Proprietary drug delivery platform
TesoRx has developed a novel drug delivery platform (DDP) to reformulate and enhance the delivery of proven drug molecules into more effective treatments. Its proliposomal technology overcomes formulation challenges of drugs that are poorly water-soluble, have low membrane permeability, have high clearance metabolism or cause systemic toxicity. The DDP can be customized based on the active molecule and the route of delivery and has been successfully applied to both solid and liquid therapies.
The underlying technology was created by TesoRx co-founder, Dr. Guru Betageri, and exclusively licensed from Western University of Health Sciences (WUHS) in Pomona, California. Ongoing application of this DDP for new drug candidates takes place in TesoRx's research and development laboratories at the TesoRx Centre of Excellence in Pomona, California.
TesoRx has applied this delivery technology for its own products and has made it available to pharmaceutical companies reformulating legacy products or developing new ones.
Oral drug delivery - oral Testosterone
The main challenge with the oral delivery of Testosterone is the high first pass metabolism of the molecule in the gastrointestinal tract, which prevents systemic uptake of the hormone in the body. Testosterone is also poorly water soluble and has proven to be extremely difficult to administer in a safe and efficacious manner.
Utilizing TesoRx's DDP, Testosterone Undecanoate (TU) is reformulated as a solid proliposomal powder that is encased in an enteric coated capsule. The capsule bypasses gastric degradation in the stomach and releases the contents in the small instestines. The hydration of the powder in the intestinal lumen leads to the formation of liposomes in situ, which encapsulates the TU molecules, and leads to the absorption of the liposome directly into the GI lymphatic system (1).
Alkaline pH levels in the intestine cause the capsule to degrade, releasing proliposomal powder that spontaneously hydrates and forms micelles and liposome complexes for lymphatic absorption (2). By bypassing the liver, the DDP allows for excellent oral bioavailability of the drug.
Intravesical chemotherapy delivery - Proliposomal Intravesical Paclitaxel (PLIP)
The proliposomal intravesical paclitaxel (PLIP) formulation is in development for intravesical administration in the treatment of non-muscle invasive bladder cancer (NMIBC). LIPAC Oncology, a subsidiary of TesoRx Pharma, is leveraging PLIP to pursue targeted chemotherapeutics in NMIBC and additional indications.
Chemotherapy agents are sometimes delivered intravesically (direct instillation into the bladder) or intraperitoneally (direct instillation into the abdobminal cavity) during or following cancer surgery to improve patient outcomes, but are not approved for this use and have limitations in efficacy, formulation and in some cases, supply.
Paclitaxel, an agent known to be highly active in systemic application for urothelial carcinomas, is lipophilic and not solubilized in the acidic environment of the bladder. Paclitaxel has not been formulated or approved to be used intravesically in its current formulation. By utilizing LIPAC’s proprietary proliposomal formulation platform to enhance permeation and solubility, we have overcome the barriers to intravesical delivery of paclitaxel. LIPAC Oncology, a subsidiary of TesoRx, has conducted preclinical and clinical studies which demonstrated superior efficacy of this approach.
Read more about how this technology is applied to TesoRx's Bladder Cancer product.