[nanoPost] Controlled release drug delivery system

Company Israel

- The company has developed a controlled release drug delivery system (DDS), which is able to escape the P-gp (P-Glycoprotein) pump and bypass the extensive pre-systemic and liver first pass metabolism, resulting in increased bioavailability following oral administration, without drug molecule or any physiological process alteration .

- This unique structure will allow changing the route of administration of highly lipophilic and P-gp substrate drugs from injectable to oral with reasonably high bioavailability and low side effects.   
 
  
- The patented technology was successfully tested on small and large animals and is now ready for starting clinical trials on humans.

The Technology

- The developed lead proprietary technology platform (patent application) consists of microencapsulated drug loaded nanocapsules (double coated oil core droplets) in the form of powder, which can be incorporated within soft or hard entero-coated gelatin capsules. The enhanced availability of the drug in coated tiny oil droplets in the intestinal environment is achieved by microencapsulating the primary nanocapsules within a gel forming polymer coating membrane.
  
- This allows the controlled release of tiny drug loaded nanocapsules, rather than the release of dissolved drug in the intestinal fluids, thus protecting against GI enzyme degradation and pre-systemic metabolism, promoting P-gp escape and lymphatic uptake of the drug. 
   
- The controlled release of the double coated oil droplets prevents the absorption of the dissolved drug that reaches the portal blood, thus avoiding the hepatic First Pass Effect.
  
   
- Preliminary research of this technology, initially tested on the Tacrolimus drug, indicated that this method significantly enhances oral bioavailability of lipophilic CYP3A and P-gp substrate drugs.

- The  novel technology is not only enabling patent extension by potentially improving oral bioavailability, reducing dose frequency or inter/intra subject variation, but exhibits marked advantages and address unmet medical needs by altering the pharmacokinetic profile of complex and potent highly lipophilic drugs undergoing presystemic degradation and first pass effect.
 
- Release of small fraction of dissolved drug and drug-loaded nanocapsules from disintegrating microparticles