A historical review of brain drug delivery

WM Pardridge - Pharmaceutics, 2022 - mdpi.com
The history of brain drug delivery is reviewed beginning with the first demonstration, in 1914,
that a drug for syphilis, salvarsan, did not enter the brain, due to the presence of a blood …

CSF, blood-brain barrier, and brain drug delivery

WM Pardridge - Expert opinion on drug delivery, 2016 - Taylor & Francis
Introduction: There are 2 misconceptions about the cerebrospinal fluid (CSF), the blood-
brain barrier (BBB), and brain drug delivery, which date back to the discovery of a barrier …

Deschloroclozapine, a potent and selective chemogenetic actuator enables rapid neuronal and behavioral modulations in mice and monkeys

Y Nagai, N Miyakawa, H Takuwa, Y Hori… - Nature …, 2020 - nature.com
The chemogenetic technology designer receptors exclusively activated by designer drugs
(DREADDs) afford remotely reversible control of cellular signaling, neuronal activity and …

Preclinical comparison of the blood–brain barrier permeability of osimertinib with other EGFR TKIs

N Colclough, K Chen, P Johnström, N Strittmatter… - Clinical Cancer …, 2021 - AACR
Purpose: Osimertinib is a potent and selective EGFR tyrosine kinase inhibitor (EGFR-TKI) of
both sensitizing and T790M resistance mutations. To treat metastatic brain disease, blood …

Elimination of substances from the brain parenchyma: efflux via perivascular pathways and via the blood–brain barrier

SB Hladky, MA Barrand - Fluids and Barriers of the CNS, 2018 - Springer
This review considers efflux of substances from brain parenchyma quantified as values of
clearances (CL, stated in µL g− 1 min− 1). Total clearance of a substance is the sum of …

Unbound Brain-to-Plasma Partition Coefficient, Kp,uu,brain—a Game Changing Parameter for CNS Drug Discovery and Development

I Loryan, A Reichel, B Feng, C Bundgaard… - Pharmaceutical …, 2022 - Springer
Purpose More than 15 years have passed since the first description of the unbound brain-to-
plasma partition coefficient (Kp, uu, brain) by Prof. Margareta Hammarlund-Udenaes, which …

Intracellular drug concentrations and transporters: measurement, modeling, and implications for the liver

X Chu, K Korzekwa, R Elsby, K Fenner… - Clinical …, 2013 - Wiley Online Library
Intracellular concentrations of drugs and metabolites are often important determinants of
efficacy, toxicity, and drug interactions. Hepatic drug distribution can be affected by many …

Subcellular mass spectrometry imaging and absolute quantitative analysis across organelles

A Thomen, N Najafinobar, F Penen, E Kay… - ACS …, 2020 - ACS Publications
Mass spectrometry imaging is a field that promises to become a mainstream bioanalysis
technology by allowing the combination of single-cell imaging and subcellular quantitative …

Rapid measurement of intracellular unbound drug concentrations

A Mateus, P Matsson, P Artursson - Molecular pharmaceutics, 2013 - ACS Publications
Intracellular unbound drug concentrations determine affinity to targets in the cell interior.
However, due to difficulties in measuring them, they are often overlooked in pharmacology …

Passive lipoidal diffusion and carrier-mediated cell uptake are both important mechanisms of membrane permeation in drug disposition

D Smith, P Artursson, A Avdeef, L Di… - Molecular …, 2014 - ACS Publications
Recently, it has been proposed that drug permeation is essentially carrier-mediated only
and that passive lipoidal diffusion is negligible. This opposes the prevailing hypothesis of …