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Effect of surfactant level on properties of celecoxib amorphous solid dispersions

Year: 2019

Journal: J. Drug Deliv. Sci. Technol., Volume 49, FEB, page 301–307

Authors: Meng, Fan; Ferreira, Rui; Zhang, Feng

Organizations: Hovione LLC

The aim of this study was to explore the influence of D-alpha-tocopheryl polyethylene glycol 1000 succinate (vitamin E TPGS) on the properties of celecoxib (CEL) amorphous solid dispersions (ASDs). ASDs consisting of CEL (20%), copovidone (CoPVP), and TPGS at various levels (0, 5, 10, and 20%) were prepared using spray drying. At 20% level, TPGS increased the dissolution rate and supersaturation of CEL ASDs. These improvements were attributed to three mechanisms: (1) improved powder wetting, (2) enhanced nanoaggregate formation, and (3) improved solubility due to the formation of TPGS micelles. TPGS was also found to affect the particle morphology of spray-dried CEL ASDs. As the TPGS level increased, the shape of the spray-dried particles transitioned from shriveled to spherical. In this ternary system, CEL was found to improve the miscibility between TPGS and CoPVP.