University of Pittsburgh researchers have developed a novel formulation for the simultaneous delivery of Verteporfin and glutaminase inhibitors to the lungs and pulmonary blood vessels. Verteporfin, an FDA-approved drug for macular degeneration, inhibits the Yap/Taz pathway involved in tissue remodeling and extracellular matrix stiffening, which leads to pulmonary hypertension. Glutaminase inhibitors, such as C968 and CB-839, target the glutaminolysis pathway, a major energy source during pulmonary hypertension. This innovative approach aims to reduce pulmonary hypertension by blocking the Yap/Taz-GLS1 axis through controlled delivery of these drugs using poly(lactic-co-glycolic) acid (PLGA) particles.
Description
The technology involves the use of 10-micrometer porous PLGA particles to encapsulate Verteporfin and glutaminase inhibitors. These particles are designed to deliver the drugs to the deep lung tissue, ensuring effective treatment of pulmonary hypertension. The porosity and size of the particles allow for fast release kinetics, with the drugs being released within 1 to 3 days. This controlled delivery mechanism prevents the fast clearance of the drugs and reduces immune-mediated clearance in the lungs, enhancing the therapeutic efficacy of the treatment.
Applications
- Treatment of pulmonary hypertension
- Controlled drug delivery to the lungs
- Potential applications in other lung diseases involving tissue remodeling and extracellular matrix stiffening
Advantages
This technology offers a novel approach to treating pulmonary hypertension by simultaneously delivering Verteporfin and glutaminase inhibitors to the lungs. The use of 10-micrometer porous PLGA particles ensures that the drugs reach the deep lung tissue and are released in a controlled manner, enhancing their therapeutic efficacy. The combination of these drugs targets both the Yap/Taz pathway and the glutaminolysis pathway, potentially providing additive or synergistic effects in reducing pulmonary hypertension. Additionally, the controlled delivery mechanism reduces the risk of fast drug clearance and immune-mediated clearance in the lungs.
Invention Readiness
The technology is currently at the concept stage, with ongoing research to develop and refine the formulation. Previous studies have demonstrated the ability of PLGA particles to encapsulate similar drugs and deliver them effectively to deep lung tissue. The invention has the potential to significantly improve the treatment of pulmonary hypertension by providing a targeted and controlled delivery system for Verteporfin and glutaminase inhibitors.
IP Status
https://patents.google.com/patent/US20200276125A1