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Biomolecules
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Drug Screening in Experimental and Clinical Studies Targeting the Blood...
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Drug Screening in Experimental and Clinical Studies Targeting the Blood Brain Barrier

A special issue of Biomolecules (ISSN 2218-273X).

Deadline for manuscript submissions: closed (15 October 2021) | Viewed by 12087

Special Issue Editor

Dr. Beatrice Mihaela Radu

E-Mail Website
Guest Editor
Department of Anatomy, Animal Physiology and Biophysics, Faculty of Biology, University of Bucharest, Bucharest, Romania
Interests: blood brain barrier; neurodegenerative disorders; neuroinflammation; electrophysiology; calcium signaling; pharmacology; drug screening

Special Issue Information

Dear Colleagues,

Blood brain barrier (BBB) is a key regulator for the access of any drug to the brain parenchyma. There are multiple transport systems in the BBB including ion channels, membrane transport of small lipophilic substances, carrier-mediated transport, receptor-mediated transport, adsorption-mediated transcytosis transport, active efflux transporters etc. Various drugs may either directly affect the transport through these systems, or indirectly regulate their gene/protein expression, thus contributing to their up/downregulation and internalization mechanisms, that finally affects the expected drug transport across the BBB. For this reason, accurate information regarding the interaction with drugs or their permeability through the BBB is necessary, making drug screening and drug safety assays mandatory for any commercial or newly synthesized drug. Moreover, the mechanisms behind BBB alterations in various pathologies must be understood to ensure the optimal drug delivery. To this purpose, experimental in silico, in vitro, and in vivo studies have brought essential information for drug development. Additionally, several strategies have been developed to increase the efficiency of drug delivery to brain parenchyma, especially in clinical situations (i.e. neuro-oncology, pharmacoresistance), where BBB transport mechanisms are altered due to the pathological condition.

For this Special Issue of Biomolecules, “’Drug screening in experimental and clinical studies targeting the blood brain barrier”, we encourage the submission of primary research and review articles that are focused on the transport and mechanism of action for commercial and newly-synthesized drugs at the BBB level, either in preclinical or clinical studies.

Dr. Beatrice Mihaela Radu
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. Biomolecules 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 2700 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

  • Blood Brain Barrier
  • In silico models
  • In vitro models
  • In vivo models
  • Clinical studies
  • Drug screening
  • Drug safety
  • Pharmacology
  • Pharmacoresistance
  • Central nervous systems disorders

Published Papers (2 papers)

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Review

31 pages, 2951 KiB  
Review
Advanced Bioinformatics Tools in the Pharmacokinetic Profiles of Natural and Synthetic Compounds with Anti-Diabetic Activity
by Ana Maria Udrea, Gratiela Gradisteanu Pircalabioru, Anca Andreea Boboc, Catalina Mares, Andra Dinache, Maria Mernea and Speranta Avram
Biomolecules 2021, 11(11), 1692; https://doi.org/10.3390/biom11111692 - 14 Nov 2021
Cited by 11 | Viewed by 4436
Abstract
Diabetes represents a major health problem, involving a severe imbalance of blood sugar levels, which can disturb the nerves, eyes, kidneys, and other organs. Diabes management involves several synthetic drugs focused on improving insulin sensitivity, increasing insulin production, and decreasing blood glucose levels, [...] Read more.
Diabetes represents a major health problem, involving a severe imbalance of blood sugar levels, which can disturb the nerves, eyes, kidneys, and other organs. Diabes management involves several synthetic drugs focused on improving insulin sensitivity, increasing insulin production, and decreasing blood glucose levels, but with unclear molecular mechanisms and severe side effects. Natural chemicals extracted from several plants such as Gymnema sylvestre, Momordica charantia or Ophiopogon planiscapus Niger have aroused great interest for their anti-diabetes activity, but also their hypolipidemic and anti-obesity activity. Here, we focused on the anti-diabetic activity of a few natural and synthetic compounds, in correlation with their pharmacokinetic/pharmacodynamic profiles, especially with their blood-brain barrier (BBB) permeability. We reviewed studies that used bioinformatics methods such as predicted BBB, molecular docking, molecular dynamics and quantitative structure-activity relationship (QSAR) to elucidate the proper action mechanisms of antidiabetic compounds. Currently, it is evident that BBB damage plays a significant role in diabetes disorders, but the molecular mechanisms are not clear. Here, we presented the efficacy of natural (gymnemic acids, quercetin, resveratrol) and synthetic (TAK-242, propofol, or APX3330) compounds in reducing diabetes symptoms and improving BBB dysfunctions. Bioinformatics tools can be helpful in the quest for chemical compounds with effective anti-diabetic activity that can enhance the druggability of molecular targets and provide a deeper understanding of diabetes mechanisms. Full article
(This article belongs to the Special Issue Drug Screening in Experimental and Clinical Studies Targeting the Blood Brain Barrier)
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23 pages, 2058 KiB  
Review
Lab-on-a-Chip Platforms as Tools for Drug Screening in Neuropathologies Associated with Blood–Brain Barrier Alterations
by Cristina Elena Staicu, Florin Jipa, Emanuel Axente, Mihai Radu, Beatrice Mihaela Radu and Felix Sima
Biomolecules 2021, 11(6), 916; https://doi.org/10.3390/biom11060916 - 21 Jun 2021
Cited by 19 | Viewed by 6911
Abstract
Lab-on-a-chip (LOC) and organ-on-a-chip (OOC) devices are highly versatile platforms that enable miniaturization and advanced controlled laboratory functions (i.e., microfluidics, advanced optical or electrical recordings, high-throughput screening). The manufacturing advancements of LOCs/OOCs for biomedical applications and their current limitations are briefly discussed. Multiple [...] Read more.
Lab-on-a-chip (LOC) and organ-on-a-chip (OOC) devices are highly versatile platforms that enable miniaturization and advanced controlled laboratory functions (i.e., microfluidics, advanced optical or electrical recordings, high-throughput screening). The manufacturing advancements of LOCs/OOCs for biomedical applications and their current limitations are briefly discussed. Multiple studies have exploited the advantages of mimicking organs or tissues on a chip. Among these, we focused our attention on the brain-on-a-chip, blood–brain barrier (BBB)-on-a-chip, and neurovascular unit (NVU)-on-a-chip applications. Mainly, we review the latest developments of brain-on-a-chip, BBB-on-a-chip, and NVU-on-a-chip devices and their use as testing platforms for high-throughput pharmacological screening. In particular, we analyze the most important contributions of these studies in the field of neurodegenerative diseases and their relevance in translational personalized medicine. Full article
(This article belongs to the Special Issue Drug Screening in Experimental and Clinical Studies Targeting the Blood Brain Barrier)
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