Developing effective treatments for CNS disorders remains a formidable
challenge due to the existence of multiple physiological barriers, primarily the bloodbrain barrier (BBB), which severely restricts medication invasion into the brain and
consequently compromises therapeutic efficacy. Effective brain-targeted drug delivery,
especially to diseased cells, requires overcoming these barriers to develop promising
therapies for brain disorders. Current research focuses on diverse nanocarrier structures
and surface-engineered, site-specific novel transporters to improve effectiveness and
minimize the untoward effects of brain therapy. These methods aim to bypass the BBB
or enhance its permeability, thereby increasing the absorption of medication in the
brain. However, the effectiveness of innovative transporter systems is influenced by
physiological factors such as Efflux-mediated excretion, Brain protein coating,
Persistence, Cytotoxicity of the nanocarriers, and patient-specific factors. Thus,
understanding the composition of the brain, the BBB, and related features is crucial for
developing effective carrier systems. Additionally, alternative routes like direct nasalto-brain drug transfer proposal promise revenue to contact the brain without the BBB
barrier. This chapter discusses the characteristics of several biological barriers, as well
as the BBB and BCSFB (blood-cerebrospinal fluid barrier), in drug treatment and the
mechanisms of drug transport that cross the BBB. It additionally explores innovative
approaches for brain-targeted drug delivery, as well as dendrimers, nanogels, inorganic
nanoparticles, liposomes, polymeric nanoparticles, nanoemulsions, quantum dots,
lipidic nanoparticles, and intranasal drug delivery. Features disturbing the drugtargeting efficacy of these innovative transporter systems are also illustrated.
Keywords: Brain, Blood-brain barrier, Drug targeting, Lipid vesicle, Nanoparticle, Pharmacotherapy, Trans nasal medication administration.
