Poorly soluble drugs are a problem. The body generally sees them as alien invaders and works like crazy to get them out of the body. It's an especially big problem for lipophilic drugs like Docetaxel, an anti-cancer drug that is quickly expelled from the intestine. One possible solution comes from Yissum Research Development, the tech transfer company of the Hebrew University of Jerusalem. Yissum reports what it's calling promising preclinical results for its a nanotech-enabled drug-delivery platform.
The technology, invented by Simon Benita, head of the Institute for Drug Research at the university, enables controlled release and increased bioavailability of oral lipophilic drugs. The problem is that a protein pump called P-glycoprotein quickly flushes the drug Docetaxel out of the intestine wall cells. Docetaxel is poorly soluble in water, so it is delivered only intravenously after being forced into solubility by surfactants, often increasing adverse side effects. What Benita and his team have done is formulate the drug into nanocapsules that are then packed into microparticles in a way that prevents expulsion from the gut. The result, the researchers say, is better oral bioavailability along with prolonged release of the drug.
Preclinical trials on rodents show oral bioavailability of the drug was 10 to 20 times higher than other oral delivery methods. Plus, the rats did not suffer from immediate side effects, the researchers said.
"Patients in need of this drug will thus greatly benefit from the ability to receive the drug in lower doses using an oral route," Yaacov Michlin, CEO of Yissum, said in a statement. "The new delivery platform has been previously shown to be effective also for other drugs, and offers a revolutionary method to bypass specific potent barriers in the intestine and the liver, thereby greatly increasing bioavailability."
- take a look at the news release