This study aims at developing an optimised nanostructured lipid carrier (NLC) of lycopene for efficient absorption following oral administration. The optimised formulation showed an average particle size of 121.9 +/- 3.66nm, polydispersity index (PDI) 0.370 +/- 0.97 and zeta potential -29.0 +/- 0.83mV. Encapsulation Efficiency (% EE) and drug loading (% DL) was found to be 84.50% +/- 4.38 and 9.54% +/- 2.65, respectively. In vitro release studies demonstrated the burst release within 4-9 h followed by sustained release over 48 h. The IC50 value of lycopene extract and optimised NLC for ABTS(+center dot) were found to be 172.37 mu g Trolox equivalent and 184.17 mu g Trolox equivalent whereas, for DPPH center dot, 117.76 mu g Trolox equivalent and 143.08 mu g Trolox equivalent respectively. Ex vivo studies and MTT assay revealed that the NLC had better permeation and cause sufficiently more cytotoxicity as compared to drug extract due to higher bioavailability and greater penetration.