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Scientific result | Brain | Pharmacology
A nano-drug has been developed for treating certain neurological diseases such as brain ischemia , as well as injuries to bone marrow. It is composed of a therapeutic molecule, adenosine, and the vector squalene, which allows it to circulate in the body and reach the areas to be treated.
Drug delivery in the body is a true pharmacological challenge, especially when treating diseases of the central nervous system. Many molecules are metabolized and quickly eliminated. Furthermore, they diffuse poorly through the blood-brain barrier that isolates the brain and spinal cord from the general circulation. Adenosine, a neurocompetent compound that acts on several receptors of the central and peripheral nervous systems, is one of them. It has never been used in the treatment of cerebral pathologies, due to its very short half-life after its administration in the blood (less than one minute), its potential side effects, and its inability to diffuse across the blood-brain barrier.
The Institut Galien, Hacettepe University (Turkey), and the CEA-IBITECS have performed and tested the vectorization of adenosine with squalene, a natural and biocompatible lipid. This assembly, in the form of 120-nm nanoparticles, was tested in murine models of cerebral ischemia and spinal cord trauma. The path of nanoparticles was followed in the bloodstream using a radioactive labeling that was performed at the CEA-IBITECS. The circulation time of the nanoparticles in the blood before their metabolization was extended relative to the administration of adenosine by itself. In addition, the researchers observed a greater interaction with the neurovascular elements to be treated. The neuroprotective effect was thereby dramatically enhanced. Moreover, no toxic hematological, cardiovascular or hepatic effects were found; the tests did not reveal any side effects on the sleep cycle or the level of food intake, either.
This discovery opens new therapeutic perspectives in the neurosciences. The functionalization of rapidly metabolized active molecules by squalene will help extend their time spent in the body, as well as the targeting of poorly accessible areas.
 An arrest of the blood supply in a cerebral artery, resulting in irreversible brain damage when the interruption is prolonged.
Squalenoyl adenosine nanoparticles provide neuroprotection after stroke and spinal cord injury | NATURE
CEA is a French government-funded technological research organisation in four main areas: low-carbon energies, defense and security, information technologies and health technologies. A prominent player in the European Research Area, it is involved in setting up collaborative projects with many partners around the world.