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Molecules 2018, 23(6), 1289; https://doi.org/10.3390/molecules23061289

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

Department of Bioorganic & Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Quds University, Jerusalem P.O. Box 20002, Palestine
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Received: 3 April 2018 / Revised: 22 May 2018 / Accepted: 24 May 2018 / Published: 28 May 2018
(This article belongs to the Special Issue Targeted Prodrugs 2018)
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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. View Full-Text
Keywords: blood brain barrier; drug penetration strategies; monoclonal antibody; peptide-vector; nanoparticles; prodrugs blood brain barrier; drug penetration strategies; monoclonal antibody; peptide-vector; nanoparticles; prodrugs
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Zeiadeh, I.; Najjar, A.; Karaman, R. Strategies for Enhancing the Permeation of CNS-Active Drugs through the Blood-Brain Barrier: A Review. Molecules 2018, 23, 1289.

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