Virpax -Model Envelta -Endogenous Enkephalin Intranasal Spray
Endogenous peptides with analgesic potential include endorphins via binding to the mu receptor, dynorphins via the kappa receptor and enkephalins via the delta receptor. Kappa and delta opioid agonists have been shown to provide analgesic benefit while sparing mu agonist toxicity1. Preclinical data supports analgesia from enkephalin without significant opioid tolerance or drug liking. Typically, exogenous enkephalins are rapidly degraded and have difficulty accessing the CNS2. Using a novel encapsulation method known as Molecular Envelope Technology (MET), leucine-enkephalin, or L-ENK can be delivered via an intranasal formulation of “protected” nanoparticles. MET increases dwell time in the nares promoting delivery via the olfactory route across the blood brain barrier and into the central nervous system.
- Neurons are exposed within the olfactory area of the nares4, facilitating the transport of drug compounds directly into the brain
- For nose-to-brain delivery, the dose must be deposited in the olfactory region, and thus, a specialized delivery device is required
- A propellant activated device has been identified that will be studied to deliver encapsulated enkephalin
TARGET MARKET
Severe post cancer pain and non-cancer analgesic market
DELIVERY SYSTEM
Intranasal Molecular Envelope Technology (MET)
POTENTIAL BENEFITS
- Enkephalin pro-drug formulation that targets delta receptors instead of mu receptors that are responsible for the majority of undesirable side effects associated with morphine
- Analgesic potential to manage acute and chronic pain, including pain associated with cancer, without the concerns of opioid tolerance, withdrawal, respiratory depression, or euphoria
- Our IND-enabling studies have determined that the MET intranasal delivery formulation bypasses the liver, avoiding potential drug to drug interactions if taking concomitant medicine
- When studied in rats, polymer nanoparticles were able to transport MET encapsulated L-ENK to the brain via the intranasal route
- Animals dosed with encapsulated L-ENK nanoparticles showed a strong anti-nociceptive response in multiple assays of evoked pain, including hot plate, Freund’s adjuvant (CFA), and spinal nerve ligation
- No analgesic tolerance was noted
- Animals dosed intranasally with unencapsulated LENK did not show an analgesic response. L-ENK was effective in morphine tolerant animals
- Conditioned place preference, a preclinical behavioral model used to study the rewarding and aversive effects of drugs, was not observed
- The National Institutes of Health (NIH) HEAL (Helping to End Addiction Long-term) Initiative is a government sponsored effort to speed scientific solutions to stem the national opioid public health crisis5
- Under the NIH HEAL Initiative, Virpax Pharmaceuticals entered a collaborative research and development agreement through the National Center for Advancing Translational Sciences (NCATS) of the NIH to study the pharmacology and safety of an intranasal enkephalin formulation for the treatment of pain