Abstract
The brain is a very delicate environment where its homeostasis is tightly regulated by the complex central nervous system components. The presence of the blood–brain barrier (BBB) represents a significant hurdle to the effective therapeutic delivery of pharmaceutical agents into the central nervous system for the treatment of neurological conditions, cerebral diseases, as well as brain tumors. To overcome this BBB hurdle, two main strategies have been used: first to traverse the BBB directly, and second, to bypass the BBB altogether. Agents can be allowed to traverse the BBB by directly affecting BBB function either due to its temporary disruption by physical means such as focused ultrasound, or by specifically targeting one or more of its biological components such as cell-surface receptors as well as drug efflux proteins. This chapter provides significant insight into the use of these strategies by comprehensively reviewing current research methodologies in preclinical and clinical settings.
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