18 February 2019

For topical use

An analgesic that is less addictive than morphine has been tested on rodents

Lina Medvedeva, XX2 century

Morphine is an extremely effective painkiller. The problem is that it is an opioid, and it is addictive and threatens to die from an overdose.

Researchers from France have found an alternative that they claim is less addictive than morphine or synthetic opioids. In addition, the results published in Science Advances (Feng et al., A new painkiller nanomedicine to bypass the blood-brain barrier and the use of morphine) show that the pain-relieving effect of the new drug lasts longer than that of opiates.

The drug has only been tested on rodents so far, so we'll have to wait to see if the effect is transferable to humans.

The scientific justification for the effectiveness of the drug is that peptides contained in our body, for example, enkephalins, bind to opioid receptors. In theory, they are less conducive to abuse than drugs such as morphine because they target peripheral opioid receptors close to the source of pain, rather than central opioid receptors located in the brain. However, they were not used in practice due to various difficulties, including problems with overcoming the blood-brain barrier.

To get rid of these obstacles, the researchers attached a leucine-cephalin peptide to a natural and biocompatible lipid called squalene. The resulting drug can be delivered directly to the source of pain by injection.

To test the effectiveness of pain relief, the researchers injected three different versions of the new drug into mice with inflamed paws. Also, the mice were injected with a fluorescent agent capable of accumulating in those places of tissues where the animal is experiencing pain. By recording the fluorescence in real time after the drug was administered, the scientists were able to identify signs that the sensitivity to pain in the paws of rats was reduced within four hours. It was noted that the analgesic effect of the new drug lasted longer than the effects of morphine.

painkiller.jpg

Images of mice with an inflamed paw immediately after the injection of an anesthetic and at various intervals, taken by the IVIS Lumina system, designed to record bioluminescence and fluorescence.

This is a promising discovery, but so far we only know that the drug worked on rodents. Before it can be prescribed to patients, it must undergo clinical trials, and this may take some time.

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