New Technology Boosts Oral Drug Delivery By 300%
Press Release | November 13, 2020

CBNS researchers have discovered a way to improve the efficacy of one of the most commonly prescribed drugs on the market, statins, by up to 300% – and which may have the capacity to revolutionise the absorption of a suite of drugs currently on the market and under development, increasing their activity without increasing toxicity.

The researchers have effectively developed a technology that packages a small amount of lipid molecules into a nanoparticle which, together with the drug, is equivalent to a large high fat meal, which aids the uptake of the drug, but without the cholesterol side effects.

The study has just been published in the journal, Drug Delivery and Translational Research.

Importantly the scientists have developed the technology, now patented, and taken it through to Phase 1 clinical trials where it showed that patients had a much higher absorption rate for the drug than that obtained from a pharmacist.

The technology is set to revolutionise what has been a significant problem in the development of new pharmaceuticals. Traditionally, almost half of new compounds identified by pharmaceutical industry screening programmes have failed to be developed because of poor water-solubility.

To test their technology they incorporated simvastatin – a commonly used cholesterol-lowering drug that reduces the risk of a heart attack – into their nanoparticles. Simvastatin is very poorly absorbed with generally only 5% of that taken orally ending up in the blood-stream.

The researchers, led by CI Professor Clive Prestidge and Ms Tahlia Meola from the University of South Australia found that – in a trial of 12 volunteers – the absorption of the nanoparticle-encased simvastatin was improved by 160% and, importantly, the essential metabolite of the drug, simvastatin acid, was increased in absorption by 350%.

According to Professor Prestidge, many drugs require some food to assist in the optimal passage of the medicine from the gut to the bloodstream where it can then travel to the target organ, “now we have developed a way to package a drug with a food effect driver, without the need for a full meal,” he said.

While simvastatin is a cheap drug, there are many other statins that are more expensive and this new technology may allow these drugs to be made more cheaply, because it allows for less of the actual statin to be used to achieve the same effect, Ms Meola said.

She added that the new technology could be delivering better and faster acting drugs within two years. The US Food and Drug Administration has a program, called the Biopharmaceutics Classification System (BCS), which is designed to speed up the approval of drugs which have had their bio-equivalence improved.

The CBNS technology has the potential to improve the bioavailability of a suite of currently available, but poorly soluble marketed drugs. A recent BCS classification of the 130 orally administered drugs on the World Health Organization’s list of essential medicines found that, of the 61 that could be classified with certainty, about one-quarter were poorly soluble.

According to Professor Prestidge, this new technology has the capacity to “rescue developmental compounds that were rejected owing to poor solubility or to improve drugs currently available which can now have their solubility improved,” he said.

“We have taken a new technology from proof of concept right through to clinical trial – which is a rare occurrence particularly for an Australian research group.”