This special issue of the Journal of Drug Targeting contains eight original articles describing different approaches of drug targeting to the brain. Since brain uptake of drugs is limited by transport through the brain capillary endothelial wall, which forms the blood-brain barrier (BBB) in vivo, all of the reports in this issue address targeted drug delivery through the BBB. Four chapters from the United States and Europe address drug targeting of large molecule pharmaceuticals, and four chapters from Japan address drug targeting of small molecule pharmaceuticals.