Many intravenously delivered Active Pharmaceutical Ingredients (APIs) are insoluble or poorly soluble in water. This can be a major hurdle in pharmaceutical development and may cause promising drugs to fail during the development process and may limit the application of approved drugs because of poor solubility. According to some estimates, between 70 and 90% of drugs in the development pipeline are classified as poorly soluble, with approximately 40% of approved drugs similarly affected.
Techniques to improve i.v. drug solubility, such as the use of solvents in the form of polymers or polyoxyl oil derivatives and ethanol, may give rise to acute and delayed adverse effects that can be severe. Adverse effects caused by carriers have been seen as an unpleasant trade off in cancer treatment and may necessitate the routine use of corticosteroid as premedication and slow infusions that limit patient flow in the busy chemotherapy suites.
To meet this unmet medical need and help improve the efficiency of the drug development process, Oasmia has developed and patented the XR-17 drug delivery platform. XR-17 increases the solubility of intravenously delivered compounds and enables Oasmia to develop innovative formulations of APIs. By combining XR-17 and an effective active pharmaceutical substance, Oasmia can create innovative and patent-protected drugs that benefit patients.
XR-17 is based on a composite of two derivatives of vitamin A. XR-17 forms particles, or micelles with an API that are just 20 to 60 nanometers in size. A human hair is about 80-100,000 nanometers wide.
Molecules that are poorly soluble in water are enclosed in the micelle core, where they can deploy into the blood. Because XR-17 is well tolerated, it makes treatments involving otherwise insoluble substances possible, without the high risk of the adverse side effects typically associated with commonly used solvents such as hypersensitivity reactions.
Oasmia’s initial focus for XR-17 is on cancer therapies, but the company believes XR-17 has potential applications in a wide range of diseases where poorly soluble APIs are a challenge.