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antidotes for the next generation of single-dose opioid overdose



IMAGE: covalent nanoparticles (top) release naloxone (purple structure) slowly over 24 hours.
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Credit: Marina Kovalyov

ORLANDO, Fla, May 31, 2019. – US epidemic of opioid gonyut unprecedented surge in deaths Fentanyl and other synthetic opioids. powerful effects fentanyl & # 39 are durable and even a tiny amount of the drug can lead to an overdose. Antidotes such as naloxone, Sun last long enough in the body to fully confront the drug that requires repeated Institute & # 39; ektsy. Now, scientists report that they are developing a single dose, the duration of opioid antidote using polymer nanoparticles.

The researchers will present their results today at the American Chemical Society (ACS) Spring 2019 National Meeting & Exposition. The ACS, the world's largest scientific society, is meeting here through Thursday. It has about 13 000 presentations on a wide range of science.

"We became interested in this problem when you try to do without painkillers addiction,» Saadyah Averick, PhD, he says. "In the process of research, we realized that the current limitation of opioid antidote."

According to the US Centers for Disease Control and Prevention, opioids such as heroin, oxycodone and fentanyl, has been implicated in more than 47,000 deaths from overdosage in 2017. These drugs all bind to the mu-opioid receptor (MOR) in the brain, which is a & # 39 is the body's natural satisfaction receptor explains Averick, a scientist at the Institute of Allegheny Network Health Research. "The drugs bind, activate the receptor and stimulate a sense of euphoria. Synthetic opioids, such as fentanyl, to turn this really, really good, "he says.

And their effects are durable. Fentanyl, which is much stronger than morphine, other opioids, can be absorbed in fatty tissue, which protects it from immediately metabolized. Then slowly released from the tissue, causing effects for several hours. Naloxone antagonist MOR and antidote, remains only in the system for about 30 minutes to an hour, however. Because of this discrepancy, repeated doses are needed to help the patient to recover. But not all patients want to go through the entire course of treatment, and they may eventually succumbed to an overdose after naloxone is metabolized.

Designed to ensure that stable, sufficient dose of the antagonist is fed for 24 hours to overcome this problem, Averick and his colleagues developed a drug delivery system. Researchers reacted naloxone, which has a multi-ring chemical structure from polylactic acid (PLA), thereby creating a polymer naloxone. They then received covalent nanoparticles (CNPS) by addition of the polymer to a solution of polyvinyl alcohol. They used a different analytical methods for the purification and analysis of the particles was 300 nanometers in diameter.

"In collaboration with the laboratory of Benedict Kolber at Duquesne University, proof of concept study showed that these nanoparticles are sufficiently straightforward naloxone release time to block the analgesic effect of morphine for 24 hours,» Averick notes. "As a next step, the study will be extended to fentanyl." While the latter work was done with mice, future studies will include an animal model that more accurately simulates how people metabolize opioids.

The researchers also plan to investigate how the exemption affects the particle size of nanoparticles with naloxone. "Ultimately, we hope to develop therapeutic interventions for fentanyl overdose, which can be used in this area, possibly forcing a short action of naloxone as an antidote to an overdose of choice," says Averick. "We expect that this drug delivery system would also be effective for other non-opioid fentanyl."

Given the fact that naloxone and other compounds, uses of teams have already considered safe, Averick predicts that the market for time-may be less than five years for a system of nanoparticles.


Press conference on this topic will be held Monday, April 1, at 9 am, Eastern Time in Orange County Convention Center. Journalists may check in at the press center. Number W231B, or watch live on YouTube HTTP: // bit.LY /ACSLive_Orlando2019 ( «ACSLive_Orlando2019» with & # 39 is case-sensitive). To ask a question online, sign in with your Google account.

The researchers acknowledge the support and funding of the Allegheny Health Network Neuroscience Institute.

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Opioid antidote next generation: covalent nanoparticles for delivery of opioid antagonists Mu


The growth of synthetic opioids has emphasized the need for new long-acting opioids antidotes. Currently available antidotes to reverse opioid overdose (eg Naloxone) has a short half-life pharmacokinetic due to rapid metabolism in the liver. Because of the relatively long time blood synthetic opioids such as fentanyl may be from & # 39; reality known as renarcotization. The short half-life of these antidotes requires multiple doses of retries turn synthetic opioid overdose. We present a new polymer-based drug delivery system which includes a high loading of naloxone in polymer nanoparticles with a zero order sustained release formulation to act as long-acting opioid reversal agent.

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