Abstract

Background: Polyphenols are promising drug candidates because of their multifaceted properties such as anti-cancer, anti-diabetic, anti-oxidant, etc. However, their potential has not been fully exploited because of their poor solubility and bioavailability. Objective: The objective of this study was to investigate the application of nanoprecipitation as a plausible means for enhancing the solubility and dissolution of chrysin employing Tween 80 as stabilizer. Methods: The effect of various process parameters such as drug concentration, stirring speed, base:acid ratio and flow rate on the particle size and solubility of chrysin nanocrystals were determined. The formulated nanoparticles were evaluated for in vitro dissolution studies and anti-inflammatory activity. Results: A minimum particle size of 150 nm was obtained for chrysin nanocrystals when drug concentration was 5 mg/ml, stirring speed 4500 rpm, base:acid ratio 0.1:1 and flow rate was 10 ml/min. The aqueous solubility of chrysin nanoparticles was enhanced to 1.12 μg/ml as compared to pure chrysin which was found to be 0.04 μg/ml. The results of in vitro dissolution studies showed enhanced dissolution of chrysin from nanoparticles (95%). Furthermore, the chrysin nanoparticles exhibited a higher free radical scavenging activity (70%). The % inhibition of rat paw edema observed with chrysin nanoparticles was 43% whereas it was only 28% with pure chrysin. Conclusion: These findings highlight the application of nanotechnology for solubility enhancement of chrysin, a polyphenol with colossal therapeutic potential.

Keywords: Acid base precipitation, anti-inflammatory, dissolution enhancement, flavone, nanonisation.

Graphical Abstract