Introduction: Sustained or controlled release of drug, genetic material and biologically active ingredient are achieved through nanoemulsion which is the novel drug delivery system. Nanoemulsion is an anisotropically clear and kinetically or thermo dynamically stable liquid solution, consisting of oil, surfactant and an aqueous phase, generally droplet diameter of 10-500 nm. Aims: The aim of the present research was formulation and evaluation of nanoemulsion for bioavailability enhancement of metaxalone drug having poor water solubility. Methods: Nanoemulsion was formulated by high shear homogenization technique using sesame oil, tween 80 and PEG 400 as a surfactant and characterized by particle size determination, polydispersity index, entrapment efficiency and zeta potential. The formulations were prepared by mixing the appropriate amount of surfactant and co-surfactant and oil. The formulation was mixed until complete dispersion occurs at 400-500 C temperature with 100 rpm. An appropriate quantity of the drug was added and the final mixture was mixed by vortexing until a transparent solution was obtained. Formulations were homogenised using a high-speed homogenizer. Results: The result confirmed that all the droplet size was less than 500 nm in size and there is no aggregation between the droplets and other parameters are suitable for enhancing the bioavailability of metaxalone drug. The optimized formulation contains droplet size 94.03nm and zeta potential -47.2 mV. In-vitro dissolution study of nanoemulsion showed 90.35 release of drug within 45 minutes. Conclusion: It was concluded that nanoemulsion of metaxalone using high shear homogenization technique gave improved drug release and could potentially improve the bioavailability of the drug.