Turmeric has been reported to reduce brain volume in mice models, TB positive and intestinal inflammation in mice models. The purpose of the study was to develop and optimize the curcumin-loaded nanostructured lipid carriers (NLCs) by hot high-pressure homogenization method in order to increase its oral bioavailability. The optimized formulation displayed the following properties, a particle size of 165.9 nm, and high entrapment efficiency, strong zeta potential providing physical stability. Sustained release was observed in vitro and in vivo pharmacokinetic analysis showed strongly increased systemic exposure and extended circulation half-life with respect to free curcumin. The study findings validate the findings that NLCs offer a potential delivery vehicle to facilitate enhanced bioavailability of poorly bioavailable bioactives and that NLCs have prospects in pharmaceutical and nutraceutical fields.