Promising dissolution enhancement effect of soluplus on crystallized celecoxib obtained through antisolvent precipitation and high pressure homogenization techniques

• Published in: Colloids and surfaces, B, Biointerfaces B, Biointerfaces, 2014-10, Vol.122, p.591-600
• Main Authors: Homayouni, Alireza, Sadeghi, Fatemeh, Varshosaz, Jaleh, Afrasiabi Garekani, Hadi, Nokhodchi, Ali
• Format: Article
• Language: English
• Subjects: Antisolvent crystallization; Calorimetry, Differential Scanning; Celecoxib; Celecoxib nanoparticles; Crystallization; Dissolution; Drugs; Freeze drying; High pressure homogenization; Homogenization; Homogenizing; Nanoparticles; Particle Size; Polyethylene Glycols - chemistry; Polyvinyls - chemistry; Powder Diffraction; Pressure; Pyrazoles - chemistry; Solid state analysis; Solubility; Solvents - chemistry; Spectroscopy, Fourier Transform Infrared; Sulfonamides - chemistry
• ISSN: 0927-7765; 1873-4367
• DOI: 10.1016/j.colsurfb.2014.07.037

•High pressure homogenization (HPH) was able to produce celecoxib nanocrystals.•HPH changed morphology and increased crystallinity of celecoxib particles.•Crystalline celecoxib showed better dissolution than amorphous celecoxib.•Freeze dried samples contained 5% solulpus showed excellent dissolution rate. Poor solubility and dissolution of hydrophobic drugs have become a major challenge in pharmaceutical development. Drug nanoparticles have been widely accepted to overcome this problem. The aim of this study was to manufacture celecoxib nanoparticles using antisolvent precipitation and high pressure homogenization techniques in the presence of varying concentrations of soluplus® as a hydrophilic stabilizer. Antisolvent crystallization followed by freeze drying (CRS-FD) and antisolvent crystallization followed by high pressure homogenization and freeze drying (HPH-FD) were used to obtain celecoxib nanoparticles. The obtained nanoparticles were analyzed in terms of particle size, saturation solubility, morphology (optical and scanning electron microscopy), solid state (DSC, XRPD and FT-IR) and dissolution behavior. The results showed that celecoxib nanoparticle can be obtained when soluplus was added to the crystallization medium. In addition, the results showed that the concentration of soluplus and the method used to prepare nanoparticles can control the size and dissolution of celecoxib. Samples obtained in the presence of 5% soluplus through HPH technique showed an excellent dissolution (90%) within 4min. It is interesting to note that celecoxib samples with high crystallinity showed better dissolution than those celecoxib samples with high amorphous content, although they had the same concentration of soluplus. DSC and XRPD proved that samples obtained via HPH technique are more crystalline than the samples obtained through only antisolvent crystallization technique.