This study investigated the cytotoxicity of asiatic acid (AA) encapsulated in different protein-carbohydrate matrices in human colon adenocarcinoma SW620, human hepatoblastoma HepG2 and diploid monkey kidney cells (Vero). Mungbean protein concentrate (MPC) and mungbean protein hydrolysate (MPH) in lactose (L) or lactose-maltodextrin (LM) mixture, were used to fabricate matrices encapsulating AA during lyophilisation. The cytotoxicity of AA was in a dose-dependent manner for HepG2 and SW620 cells, but not for Vero cells. The 50% inhibitory concentrations (IC50) of AA in HepG2 and SW620 were 120 and 130 μm respectively. The IC50 of AA encapsulated in MPH-L matrix in HepG2 was reduced from that of AA alone to 80 μm (P < 0.05). Study of the anti-cancer activity of AA, in the absence and presence of food matrices, revealed that an MPH-L matrix led AA to cause more apoptosis deaths in HepG2 cells than either a MPC-L matrix or pure AA.