Effect of micronization on Panax notoginseng: In vitro dissolution & in vivo bioavailability evaluations

Abstract

Background: Panax notoginseng (PN), the most widely used dietary supplement and herbal in Asian countries. The effect of micronization of PN is not fully clear. The aim of this study was to investigate the effects of the particle size and treatment temperature of Panax notoginseng powder (PNP) and the potential to improve the bioavailability.Methods: Several properties of PNP, including the surface morphology and thermal properties were extensively characterized by scanning electron microscopy (SEM), polarized light microscopy (PLM) and differential scanning calorimetry (DSC). The in vitro release and in vivo bioavailability of Panax notoginseng sapoins (PNS) were investigated by high-performance liquid chromatography (HPLC) and ultra-high-pressure liquid chromatography-MS/MS (UHPLC-MS/MS).Results: The results showed that particle size reduction significantly change the PNS in vitro dissolution and in vivo pharmacokinetic. The PNP with a wide size range (from 60 to 214 μm). Several properties of PNP were extensively characterized, these changes of physicochemical properties of PNP provide a better understanding of the in vitro and in vivo release behaviors of PNS. The in vitro studies demonstrated that the dissolution of PNS and particle size was nonlinear (dose- and size-dependent). The pharmacokinetic parameters of PNP in rats were determined by UHPLC-MS/MS. Powder 4 (90.38 ± 8.28 μm) showed significantly higher AUC0-T values in plasma (P < 0.05). In addition, we also investigated the influence of the hydrothermal treatment of PNP. The results showed that the PNS in vitro release and in vivo bioavailability were highest of PNP pre-treatment at 40°C.Conclusion: The PNP with a particle size around 90 μm and heat pre-treatment at 40°C would be beneficial.