- Many active ingredients exhibit very low water solubility, severely limiting their bioavailability, therapeutic efficacy, and clinical use. Polytheragene offers triblock copolymers called PTG2, which have an excellent capacity to solubilize small, highly hydrophobic molecules. PTG2 has demonstrated excellent solubilization of curcumin, paclitaxel, pheophorbide A (PheoA), and N-acetylcysteine—extremely hydrophobic molecules with recognized therapeutic properties. This solubilization results in a significant increase in their therapeutic efficacy.
- PTG2 polymers offer several major advantages: low toxicity; high modularity; and ease of formulation and use.
- The technology is based on a family of triblock copolymers called PTG2, which enable the solubilization of highly hydrophobic molecules.
- For example, curcumin, which is insoluble in water, is very efficiently solubilized with PTG2, thus promoting its internalization into cells. Curcumin has been proposed as a treatment for cystic fibrosis (CF), the most lethal genetic disease caused by mutations in the gene encoding the chloride channel of the cystic fibrosis transmembrane conductance regulator (CFTR). These mutations lead to abnormal chloride transport across the plasma membrane of many tissues and organs. ΔF508 is the most common CFTR mutation, causing misfolding of the CFTR protein and its retention in the endoplasmic reticulum (ER) for subsequent proteolytic degradation via the ubiquitin-proteasome pathway.
- Interestingly, curcumin solubilized with PTG2 promotes the functional restoration of CFTR protein expression in the plasma membrane of F508del-CFTR cells (Gonçalves et al., 2017 Eur J Pharm Biopharm. 117: 168-181).
- Other hydrophobic molecules like those used in anticancer treatment are solubilizable with PTG2 and could be more efficient.
- Insoluble molecules are often used for cosmetic purpose, PTG2 could be useful.
- Polytheragene offers a variety of PTG2 polymers for the water solubilization of various hydrophobic molecules.
- Polytheragene provides its customers with lyophilized formulations containing a hydrophobic molecule (pheophobide α; paclitaxel; curcumin; N-acetylcysteine) and a PTG2 polymer, ready for use after rehydration in a specific volume of water.
- Polytheragene also offers its customers the option of selecting a suitable PTG2 polymer to solubilize their molecules of interest.
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