The blood-brain barrier choline transporter as a brain drug delivery vector.
Choline is a ubiquitous molecule, found throughout almost every tissue in the body. Given it is a charged cation, nearly every cellular membrane has a transport mechanism to meet the intracellular and membrane need for choline. The blood-brain barrier is no exception in that a carrier-mediated transport mechanism is present to deliver choline from plasma to brain. The carrier consists of an anionic binding area that attracts positively charged quaternary ammonium groups or simple cations. Recent reports have shown this vector to be efficacious in delivering quaternary ammonium analogs of nicotine to brain. Future work is being completed to determine if other cationic or positively charged therapeutics can be effectively delivered to brain via this carrier.
Allen
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DD
Department of Pharmaceutical Sciences, School of Pharmacy, Texas Tech University Health Sciences Center, Amarillo, TX,79106-1712, USA. dallen@cortex.ama.ttuhsc.edu
Lockman
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PR
D000818:Animals; D001693:Biological Transport, Active / Q000502:physiology; D001812:Blood-Brain Barrier / Q000502:physiology*; D001921:Brain / Q000378:metabolism*; D002491:Central Nervous System Agents / Q000493:pharmacokinetics; D002794:Choline / Q000378:metabolism*; D016503:Drug Delivery Systems; D006801:Humans; D026901:Membrane Transport Proteins / Q000378:metabolism*
D002491:Central Nervous System Agents; D026901:Membrane Transport Proteins; C065637:choline transporter; D002794:Choline