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Nanocrystalization technologies have a great potential to substantially increase solubility as well as alleviate the erratic bioavailability behaviour of a range of poorly water soluble drugs. The aim of the current study was to fabricate smart nanocrystals of lumefantrine (LF) using wet milling technology (DENA DM-100) with the subsequent in vitro, in vivo evaluation and toxicity screening. This technology successfully produced nanocrystals with an average particle size (214.1 ± 0.2 nm) and PDI (0.201 ± 0.06) in a period of less than 1 h. DSC and PXRD were used to confirm crystallinity of the processed LF. The dissolution rate and saturation solubility of the processed LF was significantly (P < 0.05) increased compared to the raw and marketed tablets. The IC₅₀ value of LF nanocrystals was significantly (P < 0.05) lower than the IC₅₀ value of the raw drug and marketed tablets. In addition, LF nanocrystals at the same …