Although used on a regular basis, local anaesthetics fail in places where inflammation is present, a problem for routine dental care. Intrinsic factors of the inflammatory process prevent anaesthetics from performing their function, at safe doses. The encapsulation of local anaesthetics in nanostructured lipid carriers (NLC) produces formulations with good physicochemical characteristics and improved anaesthetic effect. In that sense we developed an NLC formulation for articaine (ATC), a local anaesthetic with increasing use in dentistry. The developed formulation showed average particle sizes of 237.6 ± 3.3 nm, low polydispersity (PDI=0.169 ±0.015) and negative zeta potentials (-42.1 ± 0.5 mV), suitable for parenteral application. ATC was successfully encapsulated (%EE = 66.8 ± 2.3%) in such lipid nanocarriers. When tested in vivo, in a rodent carrageenan-induced inflammation model, NLC-ATC decreased by 35% the inflammatory hyperalgesia response, in relation to free articaine. These results had encouraged us to propose further clinical evaluation tests to test the formulation in dentistry.