College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, 1415 South Martin Luther King Blvd, Tallahassee, FL, USA.
Foumban District Hospital, West Regional Directorate of Health, Bafoussam, West Region, Cameroon.
AAPS PharmSciTech. 2021 Dec 3;23(1):11. doi: 10.1208/s12249-021-02144-1.
Drug delivery into the brain has for long been a huge challenge as the blood-brain barrier (BBB) offers great resistance to entry of foreign substances (with drugs inclusive) into the brain. This barrier in healthy individuals is protective to the brain, disallowing noxious substances present in the blood to get to the brain while allowing for the exchange of small molecules into the brain by diffusion. However, BBB is disrupted under certain disease conditions, such as cerebrovascular diseases including acute ischemic stroke and intracerebral hemorrhage, and neurodegenerative disorders including multiple sclerosis (MS), Alzheimer's disease (AD), Parkinson's disease (PD), and cancers. This review aims to provide a broad overview of present-day strategies for brain drug delivery, emphasizing novel delivery systems. Hopefully, this review would inspire scientists and researchers in the field of drug delivery across BBB to uncover new techniques and strategies to optimize drug delivery to the brain. Considering the anatomy, physiology, and pathophysiological functioning of the BBB in health and disease conditions, this review is focused on the controversies drawn from conclusions of recently published studies on issues such as the penetrability of nanoparticles into the brain, and whether active targeted drug delivery into the brain could be achieved with the use of nanoparticles. We also extended the review to cover novel non-nanoparticle strategies such as using viral and peptide vectors and other non-invasive techniques to enhance brain uptake of drugs.
将药物递送到大脑一直是一个巨大的挑战,因为血脑屏障(BBB)对进入大脑的外来物质(包括药物)具有很强的抵抗力。在健康个体中,这种屏障对大脑具有保护作用,不允许血液中的有害物质进入大脑,同时允许小分子通过扩散进入大脑进行交换。然而,在某些疾病情况下,如包括急性缺血性中风和脑出血在内的脑血管疾病,以及包括多发性硬化症(MS)、阿尔茨海默病(AD)、帕金森病(PD)和癌症在内的神经退行性疾病,BBB 会被破坏。本篇综述旨在提供目前用于脑内药物递送的策略的广泛概述,强调新的递送系统。希望这篇综述能够激发药物跨越 BBB 递送领域的科学家和研究人员,发掘新的技术和策略,以优化药物向大脑的递送。考虑到 BBB 在健康和疾病状态下的解剖、生理和病理生理学功能,本篇综述重点介绍了最近发表的关于纳米颗粒进入大脑的渗透性以及是否可以使用纳米颗粒实现主动靶向药物递送到大脑等问题的研究结论所引出的争议。我们还扩展了综述范围,涵盖了新型非纳米颗粒策略,如使用病毒和肽载体以及其他非侵入性技术来增强药物对大脑的摄取。