AbstractThis study was aimed at preparing a stable nanostructure lipid carriers for Brucea javanica oil (BJO/NLCs) using the high-pressure homogenization (HPH) method. The obtained BJO/NLCs exhibited a particle size of approximately 180 nm and were quite stable during 30 days of storage. The entrapment efficiency (EE) and drug loading (DL) of BJO/NLCs were good, with values of up to 99.2% and 10.4%, respectively. The polydispersity index (PDI) and zeta potential values of BJO/NLCs were 0.17 and −31.2 mV, respectively. BJO/NLCs exhibited spherical or elongated particles when viewed by transmission electron microscopy (TEM). Small-angle X-ray scattering (SAXS) further confirmed that the internal structures of blank NLCs and BJO/NLCs were arranged into lamellar phases. Anti-tumor activity was studied using the MTT assay; the BJO/NLCs showed improved cytotoxicity to A549 cells. Taken together, these results indicate that this newly designed BJO/NLCs delivery system has the potential to exhibit improved BJO bioavailability.