Advances in low-dimensions nanomaterials drug-carrier have rapidly translated into clinical practice. Interestingly, the two-dimensional (2D) nanomaterials of hexagonal boron nitride (h-BN), so-called “white graphite” are relatively less explored compared to the post popular 2D graphene oxide (GO). However, the unique properties of h-BN nanomaterials make them well suited for the delivery of chemotherapeutic in cancer treatment. Recent studies have shown that the h-BN is a potential candidate in biomedical sciences, both as nanocarriers and nano-transducers. In this review, we discuss the various physicochemical properties and important concepts involved in h-BN nanosheets as anticancer drug carriers.