The early promise of boron neutron capture therapy as a method for the treatment of brain cancer has been mainly inhibited by the inherent toxicity associated with 10B-containing pharmacophores and the need for the ability to cross biological membranes. Although developments in the synthetic chemistry of polyhedral boranes have addressed issues of toxicity to a considerable extent, the delivery of 10B-agents to the site of action in a selective fashion is still a major challenge. Most of the published literature focussed on the use of ortho-carborane which despite the good catabolic stability and high 10B content is unable to cross biological membranes such as the BBB. More recently, there has been a surge of interest around the use of carbon nanotubes (CNTs) as drug delivery systems because of their ability to penetrate cells efficiently, bonding capacity and chemical stability. However, the applicability of CNTs is hindered by bundling. Non-covalent functionalization with surfactants is generally regarded as the method of choice for achieving their stabilization in aqueous media because the impact upon the stability of these materials is minimized when compared to surface chemical modification. On the other hand, covalent functionalisation provides the opportunity of tagging these delivery vessels with moieties that can provide selective targeting in a more reliable fashion. This work aims at the preparation of functionalised CNTs adopting both the aforementioned strategies containing varying amounts of 10B-containing pharmacophores. In all cases the CNTs are functionalised so to promote a selective uptake in the mitochondria of acncer cells. Their ability to facilitate the transport of 10B across the BBB as well as their suitability to selectively deliver the load to cancer cells is also tested.
No funding is available - only self-funded applications can be considered