by
Robert Gorter, MD, PhD.
February 5th, 2021
Let me try to explain in as simple terms as possible the benefits and risks of direct delivery of drugs and nanoparticles through the nose to the brain.
1) The brain is protected to some extent by the Blood-Brain Barrier, which means that many molecules and substances toxic to the brain are kept out of the central nervous system.
2) High up in the nose, the skull is very thin between the roof of the nose and the brain (about 4-5 mm) and there are two options for drugs from nanoparticles (chips? graphene oxide?) to be deposited in the brain: a) through the thousands of olfactory nerve fibres, which penetrate the nasal mucosa directly from the brain through the sieve bone b) through nanoparticles loaded with a drug (e.g. chemotherapy), which enter the brain like a “Trojan horse”.
3) We are witnessing a rush in current science to develop nano-particles to deliver into the brain: one may ask why?
4) Some liposomes (fat globules) have been developed as nano-particles to deliver drugs, which otherwise would have filtered out and remained in the bloodstream to be detoxified in (usually) the liver and/or kidneys.
5) These nanoparticles are fully synthesised and practically nothing is known outside the pharmaceutical industry about their structure or possible short- and long-term toxicity. A legitimate concern is that autoimmune diseases will appear.
6) When applying for a patent, the company or researcher in question must be able to demonstrate the benefits, etc. But filing a patent application keeps all information, which is new, secret until a patent is granted. This is to protect the patent applicant from having sensitive data stolen by rival pharmaceutical companies.
7) Why is the nose suddenly so popular for delivering drugs and nanoparticles to the brain? The barrier between the roof of the nose and the brain is very thin (about 4-5 mm) and porous bone tissue. It is part of the base of the skull (see figures in the text) and the olfactory nerves are multiple and penetrate the lamina cribrosa (sieve bone) through these tiny openings.
I have thoroughly reviewed the current scientific literature and summarised what I found. And at the end, you will find references to scientific publications.
Our concern is that these forced-upon intranasal testing for the presence of COVID-19 has been (and is still being) conducted to implement micro-chips and graphene oxide into the brain of that person.
Current drug delivery for disease processes in the brain (tumours, Parkinson’s, Multiple Sclerosis (MS), epilepsy, infections) to the brain and cerebrospinal fluid (CSF) is often severely hampered by the blood-brain barrier.
Intranasal drug delivery is non- or minimally invasive and offers a new but opportunity for drug delivery. Recent nanotechnology research and many patent applications around the world are mainly focused on overcoming typical limitations, including bioavailability, transport, brain-blood-barrier, targeted release, controlled release rate and controlled degradation. But global patent applications in recent years are specifically about new nanotechnology, which reach beyond drug application but can also affect our thinking and feeling.
Neuralink, Elon Musk’s neuro and nano-technology company, has lifted the veil on some of his ambitions to implant chips in people’s brains to improve mental and physical functioning through artificial intelligence (AI).
During a question-and-answer session during a live presentation on 17 July 2019, Musk surprised his Neuralink colleagues by announcing that the company had tested its AI technology on monkeys and pigs and with promising success.
Musk said that “a monkey was able to control a computer with its brain”, although he did not elaborate on what this entailed, but later shared that the rhesus monkey was able to control a computer and simple computer games.
Neuralink chief executive Max Hodak said he wished the company did not have to experiment on animals, but that it was a necessary “step in the process of having its technology ready to implant chips into human brains to improve mental performance and skills.”
Musk started Neuralink in 2016 and the company remained relatively under the radar until 2017 when the Wall Street Journal broke the news that he had founded the company to “merge computers with human brains”.
Developing brain chips is a curious afterthought for a man who simultaneously runs Tesla, his space exploration company SpaceX and The Boring Company, which Musk hopes will dig underground transit systems for cities.
But Neuralink focuses on one of Musk’s main interests: artificial intelligence. Musk has expressed concern that artificial intelligence (AI) could one day possibly overshadow the human race. He has set up a general research organization called OpenAI, but Neuralink has a much more tangible, futuristic goal of creating AI devices that can interact with or replace people’s brains.
The biotechnology-related drug delivery systems, such as monoclonal antibodies, genetically manipulated proteins and synthesized mRNA, (micro-chips?) can be thought of as Trojan horses.
For questions, please email epub@benthamscience.net
References:
Chapman, Colin D et al.: Intranasal Treatment of Central Nervous System Dysfunction in Humans. Pharmaceutical Research http://link.springer.com/article/10.1007/s11095-012-0915-1/fulltext.html
Djupesland, Per G et al.: Accessing the brain: the nose may know the way. Journal of Cerebral Blood & Flow Metabolism (2013), 33, 793-794; doi: 10.1038/jcbfm.2013.41.
Lorenzetti, Laura: Is the future of pharma about making good drugs great? Fortune, 27.2.2015.
Pardridge, William M: Drug transport across the blood-brain-barrier. Journal of Cerebral Blood Flow & Metabolism (2012), 32, 1959-1972; doi: 10.1038 / jcbfm.2012.126.
Phukan K, Nandy M, Sharma RB, Sharma HK. Nanosized Drug Delivery Systems for Direct Nose to Brain Targeting: A Review. Recent Pat Drug Deliv Formul. 2016;10(2):156-64. doi: 10.2174/1872211310666160321123936. PMID: 26996366.
Agrawal M, Saraf S, Saraf S, Antimisiaris SG, Chougule MB, Shoyele SA, Alexander A. Nose-to-brain drug delivery: An update on clinical challenges and progress towards approval of anti-Alzheimer drugs. J Control Release. 2018 Jul 10;281:139-177. doi: 10.1016/j.jconrel.2018.05.011. Epub 2018 May 24. PMID: 29772289.
Zorkina Y, Abramova O, Ushakova V, Morozova A, Zubkov E, Valikhov M, Melnikov P, Majouga A, Chekhonin V. Nano Carrier Drug Delivery Systems for the Treatment of Neuropsychiatric Disorders: Advantages and Limitations. Molecules. 2020 Nov 13;25(22):5294. doi: 10.3390/molecules25225294. PMID: 33202839; PMCID: PMC7697162.
Tavanti F, Pedone A, Menziani MC. Disclosing the Interaction of Gold Nanoparticles with Aβ(1-40) Monomers through Replica Exchange Molecular Dynamics Simulations. Int J Mol Sci. 2020 Dec 22;22(1):26. doi: 10.3390 / ijms22010026. PMID: 33375086; PMCID: PMC7792802.