Professor, University of Shanghai for Science and Technology, China

Speech Title: The third generation amorphous drug solid dispersion fabricated using a modified coaxial process
Abstract: The never-ending appearance of poorly water-soluble candidates as active pharmaceutical ingredients makes the dissolution improvement of poorly water soluble drugs become one of the central challenges in the field of pharmaceutics. Among the different kinds of strategies that have been broadly investigated in literature to resolve this problem, drug solid dispersion (SD) is one of the most promising ways with some commercial products. However, new methods for creating SD with super performance are always desired. The present job aimed to fabricate a third generation amorphous SD of an anti-cancer drug using a modified coaxial electrospinning process. Using a co-dissolved solution consisting of 12.5% (w/v) hydroxypropyl methylcellulose (HPMC), 2% (w/v) of tamoxifen citrate (TAM) and 2% (w/v) of PEG 2000 in CH2Cl2:ethanol (1:1, v:v) as an electrospinnable core fluid, and pure ethanol as the sheath working fluid, a modified coaxial process were conducted under a series of sheath-to-core fluid flow rate ratio. The prepared nanofiber-based third generation amorphous SDs were characterized using SEM, TEM, XRD, DSC, ATR-FTIR and the in vitro dissolution tests. The results demonstrated that the nanofibers’ diameter had a linear relationship with the sheath-to-core fluid flow rate ratio within a range of 0 to 0.4, the drug TAM was amorphously distributed all over the nanofibers, and the resultant nanofibers F4 provided an in vitro release 3.4 times faster than nanofibers F1, 17.8 times faster than the corresponding casting films, and 139 times than the raw drug particles. The synergistic action of size, structure and drug physical status of nanofiber-based 3rd SD could ensure its super performance in enhancing the rapid dissolution of poorly water-soluble drugs.
Keywords: Medicated nanofibers; Coaxial electrospinning; Solid dispersion; Anti-cancer drug; Dissolution enhancement