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Nanoparticle Drug Delivery Offers Hope for Chronic Pain

Researchers have taken the drug aprepitant—which is approved by the United States Food and Drug Administration but previously failed in clinical trials for pain—and repackaged it using a novel, nano-based technology to deliver the drug into specific compartments of nerve cells.

Researchers have taken the drug aprepitant—which is approved by the United States Food and Drug Administration but previously failed in clinical trials for pain—and repackaged it using a novel, nano-based technology to deliver the drug into specific compartments of nerve cells. The investigators report that nanoparticle-delivered aprepitant treated pain in mice and rats more effectively and for longer duration than conventional therapies, including opioids.

In the study published in Nature Nanotechnology, the authors focused on a G protein-coupled receptor called the neurokinin 1 receptor. They developed the novel treatment after discovering most pain drugs target receptors at the surface of neurons, when they should be targeting receptors within the neuron. Initially thought to function at the surface of nerve cells, activated receptors function for prolonged periods within a cell’s endosome. This activity drives pain.

The researchers developed a method that allowed nanoparticles to release aprepitant in endosomes containing the neurokinin 1 receptor, effectively blocking function in the receptor that signals pain.

The animals that received the drug via nanoparticle encapsulation experienced 3 hours to 5 hours of pain relief, whereas subjects who were given conventional antagonists or opioids were pain-free for an hour. Further trials are needed to determine if the treatment model is effective in humans.

From Dimensions of Dental Hygiene. February 2020;18(2):9.

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