A trade-off between solubility enhancement and physical stability upon simultaneous amorphization and nanonization of curcumin in comparison to amorphization alone

Amorphous ternary nanoparticle complex of curcumin-chitosan-hypromellose exhibiting built-in solubility enhancement and physical stability of curcumin

“…Second, owing to its nanoscale size, the amorphous CUR-CHI nanoplex exhibited superior supersaturation generation in vitro to microscale amorphous solid dispersion (ASD) of CUR, which represented a well-established amorphization strategy of CUR [18]. The superior supersaturation generation of the CUR-CHI nanoplex was attributed to the faster dissolution rate afforded by its nanoscale size [18].…”

“…Second, owing to its nanoscale size, the amorphous CUR-CHI nanoplex exhibited superior supersaturation generation in vitro to microscale amorphous solid dispersion (ASD) of CUR, which represented a well-established amorphization strategy of CUR [18]. The superior supersaturation generation of the CUR-CHI nanoplex was attributed to the faster dissolution rate afforded by its nanoscale size [18]. Furthermore, the CUR-CHI nanoplex also exhibited superior characteristics to the ASD of CUR and other CUR solubility enhancement strategies due to its (1) simple, fast, and cost-effective preparation involving only mixing of CUR and CHI solutions under ambient condition, and (2) high CUR utilization rate (> 90%) resulting in minimal CUR wastage [15].…”

“…Second, the CUR-CHI nanoplex exhibited poor physical stability during long-term storage in its dry-powder form, where parts of its amorphous form underwent crystallization, resulting in its diminished solubility enhancement capability [18]. Moreover, the amorphous state stability of the CUR-CHI nanoplex remained lacking even when it was stored as intimate mixtures with crystallization inhibitors [18].…”

Overview of the Manufacturing Methods of Solid Dispersion Technology for Improving the Solubility of Poorly Water-Soluble Drugs and Application to Anticancer Drugs

“…To improve the solubility and BA of poorly water-soluble drugs, several methods have been developed such as solid dispersion (SD) [23,24,25], complexation [26], lipid-based systems [27,28], micronization [29,30], nanonization [31,32,33], and co-crystals [34,35]. Among these, SD is one of the most potent and successful methods.…”

Amorphous drug-polyelectrolyte nanoparticle complex with controlled release functionality, enhanced amorphous stability, and its continuous production platform

“…Moreover, the amorphous drug nanoplex was demonstrated to exhibit superior supersaturation generation to the more conventional amorphous drug formulations (e.g. solid dispersion, surfactant-stabilized nanoparticles), albeit in limited studies using curcumin and itraconazole as the model poorly-soluble drugs [215,278].…”