The use of an amphipathic weak base having defined characteristics for the preparation of a pharmaceutical formulation for the treatment or prevention of neurodegenerative conditions. keywords: liposomes

Blood brain barrier penetration by tempamine encapsulated in liposomes

Highlights

• The invention involves the use of tempamine (TMN) encapsulated in nano sterically stabilized liposomes (nSSL). TMN is a unique antioxidant due to its activity as an oxidant and a reductant, it has the ability for partial self regeneration. As an amphiphatic weak base TMN can cross the blood brain barrier (BBB) and penetrate cells.

The Innovation

• The invention is based on the following novel findings:
• TMN protects PC12 neurons against oxidative damage in a dose dependent manner.
• nSSL-TMN formulations are effective in penetrating the BBB in experimental autoimmune encephalomyelitis (animal model for Multiple Sclerosis (MS)).
• The nSSL-TMN formulations are efficacious in preventing attacks and, more important, during the peak of the disease attack.

Key Features

• The nano-liposomal formulations could be beneficial for treatment or prevention of neurodegenerative conditions, particularly those requiring penetration of a medication through the blood brain barrier.

Development Milestones

• Successful animal trials demonstrated that intravenous administration of nSSL-TMN was more effective in reducing the clinical signs of MS as compared to the signs observed with conventional medications (Copaxone/Betaferon) or as compared to empty nSSL liposomes or free TMN.
• Two different liposomal formulations encapsulating TMN were found to be significantly effective in reducing clinical signs of Parkinson's disease in animal preliminary studies.

The Opportunity

• The World Health Organization (WHO) estimates that over 2.5 million people globally suffer from MS, ~400,000 of them in the USA and 500,000 in Europe, with large economic implications for healthcare providers. In 2006, disease modifying drugs generated total global revenues of $5.4 billion, continuously expanding with annual growth rate of 20%.

project-id 12-2006-534

Patent pending. Publication WO 2006027785