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Research Articles

Vol. 3 No. 2 (2020): October-February

Ibuprofen nanocrystals: Production, lyophilization and release profile



Ibuprofen (IBU) is a poorly water-soluble non-steroidal anti-inflammatory drug with proven effectiveness for treating inflammatory, musculoskeletal, and rheumatic disorders. Nanocrystals (NCs) have been proposed as drug delivery systems to improve the solubility and bioavailability of poorly water-soluble compounds. Ibuprofen NCs (IBU-NCs) have been produced by the melt-emulsification method using a combination of Tween®80(1.0%, w/v)/Span®80(0.5%, w/v) as surfactant as these molecules are generally recognized as safe (GRAS) as non-toxic, non-irritating and are of low cost. The obtained main particle size (z-Ave) and polydispersity index (PdI) were 159.4 ± 3.265 nm and 0.24 ± 0.007, respectively. Lyophilization slightly increased the mean particle size and PdI compared to the non-freeze-dried IBU-NCs. The obtained IBU-NCs powders were of white and fine texture. The type and concentration of cryoprotector (trehalose, glucose, sucrose) influenced both the size and the in vitro release profile tested in Franz diffusion cells. Due to the smaller z-Ave, NCs:Trehalose (2:1) of 170.6 ± 3.880 nm (0.417 ± 0.050), NCs:Glucose (3:1) of 275.3 ± 8.351 nm (0.144 ± 0.021) and NCs:Sucrose (4:1) of 223.3 ± 10.35 nm (0.402 ± 0.016) were selected for the in vitro drug release tests. Within the first 6 hours, resuspended lyophilized nanocrystals released between 50-70% of the drug.


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