Naringin processing using GAS antisolvent technique and in vivo applications

Naringin is a flavanone glycoside with various pharmacological activities, including neuroprotective and antipsychotic-like effects. However, it has poor solubility in water and oral bioavailability. This study aims to investigate the influence of gas antisolvent operational parameters (pressure, temperature, antisolvent flow rate, and initial concentration of solute) on particle diameter using a 24 Central Composite Design. Naringin particles produced were analyzed for dissolution rate and then applied to ketamine-induced hyperlocomotion in mice. Results for run with C= 5 mg•mL 1, P = 12 MPa, T = 308 K, CO2 flow rate= 15 mL.min 1 showed amorphous particles while run with C= 10 mg.mL 1, P = 8 MPa, T = 318 K, CO2 flow rate= 15 mL.min 1 kept the crystalline structure of naringin. In vivo assays showed promising results for run with crystalline particles, probably due to the increased bioavailability, and amorphous particles had similar effects to commercial naringin because of the recrystallization when in contact with the aqueous medium.