Oral drugs that can pack more of a punch

More than 25 years of research by an Israeli professor has culminated in nanocapsules that can slip through our bodies’ defenses to deliver more curing power. It may be the latest scientific trend, but Professor Simon Benita of the Hebrew …

More than 25 years of research by an Israeli professor has culminated in nanocapsules that can slip through our bodies’ defenses to deliver more curing power.

It may be the latest scientific trend, but Professor Simon Benita of the Hebrew University’s School of Pharmacy has been working with nanotechnology since long before it had a name.

His 25 years of research in nanotech has culminated in a new vehicle for oral drug delivery based on the microencapsulated double-coated nanocapsules that he developed.

Normally, our bodies’ defenses would stop and break down orally administered drugs, so that we only benefit from about three-quarters of their potential effectiveness. Now, thanks to P-gpBypass, Benita’s invention, important cancer and HIV drugs as well as a range of immunosupressants should be able to slip through those defenses to treat disease more effectively.

The oral route is preferred, but only 40 percent of all drugs are water-soluble. This means that many drugs are administered intravenously, which is less effective and may lead to unpleasant side effects, or, they are delivered orally, in which case they have limited bioavailability.

Slipping through our defenses

When delivered orally, Benita explains to ISRAEL21c, drugs activate an intestinal pump barrier, the P-gp efflux pump, and are broken down in the intestine and the liver, losing about a quarter of their potency in the process.

“We took advantage of nanotechnology to design a Trojan horse similar to Taxol [a cancer drug],” says Benita. “It’s in a nanocapsule embedded in a micro-sphere, and not releasing into the intestine. . . it’s not activating the P-gp efflux pump. . . it is so small, it slips through.”

At 100 nm, Benita’s drug-laden nanocapsules are a new drug delivery system that could make painful injections and intravenous lipophilic drugs a thing of the past.

Creating a new drug delivery mechanism, “is not as simple as it looks,” says Benita stressing that there are “many, many companies” in the industry. “We are targeting one of the most challenging pharmaceutical issues with regard to formulation. More than 50 percent of drugs existing, or as new chemical entities . . . are not water soluble,” he tells ISRAEL21c.

Encouraging results from animal testing

Benita’s solution means that pharmaceutical developers can work around the intestinal pump, bypassing the gut enzyme metabolism, delivering maximum drug power without the side effects.

Benita and his team of four at the School of Pharmacy tested his platform recently on the immunosuppressant tacrolimus which is given to transplant patients to help prevent rejection of their new organs. Their tests showed that they could deliver the drug and unlock 2.4 times its bioavailability, or active ingredients, since their size provides protection from the GI enzymes in the intestines.

These encouraging results in animal studies led the Hebrew University’s tech transfer arm, the Yissum Research Development Company, to enter into a deal with Israel-based Aurum Ventures MKI, which will test the platform with the aim of refining it for commercial success.

Aurum Ventures MKI is the technology investment arm of Morris Kahn, a prominent Israeli businessman, philanthropist and entrepreneur.

Israel excels in drug delivery

“The ability to deliver lipophilic drugs orally while bypassing specific potent barriers in the intestine and the liver carries tremendous potential,” says Yehuda Yarmut, the deputy CEO of Yissum. “Benita, a seasoned inventor and entrepreneur and co-founder of Novagali SA, one of Yissum’s most promising spin-offs, has once again demonstrated his ingenuity in developing a novel mechanism addressing many unmet medical needs.”

In Israel, a relatively small country, there appears to be a disproportionately large number of drug delivery companies. Much of this has to do with the fact that Israelis like to be entrepreneurs, but also, says Benita, because at the Hebrew University’s School of Pharmacy there is a large number of researchers who are very skilled in drug delivery technologies. “We are considered worldwide very strong in drug delivery,” he says.

The researchers both influence their students, and work themselves to create drug delivery companies and spin-offs. Some 25% of the patents at Yissum are in drug delivery, “because of the strong expertise in our department,” says Benita.

Benita founded the nanotech company Novagali in France 10 years ago for ocular delivery of drugs using nanoemulsions. The company currently has major products at various stages of development to tackle dry eye, allergy, glaucoma, retinopathies and more.

Its formulations are based on the technology platforms of Novasorb and Eyeject, which optimize bioavailability of drugs as well as safety and comfort for the patient.

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About Karin Kloosterman

Karin Kloosterman lives in Jaffa, Israel. She is a journalist, writer and blogger who focuses on the environment and clean technology from Israel and the Middle East. Published in hundreds of newspapers around the world, Karin also writes for the Huffington Post and Green Prophet.