Preparation of Free-Flowing Spray-Dried Amorphous Composites Using Neusilin^®

A highly porous additive, Neusilin^®, with high adsorption capability is investigated to improve bulk properties, hence processability of spray-dried amorphous solid dispersions (ASDs). Griseofulvin (GF) is applied as a model BCS class 2 drug in ASDs. Two grades of Neusilin^®, US2 (coarser) and UFL2 (finer), were used as additives to produce spray-dried amorphous composite (AC) powders, and their performance was compared with the resulting ASDs without added Neusilin^®. The resulting AC powders that included Neusilin^® had greatly enhanced flowability (flow function coefficient (FFC) > 10) comparable to larger particles (100 μm) yet had finer particle size (< 50 μm), hence retaining the advantage of fast dissolution rate of finer sizes. Dissolution results demonstrated that achieved GF supersaturation for AC powders with Neusilin^® was as high as 3 times that of crystalline GF concentration and was achieved within 30 min. In addition, 80% of drug was released within 4 min. The flowability improvement for AC powders with Neusilin^® was more significant as compared to spray-dried ASDs without Neusilin^®. Thus, the role of Neusilin^® in flowability improvement was evident, considering that spray-dried AC with Neusilin^® UFL2 has higher FFC than ASDs having a similar size. Lastly, the AC powders retained a fully amorphous state of GF after 3-month ambient storage. The overall results conveyed that the improved flowability and dissolution rate could outweigh the loss of drug loading resulted by addition of Neusilin^®.