Methodologies to Assess Drug Permeation Through the Blood–Brain Barrier for Pharmaceutical Research

No abstract is available for this paper.

• Publication year

  2013

• Venue

  Pharmaceutical Research

• Publication date

  2013-06-26

• Fields of study

  Biology, Medicine, Chemistry

• Identifiers
  DOI 10.1007/s11095-013-1119-zPMID 23801086
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Quantitative targeted absolute proteomic analysis of transporters, receptors and junction proteins for validation of human cerebral microvascular endothelial cell line hCMEC/D3 as a human blood-brain barrier model.

  2013cited by this paper
• Kinetic analysis of the toxicity of pharmaceutical excipients Cremophor EL and RH40 on endothelial and epithelial cells.

  2013cited by this paper
• The promiscuous binding of pharmaceutical drugs and their transporter-mediated uptake into cells: what we (need to) know and how we can do so.

  2013cited by this paper
• Advances in PET imaging of P-glycoprotein function at the blood-brain barrier.

  2013cited by this paper
• Immortalized human cerebral microvascular endothelial cells maintain the properties of primary cells in an in vitro model of immune migration across the blood brain barrier.

  2013cited by this paper
• Neurovascular Unit: a Focus on Pericytes

  2012cited by this paper
• Development of a physiologically based pharmacokinetic model for the rat central nervous system and determination of an in vitro-in vivo scaling methodology for the blood-brain barrier permeability of two transporter substrates, morphine and oxycodone.

  2012cited by this paper
• Permeation and metabolism of cocaine in the nasal mucosa

  2012cited by this paper
• Blood-Brain Barrier Permeation and Efflux Exclusion of Anticholinergics Used in the Treatment of Overactive Bladder

  2012cited by this paper
• Targeting blood-brain barrier sphingolipid signaling reduces basal P-glycoprotein activity and improves drug delivery to the brain

  2012cited by this paper
• Is there a clinical future for polymeric nanoparticles as brain-targeting drug delivery agents?

  2012cited by this paper
• Transport of drugs across the blood-brain barrier by nanoparticles.

  2012cited by this paper
• A Novel PET Protocol for Visualization of Breast Cancer Resistance Protein Function at the Blood–Brain Barrier

  2012cited by this paper
• Activation of Cannabinoid Receptor 2 Attenuates Leukocyte–Endothelial Cell Interactions and Blood–Brain Barrier Dysfunction under Inflammatory Conditions

  2012cited by this paper
• SLN approach for nose-to-brain delivery of alprazolam

  2012cited by this paper
• Tolerability, safety, pharmacokinetics, and efficacy of doxorubicin-loaded anti-EGFR immunoliposomes in advanced solid tumours: a phase 1 dose-escalation study.

  2012cited by this paper
• Steady-State Brain Glucose Concentrations During Hypoglycemia in Healthy Humans and Patients With Type 1 Diabetes

  2012cited by this paper
• Molecular MRI enables early and sensitive detection of brain metastases

  2012cited by this paper
• 1α,25‐Dihydroxyvitamin D3‐liganded vitamin D receptor increases expression and transport activity of P‐glycoprotein in isolated rat brain capillaries and human and rat brain microvessel endothelial cells

  2012cited by this paper
• How to measure drug transport across the blood-brain barrier

  2011influential reference
• Human brain endothelial cells endeavor to immunoregulate CD8 T cells via PD-1 ligand expression in multiple sclerosis

  2011cited by this paper
• Intranasal delivery of neuropeptides.

  2011cited by this paper
• In vitro primary human and animal cell-based blood-brain barrier models as a screening tool in drug discovery.

  2011cited by this paper
• In vitro models of the blood-brain barrier.

  2011influential reference
• Internal benchmarking of a human blood-brain barrier cell model for screening of nanoparticle uptake and transcytosis.

  2011cited by this paper
• Murine in vitro model of the blood-brain barrier for evaluating drug transport.

  2011cited by this paper
• The blood-brain barrier and neurotherapeutics

  2011cited by this paper
• How well can in vitro brain microcapillary endothelial cell models predict rodent in vivo blood-brain barrier permeability?

  2011cited by this paper
• Comparison of Immortalized bEnd5 and Primary Mouse Brain Microvascular Endothelial Cells as in vitro Blood–Brain Barrier Models for the Study of T Cell Extravasation

  2011cited by this paper
• Uptake and permeability studies of BBB-targeting immunoliposomes using the hCMEC/D3 cell line.

  2011cited by this paper
• Validation of in vitro cell-based human blood-brain barrier model using clinical positron emission tomography radioligands to predict in vivo human brain penetration.

  2010cited by this paper
• Comparison of in vitro cell models in predicting in vivo brain entry of drugs.

  2010cited by this paper
• Blood-brain barrier disruption and enhanced vascular permeability in the multiple sclerosis model EAE.

  2010cited by this paper
• Evaluation of various PAMPA models to identify the most discriminating method for the prediction of BBB permeability.

  2010cited by this paper
• Penetration of Drugs through the Blood-Cerebrospinal Fluid/Blood-Brain Barrier for Treatment of Central Nervous System Infections

  2010cited by this paper
• Establishment of primary cultures of human brain microvascular endothelial cells to provide an in vitro cellular model of the blood-brain barrier

  2010cited by this paper
• Improved Measurement of Drug Exposure in the Brain Using Drug-Specific Correction for Residual Blood

  2010cited by this paper
• Coexistence of passive and carrier-mediated processes in drug transport

  2010influential reference
• Structure and function of the blood-brain barrier.

  2010cited by this paper
• Establishment of a new conditionally immortalized human brain microvascular endothelial cell line retaining an in vivo blood–brain barrier function

  2010cited by this paper
• Lipophilicity in drug discovery

  2010cited by this paper
• Regulation of P-glycoprotein and other ABC drug transporters at the blood-brain barrier.

  2010cited by this paper
• Comparison of two blood-brain barrier in vitro systems: cytotoxicity and transfer assessments of malathion/oxon and lead acetate.

  2010cited by this paper
• Solubilisation of drugs within liposomal bilayers: alternatives to cholesterol as a membrane stabilising agent

  2010cited by this paper
• The transport of anti-HIV drugs across blood–CNS interfaces: Summary of current knowledge and recommendations for further research

  2009influential reference
• Evaluation of intestinal absorption of ginsenoside Rg1 incorporated in microemulison using parallel artificial membrane permeability assay.

  2009cited by this paper
• Chapter 3 - Colloidal systems for CNS drug delivery.

  2009cited by this paper
• Development of a High-Throughput Brain Slice Method for Studying Drug Distribution in the Central Nervous System

  2009cited by this paper
• Biologie de la barrière hématoencéphalique : Partie I

  2009cited by this paper
• Ionization-specific prediction of blood-brain permeability.

  2009cited by this paper
• Estimating Blood and Brain Concentrations and Blood-to-Brain Influx by Magnetic Resonance Imaging with Step-Down Infusion of Gd-DTPA in Focal Transient Cerebral Ischemia and Confirmation by Quantitative Autoradiography with Gd-[14C]DTPA

  2009cited by this paper
• Proliposomes of exemestane for improved oral delivery: formulation and in vitro evaluation using PAMPA, Caco-2 and rat intestine.

  2009cited by this paper
• Neuron-Glia Interactions as Therapeutic Targets in Neurodegeneration

  2009cited by this paper
• A new blood-brain barrier model using primary rat brain endothelial cells, pericytes and astrocytes.

  2009cited by this paper
• The blood-brain barrier in brain homeostasis and neurological diseases.

  2009cited by this paper
• Studies on distribution and metabolism of para-methoxymethamphetamine (PMMA) in rats after subcutaneous administration.

  2009cited by this paper
• ADDME – Avoiding Drug Development Mistakes Early: central nervous system drug discovery perspective

  2009cited by this paper
• [Biology of the blood-brain barrier: Part I].

  2009cited by this paper
• Corrigendum to “The transport of anti-HIV drugs across blood–CNS interfaces: Summary of current knowledge and recommendations for further research” [Antiviral Res. 82 (2) (2009) A99–A109]

  2009cited by this paper
• Comparison of blood-brain barrier permeability assays: in situ brain perfusion, MDR1-MDCKII and PAMPA-BBB.

  2009cited by this paper
• Potential use of tight junction modulators to reversibly open membranous barriers and improve drug delivery.

  2009cited by this paper
• Using the Golden Triangle to optimize clearance and oral absorption.

  2009cited by this paper
• An in vitro blood-brain barrier model for high throughput (HTS) toxicological screening.

  2008cited by this paper
• Etude comparative des thérapies anti-VIH : rôle des transporteurs d'efflux sur le passage transmembranaire des antirétroviraux au niveau des cellules CD4+ et de la barrière hémato-encéphalique

  2008cited by this paper
• Toward an optimal blood-brain barrier shuttle by synthesis and evaluation of peptide libraries.

  2008cited by this paper
• Applications of high throughput microsomal stability assay in drug discovery.

  2008cited by this paper
• The human brain endothelial cell line hCMEC/D3 as a human blood‐brain barrier model for drug transport studies

  2008cited by this paper
• Pathophysiology of the blood-brain barrier: animal models and methods.

  2008influential reference
• Brain Endothelial Cell-Cell Junctions: How to “Open” the Blood Brain Barrier

  2008cited by this paper
• Passive diffusion of polymeric surfactants across lipid bilayers.

  2007cited by this paper
• Modelling of the blood–brain barrier in drug discovery and development

  2007influential reference
• Modeling the Blood‐Brain Barrier

  2007influential reference
• A functional in vitro model of rat blood-brain barrier for molecular analysis of efflux transporters.

  2007cited by this paper
• In Silico Models to Predict Brain Uptake

  2007influential reference
• Central Nervous System Drug Disposition: The Relationship between in Situ Brain Permeability and Brain Free Fraction

  2007cited by this paper
• Evaluation of bEnd5 cell line as an in vitro model for the blood-brain barrier under normal and hypoxic/aglycemic conditions.

  2007cited by this paper
• Ion transport across transmembrane pores.

  2007cited by this paper
• Expression of drug transporters at the blood-brain barrier using an optimized isolated rat brain microvessel strategy.

  2007cited by this paper
• In Vitro Methods for Estimating Unbound Drug Concentrations in the Brain Interstitial and Intracellular Fluids

  2007cited by this paper
• Primary porcine brain microvascular endothelial cells: Biochemical and functional characterisation as a model for drug transport and targeting

  2007cited by this paper
• Predicting Penetration Across the Blood-Brain Barrier from Simple Descriptors and Fragmentation Schemes

  2007cited by this paper
• Use of Plasma and Brain Unbound Fractions to Assess the Extent of Brain Distribution of 34 Drugs: Comparison of Unbound Concentration Ratios to in Vivo P-Glycoprotein Efflux Ratios

  2007cited by this paper
• High‐Throughput Artificial Membrane Permeability Studies in Early Lead Discovery and Development

  2007influential reference
• Methods to assess drug permeability across the blood‐brain barrier

  2006influential reference
• Establishment of coculture model of blood-brain barrier in vitro for nanoparticle's transcytosis and toxicity evaluation.

  2006cited by this paper
• BRAIN DISTRIBUTION OF CETIRIZINE ENANTIOMERS: COMPARISON OF THREE DIFFERENT TISSUE-TO-PLASMA PARTITION COEFFICIENTS: Kp, Kp,u, AND Kp,uu

  2006cited by this paper
• Impaired function and expression of P-glycoprotein in blood-brain barrier of streptozotocin-induced diabetic rats.

  2006cited by this paper
• Parallel artificial membrane permeability assay: a new membrane for the fast prediction of passive human skin permeability.

  2006cited by this paper
• Astrocyte–endothelial interactions at the blood–brain barrier

  2006influential reference
• Puromycin‐purified rat brain microvascular endothelial cell cultures exhibit improved barrier properties in response to glucocorticoid induction

  2006cited by this paper
• Endocytosis at the blood–brain barrier: From basic understanding to drug delivery strategies

  2006cited by this paper
• Role of drug efflux transporters in the brain for drug disposition and treatment of brain diseases.

  2005cited by this paper
• Blood‐brain barrier‐specific properties of a human adult brain endothelial cell line

  2005cited by this paper
• Brain pericytes contribute to the induction and up-regulation of blood-brain barrier functions through transforming growth factor-beta production.

  2005cited by this paper
• Evaluation of the MDR-MDCK cell line as a permeability screen for the blood-brain barrier.

  2005cited by this paper
• Rat Brain Endothelial Cell Lines for the Study of Blood–Brain Barrier Permeability and Transport Functions

  2005cited by this paper
• Drug metabolism and pharmacokinetics, the blood-brain barrier, and central nervous system drug discovery

  2005influential reference
• Permeability Studies on In Vitro Blood–Brain Barrier Models: Physiology, Pathology, and Pharmacology

  2005cited by this paper
• Mouse syngenic in vitro blood–brain barrier model: a new tool to examine inflammatory events in cerebral endothelium

  2005cited by this paper
• P-glycoprotein deficiency at the blood-brain barrier increases amyloid-beta deposition in an Alzheimer disease mouse model.

  2005cited by this paper

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  2025cites this paper
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• Unlocking the Human Blood-brain barrier (BBB) Characteristics for the Development of Nano-Delivery Strategies for Central Nervous System Therapies

  2025cites this paper
• The duality of the BBB: breaking the myth of the blood-brain barrier breakdown

  2025cites this paper
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  2025cites this paper
• Utilizing Multifaceted Approaches to Target Drug Delivery in the Brain: From Nanoparticles to Biological Therapies

  2024influential citation
• GDNF and cAMP significantly enhance in vitro blood-brain barrier integrity in a humanized tricellular transwell model

  2024cites this paper
• In silico analysis of potential inhibitors for breast cancer targeting 17beta‐hydroxysteroid dehydrogenase type 1 (17beta‐HSD1) catalyses

  2024cites this paper
• Blood brain barrier-on-a-chip to model neurological diseases

  2023cites this paper
• Development of a new drug candidate for the inhibition of Lassa virus glycoprotein and nucleoprotein by modification of evodiamine as promising therapeutic agents

  2023cites this paper
• Establishment and Validation of a New Co-Culture for the Evaluation of the Permeability through the Blood–Brain Barrier in Patients with Glioblastoma

  2023influential citation
• An overview of in vitro 3D models of the blood-brain barrier as a tool to predict the in vivo permeability of nanomedicines.

  2023cites this paper
• Access to the CNS: Strategies to overcome the BBB.

  2023cites this paper
• In Vitro and In Silico Evaluations of Boswellia carterii Resin Dermocosmetic Activities

  2022cites this paper
• Can Natural Products Exert Neuroprotection without Crossing the Blood–Brain Barrier?

  2021cites this paper
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  2021cites this paper
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  2021cites this paper
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  2021cites this paper
• In vitro evaluation of two different type of obidoxime-loaded nanoparticles for cytotoxicity and blood-brain barrier transport.

  2020cites this paper
• Drug Development for Central Nervous System Diseases Using In vitro Blood-brain Barrier Models and Drug Repositioning

  2020cites this paper
• Acetylcholinesterase inhibitory activity, anti-inflammatory, and neuroprotective potential of Hippeastrum psittacinum (Ker Gawl.) Herb (Amaryllidaceae).

  2020cites this paper
• In vivo Glioblastoma Therapy Using Targeted Liposomal Cisplatin

  2020cites this paper
• Designing, Cytotoxic Evaluation, Molecular Docking and in Silico Pharmacokinetic Prediction of New Hydrocortisone Derivatives as Anti-Asthmatics Drugs

  2020cites this paper
• In vitro and in vivo models of BBB to evaluate brain targeting drug delivery

  2019cites this paper
• A microfluidic model of human brain (μHuB) for assessment of blood brain barrier

  2019cites this paper
• Permeability prediction for zwitterions via chromatographic indexes and classification into 'certain' and 'uncertain'.

  2019cites this paper
• Druggability profile of stilbene-derived PPAR agonists: determination of physicochemical properties and PAMPA study.

  2019cites this paper
• High Permeation Rates in Liposome Systems Explain Rapid Glyphosate Biodegradation Associated with Strong Isotope Fractionation

  2018cites this paper
• Development of new antiepileptic drug candidates: a set of lamotrigine-related compounds

  2018cites this paper
• [Consideration for future in vitro BBB models - technical development to investigate the drug delivery to the CNS].

  2018cites this paper
• Theoretical Prediction of the Complex P-Glycoprotein Substrate Efflux Based on the Novel Hierarchical Support Vector Regression Scheme

  2018cites this paper
• EGFR gene regulation in colorectal cancer cells by garlic phytocompounds with special emphasis on S-Allyl-L-Cysteine Sulfoxide

  2018cites this paper
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  2017cites this paper
• Nanopesticides: preparation, targeting, and controlled release

  2017cites this paper
• Nanoantimicrobials: Activity, Benefits, and Weaknesses

  2017cites this paper
• Selecting Good 'Drug-Like' Properties to Optimize Small Molecule Blood-Brain Barrier Penetration.

  2016cites this paper
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  2016cites this paper
• In vitro screening of nanomedicines through the blood brain barrier: A critical review.

  2016cites this paper
• Tools for studying drug transport and metabolism in the brain

  2016influential citation
• Clinical, imaging and pathological characteristics of brain implanted polylactic co-glycolic acid polymers conjugated with temozolomide.

  2015cites this paper
• Target engagement in lead generation.

  2015cites this paper
• Human Apolipoprotein E ε4 Expression Impairs Cerebral Vascularization and Blood—Brain Barrier Function in Mice

  2015cites this paper
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  2015cites this paper
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  2014cites this paper
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  2014cites this paper
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  2014cites this paper