An investigation into Sunitinib malate nanoparticle production by US- RESOLV method: Effect of type of polymer on dissolution rate and particle size distribution

The present study practiced ultrasonic-assisted rapid expansion of a supercritical CO2 solution into a liquid solvent (US-RESOLV) process for the synthesis of nanoparticles (NPs) of Sunitinib malate for the first time. Hydrophilic polymers including hydroxypropyl methylcellulose (HPMC), poly (vinyl alcohol) (PVA), chitosan (CHI) and polyethylene glycol (PEG) were utilized for modifying the size distribution and increasing the dissolution rate of the Sunitinib malate NPs. Also, we determined the impact of pressure, nozzle diameter as well as temperature on morphology, size distribution and dissolution rate of produced particles. In order to accomplish the objectives of the present study, PEG was the best polymer for controlling the particle size distribution and HPMC served as the best polymeric stabilizer for increasing the dissolution rate of the drug particles. The synthesized particles were much smaller (< 600 nm) in comparison to the unprocessed particles of Sunitinib malate. The combined effects of the smaller sizes of the particles, ultrasonication and the presence of polymers could enhance dissolution rate of the Sunitinib malate in the aqueous media.

Automated summary

In this study, ultrasonic-assisted rapid expansion of supercritical CO2 solution into a liquid solvent (US-RESOLV) process was utilized for the synthesis of Sunitinib malate nanoparticles (NPs) for the first time. Various hydrophilic polymers were used to modify the size distribution and enhance the dissolution rate of the NPs, with PEG identified as the best polymer for controlling particle size distribution and HPMC as the best polymeric stabilizer for increasing drug particle dissolution rate. The synthesized particles were significantly smaller (< 600 nm) compared to unprocessed particles, and the combination of smaller sizes, ultrasonication, and polymer presence led to an enhanced dissolution rate of Sunitinib malate in aqueous media.