Moringa oleifera (Brassicales: Moringaceae) is a medicinal plant possessing antioxidant and hepatoprotective potential. However, the poor water solubility of its bioactive constituents limits its bioavailability followed by poor efficacy. In this study, nanosuspension of M. oleifera extract was formulated to enhance the bioavailability and improved therapeutic potential. The nanosuspension of M. oleifera was prepared by using the antisolvent precipitation method and the formulation parameters were optimized through Response Surface Methodology (RSM). The optimized nanosuspension was characterized by using Scanning Electron Microscopy (SEM) and Atomic Force Microscopy (AFM). The drug released profile and oral bioavailability of optimized formulation were determined with reference to coarse extract. The antioxidant and hepatoprotective potential of the nanosuspension was also analyzed. A formulation with the particle size of 204.8 nm, polydispersity index (PDI) of 0.348 and zeta potential of -9.11 mV was successfully formulated. AFM study revealed the particle size of 92.44 nm with uniform particle size distribution. The prepared nanosuspension of M. oleifera exhibited faster dissolution velocity and 1.19-fold enhanced bioavailability as compared to its coarse extract. Furthermore, nanosuspension of M. oleifera has superior antioxidant and hepatoprotective potential as compared to its coarse extract. These findings revealed that nano-suspension is suitable for enhancing the hepatoprotective activity of M. oleifera extract. [ABSTRACT FROM AUTHOR]