Case study on furosemide nanocrystals

Use of Spray Flash Evaporation (SFE) technology to improve dissolution of poorly soluble drugs:
Case study on furosemide nanocrystals

Authors: Jean-Baptiste Coty ; Cédric Martin ; Isabella Telò and Denis Spitzer 

Highlights

    • Nanocrystallization by SFE dramatically improves the dissolution of furosemide.
    • Furosemide nanocrystals conserved initial physical-chemical properties.
    • Spray Flash Evaporation is appliable to numerous APIs in the pharmaceutical area.
    • SFE is versatile for the production of various engineered nanosystems.
    • SFE allows continuous crystallization of APIs in a single step.

Abstract

The poor solubility and related low bioavailability are a major concern for a large number of small molecule drugs, both on the market and in development. Several formulation strategies exist to overcome this issue. Among them, particle engineering is of outmost importance. The aim of this work is to present the potential of Spray Flash Evaporation (SFE), a new technology for drug particle engineering. To assess the potential of SFE, we carried out a case study on the nano-crystallization of furosemide, a BCS class IV drug. A thorough characterization of the obtained nanocrystals is presented along with a study of dissolution which highlights the solubility improvement provided by nanocrystals produced via SFE technology. The obtained results show a particle size reduction when compared to the raw material, as well as an increase of the dissolution rate of 4.5-fold.