PTG2: Hydrosolubilizing Polymers

The technology is based on a family of triblock copolymers called PTG2 that do not contain poly(propylene oxide) block and poly(ethylene oxide) blocks like pluronics. PTG2 mediates solubilization of very hydrophobic drugs. For instance, curcumin is highly solubilized with PTG2. Consequently, curcumin solubilization promotes its internalization in cells. Curumin has been proposed to cure Cystic fibrosis (CF), the most lethal genetic disease caused by mutations in the gene encoding the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Cl- channel resulting in abnormal chloride transport at the plasma membrane of many tissues and organs. ΔF508 is the most common mutation of CFTR causing a misfolding of the CFTR protein and its retention in the endoplasmic reticulum (ER) for subsequent proteolytic degradation by the ubiquitin-proteasome pathway. Cur can partially compensate the ER retention of the defective CFTR protein. Very interestingly, Curcumin/PTG2 promotes the restoration of the expression of the CFTR protein in the plasma membrane of F508del-CFTR cells (Gonçalves et al., 2017 Eur J Pharm Biopharm. 117: 168-181).

Several PTG2 are available.