A major pharmacological challenge has been the application and delivery of hydrophobic compounds as therapeutic agents. While some hydrophobic compounds may yield to chemical manipulation or emulsification, many still suffer solubility and delivery challenges. We have looked to the body’s natural mechanism for transporting insoluble compounds to develop a novel platform for delivery of these type of useful bioactive molecules.
NanoDisk is an elegant and versatile ternary complex that is the foundation of Lypro’s emerging pipeline. The scaffold binds the perimeter of the lipid bilayer, stabilzing it. The lipid bilayer provides the hydrophobic milieu entrapping the bioactive agent. The bioactive agent can be small hydrophobic molecules such as antibiotics, bioactive lipids and siRNA, to which water solubility is conferred.
While the NanoDisk platform enhances bioavailability, it can also provide specificity. Specificity may be achieved in two main ways: active targeted drug delivery, such as with antibody therapeutics, and passive delivery through enhanced tissue penetration and retention. Lypro’s platform enables both active and passive routes of delivery. The scaffold, lipid, or bioactive agent can be modified to confer targeting. The nanometer size and biocompatible nature of NanoDisk facilitates their passage through tumor vasculature and other cellular barriers. Broadly speaking, NanoDisk enhance therapeutic delivery in the following ways:
- Solubility: Bioactive agents can be solubilized as effectively as detergents.
- Enhanced potency: Less bioactive agent needed for an equivalent biological outcome improves safety.
- Enhanced Specificity: Ability to engineer NanoDisk to provide tissue specific targeting.
- Stability: Resistant to light and/or oxidation induced degradation.
- Self assembly / Ease of manufacturing: Formulation of NanoDisk is facile. Room temperature storage in a dry state facilitates an efficient supply chain. Lyophilized NanoDisk can be rehydrated with retention of characteristic properties.
- Multiple modes of administration: Intravenous or pulmonary administration are effective means to achieve systemic delivery. Work is underway to document transdermal, trans-sinus, topical and oral delivery.
Lypro has an exclusive license to the Ryan patent portfolio from Children's Hospital of Oakland Research Center. Patents have issued globally including in the United States, Europe, Japan, Australia, India and Canada.
Developed under the direction of Gladys Monroy, Ph.D., J.D., Kimberly Bolin, Ph.D. and Suzanne Haendel, J.D.
Gladys Monroy is a partner at Morrison & Foerster and a member of the Patent Hall of Fame
Kimberly Bolin is senior patent agent at Morrison & Foerster
Suzanne Haendel is the Director of Technology Transfer at Children’s Hospital of Oakland Research Institute