SBIR Phase I: Triblock copolymer micelles for enhanced drug solubilization and stability

Delaqua Pharmaceuticals Inc, Chapel Hill NC

Investigators

Abstract

The broader impact/commercial potential of this Small Business Innovation Research (SBIR) Phase I project is rooted in enhancing the therapeutic use of hydrophobic drugs and yielding improved treatment outcomes with fewer side effects. The proposed technology has the potential to revolutionize the pharmaceutical field by increasing the bioavailability of known hydrophobic drugs and stabilizing new drugs. The technology will improve the health of the American population by allowing more therapeutic to be injected at lower volumes, thereby increasing therapeutic availability and efficacy. The platform will enhance America’s economic competitiveness in the global nanopharmaceutical market by providing a critically needed solubility-enhancing carrier platform. Research, sales, manufacturing, and management jobs will also be created domestically. The technology will engage with pharma companies and academic research groups on the evaluation, co-development, and licensing of novel drug formulations that improve the therapeutic window and reduce side effects. The platform will hasten the development and success rates of therapies that address the unmet medical needs of patients suffering from a broad spectrum of indications including cardiovascular conditions, cancer, infectious diseases, and neurological conditions like Alzheimer’s and dementia. This Small Business Innovation Research (SBIR) Phase I project will enhance the efficacy and safety of hydrophobic drugs and drug candidates through a polymeric micelle approach to drug solubilization. Estimates suggest 40% of approved drugs and 90% of molecules in the discovery pipeline are poorly soluble, thereby hindering bioavailability and efficacy and preventing many late-stage drug candidates from reaching the market. Current solubility-enhancing drug carriers require high amounts of inactive excipients, which adds costs and complexity and may cause adverse side effects. As such, there is a clear need for improved drug delivery methods. This Phase I work will establish the capabilities and safety of the polymeric micelle platform as a robust and widely applicable method of solubilizing and stabilizing hydrophobic drugs to enhance therapeutic efficacy. Objectives are to 1) improve formulation of spherical micelles for enhanced stability and drug solubilization, 2) perform initial toxicity study on polymeric micelles establishing the safety of the platform, and 3) demonstrate efficacy of the platform for solubilization of compounds of different drug classes. The proposed work will generate a scalable, well-characterized, and improved polymeric product for solubilizing active but poorly soluble active pharmaceutical ingredients, thereby enhancing clinical development and commercialization of much-needed therapeutics. This award reflects NSF's statutory mission and has been deemed worthy of support through evaluation using the Foundation's intellectual merit and broader impacts review criteria.