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Having achieved a significant bioavailability of curcumin by its incorporation into SLNs (C-SLNs) during pharmacokinetic (32–155 times) and pharmacodynamic (3–4 times) studies, our intent was to proof their targeting to brain. Hence, fluorescent/confocal microscopy, biodistribution and gamma scintigraphy techniques were explored to observe the presence of C-SLNs in the brain.1 h post p.o administration of C-SLNs/free curcumin (C-S) to rats, blood was withdrawn, following which the animals were sacrificed and their harvested brains were frozen at −80 °C. The obtained plasma and brain cryosections were observed for fluorescence under fluorescent/confocal microscope.Biodistribution study was performed using 99mTc-labeled C-SLNs and C-S in Balb/c mice after p.o. and i.v. administration and % radioactivity/g organ was recorded. Subsequent to this gamma scintigraphs of the New Zealand rabbits following similar treatments were performed.Presence of yellow fluorescent particles in plasma and brain indicated effective delivery of C-SLNs across the gut wall and the BBB. BloodAUCoral value for C-SLNs was 8.135 times greater than that for C-S, confirming a prolonged circulation of former. The ratio of blood AUCi.v. C-SLN/C-S in blood is ≤1 while the ratio in brain promisingly indicates 30 times higher preferential distribution of C-SLNs into brain confirming their direct delivery.