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First step to the improvement of the blood brain barrier passage of atazanavir encapsulated in sustainable bioorganic vesicles

Abstract : The blood - brain barrier (BBB) prevents the majority of therapeutic drugs from reaching the brain following intravenous or oral administration. In this context, polymer nanoparticles are a promising alternative to bypass the BBB and carry drugs to brain cells. Amphiphilic cyclodextrins can form self-assemblies whose nanoparticles have a 100-nm-diameter range and are thus able to encapsulate drugs for controlled release. Our goal is to propose an optimized chemical synthesis of amphiphilic cyclodextrin, which remains a challenging task which commonly leads to only a low-milligram level of the high purity compound. Such cyclodextrin derivatives were used to prepare vesicles and to study their ability to vectorize a drug through the BBB. As a result, we introduced a convergent synthesis for a family of lipophosphoramidyl permethylated β-CDs (Lip-β-CDs) with various chain lengths. It was demonstrated that mixed vesicles comprised of phosphatidylcholine (POPC) and LipCDs were able to encapsulate atazanavir (ATV), a well-known protease inhibitor used as an antiretroviral drug against HIV. We highlighted that neo-vesicles promote the penetration of ATV in endothelial cells of the BBB, presumably due to the low fusogenicity of Lip-β-CDs.
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https://hal.archives-ouvertes.fr/hal-02980826
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Submitted on : Saturday, July 9, 2022 - 4:11:20 PM
Last modification on : Tuesday, September 27, 2022 - 4:32:48 AM

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Florian Nolay, Emmanuel Sevin, Mathieu Létévé, Abed Bil, Fabien Gosselet, et al.. First step to the improvement of the blood brain barrier passage of atazanavir encapsulated in sustainable bioorganic vesicles. International Journal of Pharmaceutics, Elsevier, 2020, 587, pp.119604. ⟨10.1016/j.ijpharm.2020.119604⟩. ⟨hal-02980826⟩

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