Upscaling co-amorphous formulation of naringin-quinacrine dihydrochloride translating from laboratory to pilot scale using spray drying for improved physicochemical and mechanical properties.

The current work focuses on improving the poor physicochemical and mechanical properties of naringin (NRN) and quinacrine dihydrochloride (QDH) by formulating a co-amorphous system where the properties of individual drugs complement each other. Additionally, an attempt was made to evaluate the effectiveness of spray-drying in scaling up the stable co-amorphous formulations produced by lab-scale process like rotary evaporation. Analytical processes including PXRD, DSC, SEM, and FT-IR spectroscopy confirmed the amorphization of NRN-QDH and molecular interactions between two. A significant enhancement in the NRN solubility along with 10 &19-folds improvement in dissolution rate was observed in FaSSGF & FaSSIF. The flow properties and compression behaviour of QDH were improved in the resultant co-amorphous formulation as confirmed by the micromeritics and Heckel analysis. These positive results encourage further investigation of the preclinical studies to prove the pharmacokinetic and dynamic benefits of this combination and their successful transfer to clinical applications. [Display omitted] • A stable CAMs was developed at lab-scale and scaled up using spray drying. • Optimized CAMs achieved enhanced solubility and dissolution rate of NRN. • Optimized CAMs showed superior compression behaviour in the Heckel analysis. • NRN-QDH offers complementary benefits in improving physico-mechanical properties. [ABSTRACT FROM AUTHOR]