In this article Gianpiero Calabrese, John J. Nesnas, Eugen Barbu, Dimitris Fatourosand John Tsibouklis discuss how developments in the synthetic chemistry of polyhedral boranes have addressed issues oftoxicity to a considerable extent. They also discuss the optimisation of the transport and the delivery of boronated agentsto the site of action and the development ofinnovative formulation strategies.