The purpose of this research work was to formulate the stable nanosuspension of Ginkgo biloba to increase its oral bioavailability. To achieve this goal, initially nanosuspensions of G. biloba were prepared with six different stabilisers. Afterwards, other formulation conditions were optimised with response surface methodology. Stabiliser screening study selected sodium lauryl sulphate as stabiliser to formulate the nanosuspension of G. biloba by antisolvent precipitation method. Under suggested optimal conditions of software, nanosuspension of G. biloba with mean particle size 139.5 nm, polydispersity index 0.258 and zeta potential 58.7 mV was prepared. Atomic force microscopy showed sheet like shape and very well distribution of G. biloba nanoparticles with approximate height of 15-30nm. Optimised nanosuspension of G. biloba demonstrated greater in-vitro dissolution and more plasma concentration of quercetin in G. biloba nanosuspension administrated rats in comparison to coarse suspension. Moreover, cytotoxicity study revealed no toxic effects of formulated nanosuspension.