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The aims of the present study were to evaluate the microstructure and study the in vitro/in vivo transdermal delivery of nanostructured lipid carriers (NLCs) loaded with alkaloid of Aconitum sinomontanum (AAS) compared with solid lipid nanoparticles (SLNs).Aqueous dispersions of NLCs were successfully prepared which had a particle size of 160.5 nm, a ZP of-24.8 mV with higher encapsulation efficiencies.