in clinical trials.
Polymeric micelles are formed by mixing an amphiphilic polymer, such as PEG-DPSE, and a hydrophobic passenger drug, such as rapamycin, into an organic solvent to form a solution; removing the solvent from the solution; and resuspending the solvent-free mixture in water or buffer. The micelles then can be administered intravenously to a patient undergoing treatment for cancer or another disease. However, the degree to which any given passenger drug compound can be loaded into a micelle for therapeutic use is limited by the structural relationship between the compound and the hydrophobic core of the carrier.
THE INVENTION
UW-Madison researchers have developed formulations for efficiently loading hydrophobic compounds into polymeric micelles. Adding alpha-tocopherol (vitamin E) as an excipient enhances the drug loading capacity and stability of the micelles, possibly by modifying their core properties. PEG-DPSE micelles containing rapamycin normally come out of solution in less than two hours; however, when tocopherol is added, the micelles are stable for several days. The addition of tocopherol also increases the loading of rapamycin into the micelles more than three-fold. Similar results have been obtained with novel analogs of the HSP 90 inhibitor geldanamycin.
APPLICATIONS
- Delivering insoluble therapeutic compounds
- Treating cancer and other diseases
- Combination therapy
KEY BENEFITS
- Allows solubilization of potential drug candidates, such as rapamycin and analogs of geldanamycin, previously thought to be incompatible with existing polymeric carriers
- Significantly enhances the drug loading capacity of polymeric micelles
- Improves administration of combination therapy
- Enhances the stability of micelles
- Does not significantly affect the size of the micelle composition
- Vitamin E is not toxic to living organisms
- Micelle compositions are easy to store and deliver, circulate in the blood for a long time, are excreted by the kidneys at low levels, and can be targeted to tumors
ADDITIONAL INFORMATION
For More Information About the Inventors
Intellectual Property Status
Tech Fields
Drug Discovery - Drug delivery
FIGURES
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| Schematic illustration of micelle formation and a micelle-encapsulated drug. |
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| Transmission electron microscopy image of block copolymer micelles (18,000x). |
CONTACT INFORMATION
For current licensing status, please contact our team at
licensing@warf.org
or phone 608.262.4924. (Clicking this link will open a contact form in a popup window. If you have problems viewing the form, try disabling your popup blocker software.)
WARF: A Leader in Technology Transfer Since 1925
Since its founding as the patenting and licensing arm of the University of Wisconsin-Madison, WARF has been working with business and industry to transform university research into products that benefit society. WARF intellectual property managers and licensing staff members are leaders in the field of university-based technology transfer. They are familiar with the intricacies of patenting, have worked with researchers in relevant disciplines, understand industries and markets, and have negotiated innovative licensing strategies to meet the individual needs of business clients.
The University of Wisconsin and WARF -
A Single Location to Accelerate Translational Development of New Drugs
The 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 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 soon, the Wisconsin Institutes for Discovery, made up of innovative private and public interdisciplinary biomedical research institutes. The highly qualified experts at these facilities are ready to work with you to create a library of candidates for drug development.
Since its founding as the patenting and licensing arm of the University of Wisconsin-Madison, WARF has been working with business and industry to transform university research into products that benefit society. WARF intellectual property managers and licensing staff members are leaders in the field of university-based technology transfer. They are familiar with the intricacies of patenting, have worked with researchers in relevant disciplines, understand industries and markets, and have negotiated innovative licensing strategies to meet the individual needs of business clients.
The University of Wisconsin and WARF -
A Single Location to Accelerate Translational Development of New Drugs
The 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 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 soon, the Wisconsin Institutes for Discovery, made up of innovative private and public interdisciplinary biomedical research institutes. The highly qualified experts at these facilities are ready to work with you to create a library of candidates for drug development.
