The Preparation of Apigenin Nanoparticles and the Study of Their Anti-Inflammatory and Anti-Tumor Activities In Vitro

Abstract

Apigenin (API) has many biological activities, but its poor solubility limits its clinical application. In this research, API nanoparticles were prepared by the liquid antisolvent precipitation (LAP) technique, which effectively improved the solubility and bioavailability of API. Through the design of a single-factor test, the effects of the type and dosage of surfactants, API concentration, the antisolvent to solvent volume ratio, the speed and time of stirring, the temperature of precipitation, and the dropping speed on the MPS (mean particle size) of API nanosuspension were carried out. The optimum technological conditions were determined as follows: 5 mg/mL of tween 80 as a surfactant, 20 mg/mL of API, an antisolvent/solvent volume ratio of 10, a 1200 r/min stirring speed for 5 min, a 45 °C precipitation temperature, and a 1 mL/min dropping speed. Under the optimum conditions, we obtained API nanosuspension with 170.5 nm MPS and then it was freeze-dried to obtain the API nanoparticles. Moreover, we characterized the API nanoparticles by SEM, FTIR, XRD, DSC, and TG. Results showed that although API nanoparticles transformed into an amorphous form, their internal chemical structure had not been changed and had a higher solubility. Finally, API nanoparticles’ anti-inflammatory activities were evaluated by observing the effect of API on nitric oxide (NO) production and IL-10 production toward RAW264.7 cells induced by lipopolysaccharide (LPS). Moreover, the anti-tumor effect of API was determined by testing cell viability and apoptosis. The results suggested that API nanoparticles exhibited much better anti-inflammatory and anti-tumor activities compared to raw API.