Antisense brain targeting

Penichet ML, et al. An antibody-avidin fusion protein specific for the transferrin receptor serves as a delivery vehicle for effective brain targeting initial applications in anti-HIV antisense drug delivery to the brain. J Immunol 1999 163(8) 4421—4426. 

T. Sharp, and P.J. Harrison. 1997. Critical issues in the antisense inhibition of brain gene expression in vivo experiences targetting the 5-HT1A receptor. Neurochem. Int. 31 349-362. 

Peptide nucleic acids (PNA) are novel antisense oligonucleotides (see Section 1.6.2) which contain a polypeptide backbone. Receptor-mediated transcytosis can be exploited to promote their delivery to the CNS. For example, the attachment of PNAs to the anti-transferrin (0X26) receptor antibodies has been shown to increase the brain uptake of the PNAs, without loss of the ability of the PNAs to hybridize to target mRNA. However, antisense agents will not exert pharmacologic effects in vivo following delivery to... 

Khan, A. et al.. Site-specific administration of antisense oligonucleotides using biodegradable polymer microspheres provides sustained delivery and improved subcellular biodistribution in the neostriatum of the rat brain, /. Drug Target, 8,319,2000. 

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