Choline has many physiological functions throughout the body that are dependent on its available local supply. However, since choline is a charged hydrophilic cation, transport mechanisms are required for it to cross biological membranes. Choline transport is required for cellular membrane construction and is the rate-limiting step for acetylcholine production. Transport mechanisms include: (1) sodium-dependent high-affinity uptake mechanism in synaptosomes, (2) sodium-independent low-affinity mechanism on cellular membranes, and (3) unique choline uptake mechanisms (e.g., blood-brain barrier choline transport). A comprehensive overview of choline transport studies is provided. This review article examines landmark and current choline transport studies, molecular mapping, and molecular identification of these carriers. Information regarding the choline-binding site is presented by reviewing choline structural analog (hemicholinium-3 and 15, and other nitrogen/methyl-hydroxyl compounds) inhibition studies. Choline transport in Alzheimer's disease, brain ischemic events, and aging is also discussed. Emphasis throughout the article is placed on targeting the choline transporter in disease and use of this carrier as a drug delivery vector.