Background: Current cerebral drug delivery to the brain and Cerebrospinal Fluid (CSF) is
limited by the Blood-Brain Barrier (BBB) or the blood-blood Cerebrospinal Fluid (CSF) barrier. The
popular, non-invasive, intranasal delivery provides an exciting route for topical and systemic applications.
For example, intranasal drug delivery of Central Nervous System (CNS) drugs can be designed
to pass the BBB barrier via the nose-to-brain pathways. Recent nanotechnology research and patenting
focus mainly on overcoming typical limitations including bioavailability, transport, BBB penetration,
targeted delivery, controlled release rate and controlled degradation.
Objective: The aim of the present study was to assess the state-of-the-art of nose-to-brain drug delivery
systems and the role of nanotechnology in targeted delivery for the treatment of CNS and related therapeutic
Methods: Patent and related searches were made with analytics to explore and organize nanotech work
in intranasal drug delivery to the brain. Technical advancements were mapped by API, formulation and
performance criteria. Patents and published patent applications were searched with concept tables of
keywords, metadata (e.g., assignee) and patent classes (e.g., International Patent Classes and Cooperative
Results: The reviewed patents and published applications show a focus on formulations and therapeutic
indications related to the nano-based nose-to-brain drug delivery. The main patented materials were
surface modifiers, delivery systems and excipients.
Conclusion: Surface modified nanoparticles can greatly improve drug transport and bioavailability of
drugs, particularly higher molecular weight drugs. The most commonly used surface modifiers were
chitosan, lectin and cyclodextrin-cross-linker complex. Nanoformulations of herbal drugs could increase
drug bioavailability and reduce toxicity. Biotechnology-related drug delivery approaches such
as monoclonal antibodies and genetically engineered proteins (molecular Trojan horses) deliver large