Preparation of astragaloside IV (AS-IV) nanoparticles via SAS process for anticancer efficacy: Optimization based on Box-Behnken Design

Abstract

Despite significant advances in drug formulation, the clinical application of most active pharmaceutical ingredients from traditional Chinese herbs remained a significant challenge due to their poor solubility. To address this crucial issue, astragaloside-IV (AS-IV) was selected as a model drug to prepare nanoparticles with a large specific surface area via a constant, steady, and well-organized supercritical antisolvent (SAS) method. Initially, the optimal range of nanoparticle nucleation was determined by a single-factor investigation under altered critical conditions. Under the optimized conditions obtained from the Box-Behnken Design model analysis (AS-IV solution flow rate (F): 0.85 mL/min, Temperature (T): 42 ℃, Pressure (P): 120 bar), the SAS process resulted in nanospheres with smooth surface and narrow particle size distribution. After the SAS process treatment, AS-IV with altered physical states presented improved solubility and enhanced in vitro antiproliferative effects compared to untreated AS-IV, illustrating the potential application of the SAS method in promoting the bioavailability of low water-soluble drugs.