Strategies for Enhancing the Permeation of CNS-Active Drugs through the Blood-Brain Barrier: A Review

Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry
Isra' ZeiadehRafik Karaman

Abstract

Background: The blood brain barrier (BBB) is a dynamic and functional structure which poses a vast challenge in the development of drugs acting on the central nervous system (CNS). While most substances are denied BBB crossing, selective penetration of substances mainly occurs through diffusion, carrier mediated transport, or receptor mediated transcytosis. Methods: Strategies in enhancing BBB penetration have been reviewed and summarized in accordance with their type of formulation. Highlights in monoclonal antibodies, peptide-vectors, nanoparticles, and simple prodrugs were included. Conclusion: Nanoparticles and simple prodrugs, for example, can be used for efficient BBB penetration through inhibition of efflux mechanisms, however, monoclonal antibodies are the most promising strategy in BBB penetration. Close follow-up of future development in this area should confirm our expectation.

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Aug 18, 2018·Expert Opinion on Drug Metabolism & Toxicology·Qianwen Wang, Zhong Zuo
Feb 5, 2019·Expert Opinion on Drug Discovery·Anas Najjar, Rafik Karaman
Sep 15, 2019·Journal of Experimental & Clinical Cancer Research : CR·Fang WangPeng Shang
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May 10, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Rosa BuonfiglioRosella Ombrato
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Oct 4, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Inbar SchlachetAlejandro Sosnik
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May 1, 2021·International Journal of Molecular Sciences·Gabriel LutaCrina E Tiron
May 11, 2021·Journal of Molecular Neuroscience : MN·Yi-Sha GuoXia Bi

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Methods Mentioned

BETA
antisense oligonucleotides
enzyme replacement therapy

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