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Pharmaceutics
Special Issues
Brain-Targeted Drug Delivery Volume II
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Brain-Targeted Drug Delivery Volume II

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 (1 April 2023) | Viewed by 7849

Special Issue Editor

Dr. Flávia Sousa

E-Mail Website
Guest Editor
Adolphe Merkle Institute, University of Fribourg, CH-1700 Fribourg, Switzerland
Interests: drug delivery; nanotechnology; biomaterials
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

At present, brain diseases affect one in six people worldwide, and include a wide range of neurological diseases from Alzheimer’s and Parkinson’s disease to epilepsy, brain injuries, brain cancer, neuroinfections and strokes. The treatment of these diseases is complex and limited due to the presence of the blood–brain barrier (BBB), which covers the entirety of the brain. The BBB not only has the function of protecting the brain from harmful substances, but is also a metabolic barrier and a transport regulator of nutrients/serum factors/neurotoxins. Knowing these characteristics when it comes to the treatment of brain diseases makes it easy to understand the lack of efficacy of therapeutic drugs, resulting from the innate resistance of the BBB to permeation. To overcome this limitation, drug delivery systems based on nanotechnology/microtechnology have been wisely developed. Brain-targeted drug delivery allows for targeted therapy with a higher therapeutic efficacy and few side effects, because it targets moieties present in the drug delivery systems.

Due to the success of our first Special Issue, “Brain-Targeted Drug Delivery”, we decided to create a Volume II of the same Special Issue. Our goal is to highlight papers describing current advances in brain-targeted drug delivery systems for the treatment of brain-related diseases such as neurodegenerative diseases, brain cancer and brain injuries. We hope these novel approaches greatly contribute to the improvement of the lives of patients with brain pathologies.

Dr. Flávia Sousa
Guest Editor

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 submissions that pass pre-check are 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 2900 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.

Keywords

  • drug delivery systems
  • brain diseases
  • brain cancer
  • brain injuries
  • targeted therapy
  • neurodegenerative diseases
  • nanoparticles
  • microparticles
  • brain therapy
  • nanomedicine
  • blood–brain barrier

Published Papers (4 papers)

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Research

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16 pages, 5652 KiB  
Article
The Improved Brain-Targeted Drug Delivery of Edaravone Temperature-Sensitive Gels by Ultrasound for γ-ray Radiation-Induced Brain Injury
by Qian Li, Yizhi Zhang, Jinglu Hu, Bochuan Yuan, Pengcheng Zhang, Yaxin Wang, Xu Jin, Lina Du and Yiguang Jin
Pharmaceutics 2022, 14(11), 2281; https://doi.org/10.3390/pharmaceutics14112281 - 25 Oct 2022
Cited by 4 | Viewed by 1178
Abstract
Radiation-induced brain injury (RBI) is a common neurological disease caused by ionizing radiation (IR). Edaravone (EDA) is a free radical scavenger, has the potential to treat RBI. EDA loaded temperature-sensitive gels (TSGs) were prepared for subcutaneous injection to improve inconvenient administration of intravenous [...] Read more.
Radiation-induced brain injury (RBI) is a common neurological disease caused by ionizing radiation (IR). Edaravone (EDA) is a free radical scavenger, has the potential to treat RBI. EDA loaded temperature-sensitive gels (TSGs) were prepared for subcutaneous injection to improve inconvenient administration of intravenous infusion. RBI mice model was established by irradiation of 60Co γ-ray on head. EDA TSGs could improve spontaneous behavior, learning and memory and anxiety of RBI mice by behavior tests, including the open field test, the novel object recognition test, the elevated plus maze test and the fear conditioning test. The therapeutic effects were enhanced with the assistance of ultrasound. Alleviative pathological changes, decreased the expression of Molondialdehyde (MDA) and Interleukin-6 (IL-6) in the hippocampus of brain, indicated reduced oxidative stress and inflammatory response with the treatment of EDA TSGs and ultrasound. Moreover, ultrasound was superior to the use of EDA TSGs. Safe and effective EDA TSGs were prepared for RBI, and the feasibility of brain-targeted drug delivery enhanced by ultrasound was preliminarily demonstrated in this study. Full article
(This article belongs to the Special Issue Brain-Targeted Drug Delivery Volume II)
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16 pages, 5622 KiB  
Article
Injectable pH Thermo-Responsive Hydrogel Scaffold for Tumoricidal Neural Stem Cell Therapy for Glioblastoma Multiforme
by Jasmine L. King, Panita Maturavongsadit, Shawn D. Hingtgen and S. Rahima Benhabbour
Pharmaceutics 2022, 14(10), 2243; https://doi.org/10.3390/pharmaceutics14102243 - 20 Oct 2022
Cited by 8 | Viewed by 1899
Abstract
Glioblastoma multiforme (GBM) is the most common malignant brain tumor in adults and despite recent advances in treatment modalities, GBM remains incurable. Injectable hydrogel scaffolds are a versatile delivery system that can improve delivery of drug and cell therapeutics for GBM. In this [...] Read more.
Glioblastoma multiforme (GBM) is the most common malignant brain tumor in adults and despite recent advances in treatment modalities, GBM remains incurable. Injectable hydrogel scaffolds are a versatile delivery system that can improve delivery of drug and cell therapeutics for GBM. In this report, we investigated an injectable nanocellulose/chitosan-based hydrogel scaffold for neural stem cell encapsulation and delivery. Hydrogels were prepared using thermogelling beta-glycerophosphate (BGP) and hydroxyethyl cellulose (HEC), chitosan (CS), and cellulose nanocrystals (CNCs). We evaluated the impact of neural stem cells on hydrogel gelation kinetics, microstructures, and degradation. Furthermore, we investigated the biomaterial effects on cell viability and functionality. We demonstrated that the incorporation of cells at densities of 1, 5 and 10 million does not significantly impact rheological and physical properties CS scaffolds. However, addition of CNCs significantly prolonged hydrogel degradation when cells were seeded at 5 and 10 million per 1 mL hydrogel. In vitro cell studies demonstrated high cell viability, release of TRAIL at therapeutic concentrations, and effective tumor cell killing within 72 h. The ability of these hydrogel scaffolds to support stem cell encapsulation and viability and maintain stem cell functionality makes them an attractive cell delivery system for local treatment of post-surgical cancers. Full article
(This article belongs to the Special Issue Brain-Targeted Drug Delivery Volume II)
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16 pages, 3424 KiB  
Article
D-DOPA Is a Potent, Orally Bioavailable, Allosteric Inhibitor of Glutamate Carboxypeptidase II
by Sadakatali S. Gori, Ajit G. Thomas, Arindom Pal, Robyn Wiseman, Dana V. Ferraris, Run-duo Gao, Ying Wu, Jesse Alt, Takashi Tsukamoto, Barbara S. Slusher and Rana Rais
Pharmaceutics 2022, 14(10), 2018; https://doi.org/10.3390/pharmaceutics14102018 - 23 Sep 2022
Cited by 2 | Viewed by 1893
Abstract
Glutamate carboxypeptidase-II (GCPII) is a zinc-dependent metalloenzyme implicated in numerous neurological disorders. The pharmacophoric requirements of active-site GCPII inhibitors makes them highly charged, manifesting poor pharmacokinetic (PK) properties. Herein, we describe the discovery and characterization of catechol-based inhibitors including L-DOPA, D-DOPA, and caffeic [...] Read more.
Glutamate carboxypeptidase-II (GCPII) is a zinc-dependent metalloenzyme implicated in numerous neurological disorders. The pharmacophoric requirements of active-site GCPII inhibitors makes them highly charged, manifesting poor pharmacokinetic (PK) properties. Herein, we describe the discovery and characterization of catechol-based inhibitors including L-DOPA, D-DOPA, and caffeic acid, with sub-micromolar potencies. Of these, D-DOPA emerged as the most promising compound, with good metabolic stability, and excellent PK properties. Orally administered D-DOPA yielded high plasma exposures (AUCplasma = 72.7 nmol·h/mL) and an absolute oral bioavailability of 47.7%. Unfortunately, D-DOPA brain exposures were low with AUCbrain = 2.42 nmol/g and AUCbrain/plasma ratio of 0.03. Given reports of isomeric inversion of D-DOPA to L-DOPA via D-amino acid oxidase (DAAO), we evaluated D-DOPA PK in combination with the DAAO inhibitor sodium benzoate and observed a >200% enhancement in both plasma and brain exposures (AUCplasma = 185 nmol·h/mL; AUCbrain = 5.48 nmol·h/g). Further, we demonstrated GCPII target engagement; orally administered D-DOPA with or without sodium benzoate caused significant inhibition of GCPII activity. Lastly, mode of inhibition studies revealed D-DOPA to be a noncompetitive, allosteric inhibitor of GCPII. To our knowledge, this is the first report of D-DOPA as a distinct scaffold for GCPII inhibition, laying the groundwork for future optimization to obtain clinically viable candidates. Full article
(This article belongs to the Special Issue Brain-Targeted Drug Delivery Volume II)
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Review

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32 pages, 2853 KiB  
Review
Harnessing Ultrasound for Targeting Drug Delivery to the Brain and Breaching the Blood–Brain Tumour Barrier
by Anita Barzegar-Fallah, Kushan Gandhi, Shakila B. Rizwan, Tania L. Slatter and John N. J. Reynolds
Pharmaceutics 2022, 14(10), 2231; https://doi.org/10.3390/pharmaceutics14102231 - 19 Oct 2022
Cited by 9 | Viewed by 2532
Abstract
Despite significant advances in developing drugs to treat brain tumours, achieving therapeutic concentrations of the drug at the tumour site remains a major challenge due to the presence of the blood–brain barrier (BBB). Several strategies have evolved to enhance brain delivery of chemotherapeutic [...] Read more.
Despite significant advances in developing drugs to treat brain tumours, achieving therapeutic concentrations of the drug at the tumour site remains a major challenge due to the presence of the blood–brain barrier (BBB). Several strategies have evolved to enhance brain delivery of chemotherapeutic agents to treat tumours; however, most approaches have several limitations which hinder their clinical utility. Promising studies indicate that ultrasound can penetrate the skull to target specific brain regions and transiently open the BBB, safely and reversibly, with a high degree of spatial and temporal specificity. In this review, we initially describe the basics of therapeutic ultrasound, then detail ultrasound-based drug delivery strategies to the brain and the mechanisms by which ultrasound can improve brain tumour therapy. We review pre-clinical and clinical findings from ultrasound-mediated BBB opening and drug delivery studies and outline current therapeutic ultrasound devices and technologies designed for this purpose. Full article
(This article belongs to the Special Issue Brain-Targeted Drug Delivery Volume II)
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