A Practical Approach to Computational Models of the Blood–Brain Barrier

2007 ◽  
pp. 109-150
Author(s):  
M. Adenot
Keyword(s):  
Blood Brain Barrier ◽  
Computational Models ◽  
Practical Approach ◽  
Brain Barrier ◽  
Blood Brain

scholarly journals RP-18 HPLC Analysis of Drugs’ Ability to Cross the Blood-Brain Barrier

2019 ◽  
Vol 2019 ◽  
pp. 1-12 ◽  
Author(s):  
Anna W. Sobańska ◽  
Adam Hekner ◽  
Elżbieta Brzezińska
Keyword(s):  
Blood Brain Barrier ◽  
Computational Models ◽  
Pharmaceutical Preparations ◽  
Brain Barrier ◽  
Analytical Models ◽  
Blood Brain ◽  
Bbb Permeability ◽  
Physicochemical Data ◽  
Chromatographic Parameters ◽  
Hplc Data

One hundred ten compounds of diverse structures (actives and excipients used in pharmaceutical preparations) were studied by RP-18 HPLC with acetonitrile-pH 7.4 phosphate buffer 1 : 1 (v/v) as the mobile phase. The relationships between the BBB permeation coefficients and the chromatographic parameters log k and (log k)/PSA were compared to those between the blood-brain barrier (BBB) permeation parameters and the RP-18 TLC descriptors Rf and Rf/PSA known from our earlier studies. It was found that the correlations between the BBB permeability and the HPLC data are slightly worse than those achieved for the thin-layer chromatographic data. MLR analysis based upon the physicochemical data confirmed the value of the molecular descriptors, related to the CNS bioavailability. These variables, combined with the HPLC data, made it possible to generate computational models, explaining 70–96% of the total variance of the CNS bioavailability. Contrary to TLC Rf, the advantage of the modification of HPLC log k with PSA (polar surface area) has not been confirmed and the results obtained with log k are superior to those obtained after a novel (log k)/PSA parameter has been introduced. Establishing a firm threshold limit of (log k)/PSA, log k, or even k and k/PSA to distinguish between the CNS+ and CNS− compounds was impossible. On the other hand, discriminant function analyses involving log k and (log k)/PSA as discriminating variables separated the CNS+ and CNS− compounds with the success rate ca. 90%. On the basis of these results, it was concluded that the RP-18 HPLC analytical models are entirely successful in studies and predictions of the BBB permeability.

Comparative in vivo and pathological analysis of the blood-brain barrier in mouse telencephalic transplants

1996 ◽  
Vol 22 (2) ◽  
pp. 118-128 ◽  
Author(s):  
S. Isenmann ◽  
S. Brandner ◽  
G. Kuhne ◽  
J. Boner ◽  
A. Aguzzi
Keyword(s):  
Blood Brain Barrier ◽  
Brain Barrier ◽  
Pathological Analysis ◽  
Blood Brain

Conformationally Constrained Peptide Drugs Targeted at the Blood-Brain Barrier

1995 ◽  
Author(s):  
Thomas P. Davis ◽  
Thomas J. Abbruscato ◽  
Elizabeth Brownson ◽  
Victor J. Hruby
Keyword(s):  
Blood Brain Barrier ◽  
Brain Barrier ◽  
Peptide Drugs ◽  
Conformationally Constrained ◽  
Blood Brain

In a rat model of transient ischemia, acute albumin leakage across the blood-brain barrier is often followed by rapid cellular uptake

2005 ◽  
Vol 25 (1_suppl) ◽  
pp. S277-S277
Author(s):  
Tavarekere N Nagaraja ◽  
Kelly A Keenan ◽  
Joseph D Fenstermacher ◽  
Robert A Knight
Keyword(s):  
Blood Brain Barrier ◽  
Cellular Uptake ◽  
Rat Model ◽  
Brain Barrier ◽  
Transient Ischemia ◽  
Blood Brain ◽  
Albumin Leakage
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