Tauopathies are neurodegenerative disorders characterized by the deposition of abnormal tau protein in
the brain. The application of potentially effective therapeutics for their successful treatment is hampered by the
presence of a naturally occurring brain protection layer called the blood-brain barrier (BBB). BBB represents one
of the biggest challenges in the development of therapeutics for central nervous system (CNS) disorders, where
sufficient BBB penetration is inevitable. BBB is a heavily restricting barrier regulating the movement of molecules,
ions, and cells between the blood and the CNS to secure proper neuronal function and protect the CNS
from dangerous substances and processes. Yet, these natural functions possessed by BBB represent a great hurdle
for brain drug delivery. This review is concentrated on summarizing the available methods and approaches for
effective therapeutics’ delivery through the BBB to treat neurodegenerative disorders with a focus on tauopathies.
It describes the traditional approaches but also new nanotechnology strategies emerging with advanced medical
techniques. Their limitations and benefits are discussed.