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

Zhixing Lin, Kai Zheng, Mohammad A. Azad, Rajesh N. Davé

Research output: Contribution to journalArticlepeer-review

1 Scopus citations

Abstract

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®. Graphical Abstract: [Figure not available: see fulltext.].

Original languageEnglish (US)
Article number51
JournalAAPS PharmSciTech
Volume24
Issue number1
DOIs
StatePublished - Jan 2023

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

Keywords

  • Amorphous composite
  • Amorphous solid dispersions
  • Flowability
  • Neusilin
  • Spray drying

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