Purpose. Boron neutron capture therapy (BNCT) is a form of radiochemot
herapy that is becoming increasingly important for the treatment of ma
lignant gliomas, malignant melanomas and other forms of cancer. Target
ed delivery of boron to tumors is a critical prerequisite for successf
ul BNCT. Methods. Strategies that involve synthetic chemical approache
s and biochemical and biophysical approaches are employed to meet this
requirement. Compounds developed for targeting to tumors include boro
captate sodium (BSH) and p-boronophenylalanine (BPA) which are current
ly in clinical use. Results. Boronated porphyrins. nucleosides, nucleo
tides and other boronated compounds show potentials as targeting molec
ules. Conjugation of boron compounds to macromolecules such as monoclo
nal antibodies, epidermal growth factor and dextran is also employed f
or active or passive tumor targeting. Conclusions. Boron delivery via
microparticulate carriers such as liposomes, high density lipoproteins
and microcapsules is also attractive for its potential application in
BNCT.