The brain is protected against invading organisms and unwanted substances by the blood–brain barrier (BBB). The BBB also blocks the transport of drugs and diagnostic agents into the brain, making delivery to the brain challenging.
Curtin University researchers have developed a delivery system which uses nanoparticles combined with dual targeting ligands for delivery of a wide variety of payloads into the brain. The ligands target:
1) the BBB (or the nasal mucosa membrane as an alternative entry point); and
2) the neuronal cells inside the brain.
Dual targeting promotes both the transport into and the residence time of the payload inside the brain.
The ‘Nanodelivery’ system is capable of delivering a single or dual payloads to the target. The payload can be small molecules, antibodies, DNA, RNA, proteins and peptides for use as therapeutic or diagnostic agents, sensors, labels and trafficking molecules. The payload can be hydrophilic or hydrophobic, small or large, and can be incorporated individually into nanoparticles or in a combination. The Nanodelivery system can be used in animals or humans via either intravenous or intranasal route of administration.
This platform technology can overcome the challenge of delivery across the BBB. In doing so, it opens up the opportunities for new diagnosis and treatment of central nervous system diseases (CNS) such as brain infection, brain tumour, Parkinson’s disease, dementia, Alzheimer’s disease and stroke. This technology can be used to reformulate existing drugs for more effective use in the brain.
Our technology offers the following advantages:
- Dual payload
- Versatile, suitable for water soluble, water insoluble, small or large molecules as payload
- Biocompatible and biodegradable
- Unique dual ligand technology which can target different cells for transport into the brain and prolonged residence of payload.
- Sustained release of payload
- Long-term stability of payload
Dr Yan Chen of Curtin University’s School of Pharmacy and Biomedical Sciences is the leader of the research team. Dr Chen is an experienced researcher in micro/nanotechnology for drug delivery, has worked for a large pharmaceutical company and is also inventor of several controlled-release drug formulations.
Stage of development
The proof-of-concept studies have been completed in an in vitro BBB model showing cellular uptake and enhanced transport across the tight junction. These cellular studies also confirmed the Nanodelivery system is not toxic.
Brain uptake has been demonstrated in vivo in a rat model using rivastigmine (an anti-dementia drug), demonstrating a more than 6-fold increase in the amount of drug delivered into the brain, when compared to the conventional drug solution given intravenously.
The further testing of the Nanodelivery system in an animal model of Alzheimer’s disease is underway.
Curtin is seeking partners to support the further development and testing of this platform technology in pre-clinical testing, with a view to identifying a drug to take into clinical trials.
Russell Nicholls – Deputy Director, Commercialisation, Curtin University
Phone: +61 410 285554