Targeting Brain Drug Delivery with Macromolecules Through Receptor-Mediated Transcytosis

Brain diseases pose significant treatment challenges due to the restrictive nature of the blood–brain barrier (BBB). Recent advances in targeting macromolecules offer promising avenues for overcoming these obstacles through receptor-mediated transcytosis (RMT). We summarize the current progress in t...

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Main Authors: Yuanke Li, Ruiying Liu, Zhen Zhao
Format: Article
Language:English
Published: MDPI AG 2025-01-01
Series:Pharmaceutics
Subjects:
Online Access:https://www.mdpi.com/1999-4923/17/1/109
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author Yuanke Li
Ruiying Liu
Zhen Zhao
author_facet Yuanke Li
Ruiying Liu
Zhen Zhao
author_sort Yuanke Li
collection DOAJ
description Brain diseases pose significant treatment challenges due to the restrictive nature of the blood–brain barrier (BBB). Recent advances in targeting macromolecules offer promising avenues for overcoming these obstacles through receptor-mediated transcytosis (RMT). We summarize the current progress in targeting brain drug delivery with macromolecules for brain diseases. This exploration details the transport mechanisms across the BBB, focusing on RMT and its use of natural ligands for drug delivery. Furthermore, the review examines macromolecular ligands such as antibodies, peptides, and aptamers that leverage RMT for effective BBB traversal. Advancements in macromolecules-based delivery systems for brain diseases are summarized, emphasizing their therapeutic potential and limitations. Finally, emerging RMT strategies, including viral vectors, exosomes, and boron neutron capture therapy, are discussed for their precision in brain-targeted treatments. This comprehensive overview underscores the potential of RMT-based approaches to revolutionize brain disease therapy.
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spelling doaj-art-d2830ec13eb54ee8ad02611303e4aeb82025-01-24T13:45:59ZengMDPI AGPharmaceutics1999-49232025-01-0117110910.3390/pharmaceutics17010109Targeting Brain Drug Delivery with Macromolecules Through Receptor-Mediated TranscytosisYuanke Li0Ruiying Liu1Zhen Zhao2State Key Laboratory of Medicinal Chemical Biology, Key Laboratory of Bioactive Materials for the Ministry of Education, College of Life Sciences and Frontiers Science Center for Cell Responses, Nankai University, Tianjin 300071, ChinaNational Key Laboratory of Intelligent Tracking and Forecasting for Infectious Diseases, TEDA Institute of Biological Sciences and Biotechnology, Nankai University, Tianjin 300457, ChinaKey Laboratory of Molecular Biophysics, Institute of Biophysics, School of Health Sciences & Biomedical Engineering, Hebei University of Technology, Tianjin 300401, ChinaBrain diseases pose significant treatment challenges due to the restrictive nature of the blood–brain barrier (BBB). Recent advances in targeting macromolecules offer promising avenues for overcoming these obstacles through receptor-mediated transcytosis (RMT). We summarize the current progress in targeting brain drug delivery with macromolecules for brain diseases. This exploration details the transport mechanisms across the BBB, focusing on RMT and its use of natural ligands for drug delivery. Furthermore, the review examines macromolecular ligands such as antibodies, peptides, and aptamers that leverage RMT for effective BBB traversal. Advancements in macromolecules-based delivery systems for brain diseases are summarized, emphasizing their therapeutic potential and limitations. Finally, emerging RMT strategies, including viral vectors, exosomes, and boron neutron capture therapy, are discussed for their precision in brain-targeted treatments. This comprehensive overview underscores the potential of RMT-based approaches to revolutionize brain disease therapy.https://www.mdpi.com/1999-4923/17/1/109receptor-mediated transcytosisCNSligandsantibodypeptideaptamer
spellingShingle Yuanke Li
Ruiying Liu
Zhen Zhao
Targeting Brain Drug Delivery with Macromolecules Through Receptor-Mediated Transcytosis
Pharmaceutics
receptor-mediated transcytosis
CNS
ligands
antibody
peptide
aptamer
title Targeting Brain Drug Delivery with Macromolecules Through Receptor-Mediated Transcytosis
title_full Targeting Brain Drug Delivery with Macromolecules Through Receptor-Mediated Transcytosis
title_fullStr Targeting Brain Drug Delivery with Macromolecules Through Receptor-Mediated Transcytosis
title_full_unstemmed Targeting Brain Drug Delivery with Macromolecules Through Receptor-Mediated Transcytosis
title_short Targeting Brain Drug Delivery with Macromolecules Through Receptor-Mediated Transcytosis
title_sort targeting brain drug delivery with macromolecules through receptor mediated transcytosis
topic receptor-mediated transcytosis
CNS
ligands
antibody
peptide
aptamer
url https://www.mdpi.com/1999-4923/17/1/109
work_keys_str_mv AT yuankeli targetingbraindrugdeliverywithmacromoleculesthroughreceptormediatedtranscytosis
AT ruiyingliu targetingbraindrugdeliverywithmacromoleculesthroughreceptormediatedtranscytosis
AT zhenzhao targetingbraindrugdeliverywithmacromoleculesthroughreceptormediatedtranscytosis