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Experimental 'nano-painkiller' is more effective than morphine but has low addiction risk, scientists discover

Driven by opioid addictions, more than 70,000 Americns died of drug overdoses in 2017. Many experts blame prescription painkillers for starting the epidemic. But 1.5 billion people worldwide live with chronic pain - and there are no treatment options as effective as opioids. Researchers from Paris-Saclay University re-engineered a compound that exists in the body to treat pain with less addiction risk in rats.

Scientists believe an experimental 'nano-painkiller' could be safer, non-addictive alternative to the drugs fueling the current opioid crisis, according to a new study.

Collaborating researchers at Paris-Saclay University in France gave their innovative drug to rats with painful, inflamed feet.

The animals seemed to be in less pain, but didn't show any signs of dangerous side effects - namely, addiction - that come with opioid pain relievers.

In 2017, 70,237 Americans died of drug overdoses, driven by the epidemic. But 1.5 billion people around the world suffer chronic pain that can make every day unbearable.

We are in desperate need of safer ways to treat pain - and the international team of scientists hope they may have found one way of doing so.

Purdue Pharmaceuticals' drug OxyContin probably became the blockbuster that it did in part because it is so addictive - but also because it worked.

But the scales are quickly tipping on Americans' perception of the drug. It may be doing more harm than good.

This shift does not bode well for people in genuine need of pain relief though. Yet, so far, few treatments - including anti-inflammatory drugs and cannabis - have proven sufficient.

So the race is on to make the next generation of painkillers, without addiction.

Opioids bind with matching receptors to dull pain signalling and turn on the brain's reward and pleasure system.

But there are also natural compound in the body that act on these receptors, including a small peptide called enkephalin.

We know of four different opioid receptor systems – the Mu, Delta, Kappan and receptor like-1 sets.

Current opioid drugs like OxyContin bind with the Mu receptors.

But enkaphalin peptides are a match for the Delta systems.

On its own, enkaphalin struggles to cross the blood-brain barrier, a deficit that dampens its alleviating pain as effectively.

So Dr Patrick Covreur a leading nano-oncologist at and Universite Paris-Sud and his collaborators re-engineered enkaphalin with nanoparticles – tiny particles that scientists are increasingly using to make sure drugs are delivered as effectively and efficiently to their targets as possible.

The researchers fused the peptide and nanoparticles that make the new comgination more ‘attracted’ to the source of pain, and could move better through the body because they were dissolved in a natural type of biological fat.

When they gave the rats the new drug through an IV, the animals seemed to become less sensitive to pain, as tested by their responses when heat was applied close to the swollen tender paws.

What’s more, the nano-painkiller’s effects seemed to last longer than morphine’s did, the researchers reported.

Because the drug was acting on more peripheral opioid receptors, it presents less danger of addiction.

If the nano-painkiller has similar effects and proves equally safe in humans, it may be a promising option for the future of pain management.

14 February 2019


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