The blood brain barrier (BBB) is a highly selective semipermeable complex, and only about 2% of small molecules in the blood can penetrate it. Because of this, drug delivery to the brain is fairly ineffective. Research into receptors expressed on the BBB is promising, however, many receptors (glucose transporter 1, transferrin receptor, LDL-receptor related protein, etc.) are highly expressed in other tissues, organs or cells eliciting strong off-target effects. There is an urgent need for carriers with greater efficiency and lesser toxicity that can cross the BBB to deliver therapeutic agents and diagnostic agents to the brain.
Researchers at Arizona State University have developed novel functionalized nanoparticles (NPs) that are able to cross the BBB by targeting a membrane transport protein that is highly expressed on the endothelium of the BBB. These NPs can carry diagnostic agents for brain imaging, therapeutic or bioactive compounds for brain disease treatment, inhibitors for enhancing BBB permeability, and more. These NPs enhance drug delivery by prolonging the interaction time of the drug with the BBB to improve the possibility of penetration and using the transport function of the target to deliver a variety of agents across the BBB. The NPs can be administered via intravenous injection, intranasal route, transdermal patches, and possibly other routes. The targeted delivery approach will enhance brain delivery efficacy of agents and decrease their side effects and toxicity. Mice studies have been conducted to confirm binding and targeting.
These nanoparticles can carry and deliver a variety of agents to the brain for both diagnostic and therapeutic applications with the potential for low off-target effects and toxicity.
Potential Applications
- Delivery of agents across the BBB
- Treatment of brain cancers, neurodegenerative diseases such as AD, PD, ataxia, HD, motor neuron diseases and more, metabolic disorders, infections, opioid overdose, body temperature disorders, progressive supranuclear palsy, food intake disorders, temperature regulation, mood disorders, etc.
- Imaging of brain diseases
- Neural research
Benefits and Advantages
- The membrane transport protein that is targeted is highly expressed on the endothelium of the BBB with low expression in other tissues and organs
- Off-target effects should be very low
- High target specificity to the brain
- Targeted delivery of the nanoparticles could enhance therapeutic delivery efficacy with decreased side effects and toxicity
- Can be administered via IV injection, intranasally, transdermal patches, and more
For more information about the inventor(s) and their research, please see