Special Issue "Targeted Drug Delivery to the Brain"

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Delivery and Controlled Release".

Deadline for manuscript submissions: closed (30 April 2021).

Special Issue Editors

Prof. Toyofumi Suzuki
E-Mail Website1 Website2
Guest Editor
School of Pharmacy, Nihon University, 7-7-1 Narashinodai, Funabashi, Chiba 274-8555, Japan
Interests: brain drug targeting; blood-brain barrier transport; nose-to-brain drug delivery
Dr. Takanori Kanazawa
E-Mail Website1 Website2
Guest Editor
University of Shizuoka, School of Pharmaceutical Sciences, Laboratory of Pharmaceutical Engineering
Interests: drug delivery system; ASO/siRNA delivery; nose-to-brain delivery; topical application; polymer-based micelles; liposomes; functional peptides; spinal cord diseases; CNS disorders
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Special Issue Information

Dear Colleagues,

We would like to invite you to contribute to this Special Issue entitled “Targeted Drug Delivery to the Brain”.

The number of neurodegenerative diseases such as Alzheimer’s disease and vascular dementia is increasing rapidly, and the development of superior therapeutic agents is expected. Drug transfer to the brain is mainly controlled by the substance transfer function of the blood–brain barrier (BBB). To overcome the BBB, compounds can be structurally modified, providing them with physicochemical properties that promote their passive diffusion, taking advantage of the uptake and transport systems operating through endogenous transporters and receptors expressed on the BBB, or designing structures that are not recognized by the efflux transport system. With advances in research technology, the anatomical entities of the BBB and the expression of transport-related proteins have been elucidated, but the full picture of the BBB transport function of drugs is not clear yet. Therefore, the development of brain delivery systems using endogenous BBB permeation systems will become more important as more diverse central nervous system drugs are made available. On the other hand, it is possible to use potential routes that bypass or avoid the BBB. In recent years, the existence of a nasal-to-brain route has attracted attention for direct drug delivery to the brain and the central nervous system. This nose-to-brain delivery route is also expected to be non-invasive and effective for peptides and nucleic acid drugs that are difficult to directly administer in the central nervous system by conventional methods such as the oral and intravenous routes. Currently, many researchers are focusing on nose-to-brain delivery technologies and transport mechanisms for a variety of compounds, from small molecules to biopharmaceuticals. In order to efficiently deliver drugs from the nose to the central nervous system, it is essential to design a drug delivery system based on drug nanocarriers that is retained in the intranasal cavity and promotes drug permeability in the nasal mucosa. Considering this scenario, this Special Issue invites articles dealing with the following topics:

  • Blood–brain barrier transport
  • Transport mechanisms at the blood–brain barrier
  • Drug delivery systems to the brain.
  • Intranasal delivery to the brain
  • Transport mechanisms from nose to brain

Prof. Toyofumi Suzuki
Dr. Takanori Kanazawa
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All papers will be peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceutics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2200 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.


  • targeted drug delivery
  • CNS drug delivery
  • enhancing delivery
  • nanocarriers
  • nanoparticles
  • nanopharmaceuticals
  • nanomedicine: pharmaceutical nanotechnology
  • blood–brain barrier
  • transporter
  • transport mechanism
  • intranasal delivery
  • intranasal delivery device
  • nasal route
  • nose-to-brain delivery: route of delivery
  • mucoadhesion
  • mucos-penetrating particles
  • brain disease
  • neurological disorders
  • brain injury
  • central nervous disorder
  • neurodegenerative diseases

Published Papers (1 paper)

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In Vitro Evaluation of Nasal Aerosol Depositions: An Insight for Direct Nose to Brain Drug Delivery
Pharmaceutics 2021, 13(7), 1079; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13071079 - 14 Jul 2021
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The nasal cavity is an attractive route for both local and systemic drug delivery and holds great potential for access to the brain via the olfactory region, an area where the blood–brain barrier (BBB) is effectively absent. However, the olfactory region is located [...] Read more.
The nasal cavity is an attractive route for both local and systemic drug delivery and holds great potential for access to the brain via the olfactory region, an area where the blood–brain barrier (BBB) is effectively absent. However, the olfactory region is located at the roof of the nasal cavity and only represents ~5–7% of the epithelial surface area, presenting significant challenges for the deposition of drug molecules for nose to brain drug delivery (NTBDD). Aerosolized particles have the potential to be directed to the olfactory region, but their specific deposition within this area is confounded by a complex combination of factors, which include the properties of the formulation, the delivery device and how it is used, and differences in inter-patient physiology. In this review, an in-depth examination of these different factors is provided in relation to both in vitro and in vivo studies and how advances in the fabrication of nasal cast models and analysis of aerosol deposition can be utilized to predict in vivo outcomes more accurately. The challenges faced in assessing the nasal deposition of aerosolized particles within the paediatric population are specifically considered, representing an unmet need for nasal and NTBDD to treat CNS disorders. Full article
(This article belongs to the Special Issue Targeted Drug Delivery to the Brain)
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