XEL 001HP – Huperzine A Transdermal Matrix Patch

What is Huperzine A?

Huperzine A is a naturally occurring Lycopodium alkaloid found in an extract from the club moss Huperzia serrata that has been used for centuries in Chinese herbal medicine. For past decades, Huperzine A has been a prescription medication in China for the treatment of dementia.

Huperzine A has been proven to be a powerful, highly selective and reversible inhibitor of acetyl cholinesterase (AChE), and easily crosses the blood-brain barrier. In addition, Huperzine A has anti-oxidative properties and possesses neuro-protective properties against glutamate that induces neuronal toxicity at the N-methyl-D-aspartate (NMDA) receptor. Furthermore, Huperzine A reduces the neurotoxic effects of β-amyloid and diminishes β-amyloid generation.

The clinical studies performed in China to-date showed Huperzine A to be more effective than other cholinesterase inhibitors currently on the market, and the US clinical Phase II trials with Huperzine A oral tablets conducted by Dr. Paul Aisen, the nation's leader for AD therapy clearly demonstrated the efficacy and safety of Huperzine A in the treatment of AD.

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What is the Mechanism of Action?

Huperzine A exhibits several mechanisms of action that are relevant to Alzheimer's Disease:

  • Acetyl cholinesterase (AChE) inhibition
    Huperzine A is a potent, selective and reversible inhibitor of acetyl cholinesterase (AChE), the enzyme that breaks down or degrades acetylcholine (ACh). ACh is a neurotransmitter (brain signaling molecule) associated with memory and cognitive function. ACh reductions have been associated with memory loss or cognitive impairment in AD patients. AChE inhibitor drugs inhibit the breakdown of ACh to make more ACh available. Currently four AChE inhibitors are on the market in the US for the treatment of mild-to-moderate Alzheimer's Disease and other cognitive impairment.
  • NMDA receptor antagonism
    Huperzine A also has N-methyl-D-aspartate (NMDA) receptor antagonist activity. The stimulation of NMDA receptors by the neurotransmitter glutamate has been implicated in the pathology of neurodegenerative disorders, including Alzheimer's Disease. Accordingly, a drug that blocks excessive NMDA receptor activity may protect against glutamate mediated excito-toxicity and nerve cell death. Currently, one NMDA receptor antagonist is on the market in the US, which has therapeutic effect on moderate-to-severe Alzheimer's Disease.
  • Anti-oxidant activity
    Huperzine A has anti-oxidant properties. The oxidative stress caused by free radicals or reactive oxygen species is one of the earlier symptoms in the pathogenesis of AD. Increased oxidation of lipid, protein and DNA molecules has been reported in both Alzheimer's Disease and mild cognitive Impairment. A human clinical study conducted in China with oral Huperzine A demonstrated significant reductions in blood markers of oxidative stress.
  • Anti-amyloid activity
    Huperzine A also exhibits anti-amyloid properties. The pathogenesis of AD patients shows the formation of amyloid plaques (senile plaques) on blood vessels and outside nerve cells within the brain, resulting in nerve cell death. Pre-clinical studies demonstrated that Huperzine A is protective against β-amyloid induced nerve cell death.

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What are the Benefits of Huperzine A?

  • Treatment of Alzheimer's Disease
  • Treatment of Vascular dementia
  • Treatment of cognitive and memory impairment
  • Learning and memory retention
  • Improved focus and concentration
  • Improved nerve transmission to muscles
  • Powerful and reversible long-term inhibitor of AChE activity in the brain
  • Dementia resulting from strokes and senile or presenile dementia
  • Improved clinical picture for patients with myasthenia gravis
  • Improved short-term and long-term memory in-patients with cerebral arteriosclerosis (hardening of arteries in the brain)
  • Alleviation of symptoms related to glaucoma
  • Prevention of organophosphate pesticide toxicity
  • Prevention of nerve gas toxicity

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Why is Huperzine A Transdermal Patch Better?

Transdermal drug delivery offers many advantages over tablets and other solid dosage forms, including reliable blood levels, improved drug absorption, minimized side effects, less frequent doses, and better patient compliance.

Our once-a-week Huperzine A transdermal patch can provide a better therapy over the current oral dosage forms, and is clearly preferable treatment method to AD patients and caregivers.

The pre-clinical study for the product development of the Huperzine A transdermal patch has been completed, and the prototype matrix patch is ready for IND filing for the further clinical development.

  • Formulation Development Report – complete
  • Formulation Specification Report - complete
  • Accelerated Product Stability Report - complete
  • Huperzine A HPLC Method Development and Validation Report – complete
  • Enhancer HPLC Method Development and Validation Report – complete
  • Report of Primary Skin Irritation (PSI) Study in Rabbits – complete
  • Report of Dermal Sensitization Study in Guinea Pigs - complete
  • Human Placebo Wearing Study Report - complete

Daily Delivery of Huperzine A from a 10 cm2 Transdermal Patch cross Human Cadaver Skin for up to seven days

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