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XR17 technology platform

A significant problem in product development for new pharmaceuticals is that many promising substances are insoluble in water. In many cases, a promising substance may be discontinued due to insufficient water solubility. Alternatively, different carriers can be used, for example in the form of polymers or oil derivatives. These carriers may often give rise to adverse effects that can be severe. Adverse effects, caused by the carriers, have been accepted in cancer treatment since the drugs are effective and the alternative would otherwise be that the patient is not treated.

In the light of this, Oasmia developed and patented XR17 platform is special in that is it is able to increase solubility of insoluble compounds. XR17 is based on a mixture of two derivatives (XMeNa and 13XMeNa) of vitamin A. The nanoparticles that XR17 forms with the API are called micelles and are between 20 and 60 nanometers in size. It has a water-soluble (hydrophilic) outer and a fat-soluble interior, which means that molecules that are poorly soluble in water will be enclosed in the micelle core resulting in water soluble properties of the micelle-drug nanoparticles allowing administration into the blood. As a comparison, a strand of DNA is two nanometres wide, a red blood cell approximately 7,000 nanometres and a human hair approximately 70,000 nanometres. Since XR17 in itself is well tolerated by the body, treatments with insoluble substances can be made more effective and adverse effects from other solubility enhancers (for example Cremophor (“CrEL”)) can be reduced. 

Advantages of XR17

The XR17 technology makes it possible to encapsulate both individual APIs and combinations of many APIs with different solubility profiles. The beneficial properties of XR17 have been confirmed by Oasmia’s toxicological and clinical studies. Oasmia assesses that possible advantages of XR17 are that it:

  • Improves solubility, which results in a safer way of administering APIs to humans and animals intravenously;
  • Shortens the infusion time, which makes the treatment more convenient for patients; and
  • Removes risk of serious hypersensitivity reactions against existing solvents such as CrEL and polysorbate 80, hence reducing the need of required premedication.