Natural products have been successfully used for treating various ailments since ancient times and currently there are several natural product based anti-cancer agents used as the main therapy to treat cancer patients or as a complimentary treatment to chemotherapy or radiation.Balanocarpol, which is a promising natural product that has been isolated from Hopea dryobalanoides, has been studied as a potential anticancer agent but its application is limited due to its high toxicity, low water solubility, and poor bioavailablity. Therefore, the aim of this study was to improve the balanocarpol characteristics and improve its anticancer activity through its encapsulation into a bilayer structure of a lipid-based nanoparticle drug delivery system where the application of nanotechnology can help in improving such limitations of balanocarpol. The compound first was extracted and isolated from H. dryobalanoides.Niosome nanoparticles composed of span 80 (SP80) and cholesterol were formulated through innovative microfluidic mixing method for the encapsulation and delivery of balanocarpol. The prepared particles were spherical, small, and uniform with an average particles size and polydispersity index ~ 175 nm and 0.088 respectively. The encapsulation of balanocarpol into the SP80 niosomes resulted in an encapsulation efficiency of ~ 40%. The niosomes formulation loaded with balanocarpol showed superior anticancer effect over the free compound when tested in vitro on human ovarian carcinoma (A2780) and human breast carcinoma (ZR-75-1). This is the first study that report the use of SP80 niosomes for successful encapsulation and delivery of balanocarpol into cancer cells.