The study aimed to develop lipid nanoparticles using excipients compatible with carvedilol (CARV) for enhanced transdermal drug delivery. Nanostructured lipid carriers (NLC) were successfully obtained and fully characterised. Franz diffusion cells were used for release and in vitro permeation studies in the porcine epidermis (EP) and full-thickness rat skin. NLC4 and NLC5 (0.5 mg/mL of CARV) presented small size (80.58 +/- 1.70 and 116.80 +/- 12.23 nm, respectively) and entrapment efficiency of 98.14 +/- 0.79 and 98.27 +/- 0.99%, respectively. CARV-loaded NLC4 and NLC5 controlled drug release. NLC4 allowed CAR permeation through porcine EP in greater amounts than NLC5, i.e. 11.83 +/- 4.71 mu g/cm(2) compared to 3.06 +/- 0.79 mu g/cm(2). NLC4 increased CARV permeation by 2.5-fold compared to the unloaded drug in rat skin studies (13.73 +/- 4.12 versus 5.31 +/- 1.56 mu g/cm(2)). NLC4 seems to be a promising carrier for the transdermal delivery of CARV.