The aim of this study is (i) to fabricate a nanoparticle formulation of ketoprofen (Keto) using a relatively new family of macrocycles as the carrier for drug delivery: cucurbit[6]uril (CB[6]), (ii) to evaluate its in vitro dissolution and (iii) to investigate its in vivo pharmaceutical property. The CB[6]–Keto nanoparticles were prepared by emulsion solvent evaporation method. Morphology and size of the successfully prepared nanoparticles were then confirmed using a transmission electron microscope and dynamic light scattering. It was shown that they are spherical with hydrodynamic diameter of 200–300 nm. The in vitro dissolution studies of CB[6]–Keto nanoparticles were conducted at pH 1.2 and 7.4. The results indicated that there is a significant increase in Keto concentration at pH 7.4 compared to pH 1.2. For the in vivo assessment, CB[6]–Keto nanoparticles and referential profenid were administered by oral gavages to rabbits. The results implied that CB[6]–Keto nanoparticles remarkably increased area under the curve compared to profenid.
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