Abstract

Auristatin PE (PE) as an anti-microtubule agent possesses good anticancer activity. However, the poor target effect and strong side effect limit the clinical application of PE. Boron nitride nanotubes (BNNTs) represent an outstanding carrier candidate providing a wise choice for liver-targeted drug delivery. A drug delivery system based on BNNTs and PE (BNNTs-PE) against liver cancer cells was designed and constructed in this study. Firstly, BNNTs were prepared and hydroxylated, subsequently, PE was loaded onto BNNTs by noncovalent conjugation and was stable at neutral pH but released at pH 4.49. It was found that BNNTs-PE demonstrates an enhanced anticancer activity against Hep G2 cells in comparison with free PE. BNNTs-PE kills cancer cells in a manner of mitochondria–mediated apoptosis pathway through reducing the mitochondrial membrane potential, activating caspase cascade. This BNNTs-PE system may be very promising for the treatment of liver cancer in the future.