Drug Targeting to the Brain

By W. Pardridge. Pharmaceutical Research, 2007

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The blood-brain barrier: an engineering perspective (2013, background): “The lipid composition of the membrane of human BMECs is ∼33% phosphatidyl choline (PC), 25% phosphatidyl ethanolamine (PE), 17% sphyngomyelin (Sph), 11% phosphatidyl serine (PS), 4.8% phosphatidyl inositol (PI; Siakotos et al., 1969; Tewes and Galla, 2001).”
Nanoparticle-mediated brain drug delivery: Overcoming blood-brain barrier to treat neurodegenerative diseases. (2016, background): “However, in recent years, only a minor number of brain-directed pharmaceuticals have reached the market (3–5%) since most of them were incapable of crossing the BBB in vivo [38].”
Glutamate as a neurotransmitter in the healthy brain (2014, background): “These barriers are important both from a physiological point of view because they are essential for brain homeostasis, and from a phar- macological point of view because they prevent drugs from entering brain tissue (Deboer and Gaillard 2007; Teichberg 2007).”
Approaches to transport therapeutic drugs across the blood-brain barrier to treat brain diseases. (2010, methodology): “It has been reported that approximately 98% of the small molecules and nearly all large molecules (mw N 1 kD, kilodaltons), such as recombinant proteins or gene-based medicines do not cross the BBB (Pardridge, 1998, 2007c).”