Are there any in vitro assays to evaluate or predict the ability of small molecules to cross blood brain barrier ?
The substance will be lipid soluble to cross blood-brain barrier.
Dear Mr Gabr,
Apart from in-silico predictions, one can use several in vivo and in vitro assay to measure permeability across BBB. I have attached one such paper describing cell based assay and other paper is review summarising other possible means.
Hope it helps !
Best Nand
Article How to Measure Drug Transport across the Blood-Brain Barrier
Article Cell- Based in Vitro Blood-Brain Barrier Model Can Rapidly E...
I am not expert in brain barrier permeability, but I know that PAMPA assay can be used to evaluate the permeability of compounds in certain membranes. For people more experienced in the field, is there any PAMPA methodology for brain barrier?
Best wishes
As pointed above perfectly, PAMPA is a really good metrics to determine BBB+/- of a given compound. However, there are plenty of variables to be considered, such as lipid composition (similar to the ones reported in the BBB), the incubation time and solubility of the compound with other co-solvent (DMSO percentage might affect to the PAMPA prediction, but only in the value obtained, not in the scale). Besides PAMPA, computational methods, despite the current efforts, are not accurated enough to anticipate BBB +/- permeability. One potential rule-of-thumb is the combination of TPSA (topological surface polar area) in conjunction with LogP metrics (AlogP, ClogP...), that at the very end results in highly endongenous prediction.
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