Enhanced solubility and in vitro drug release of diosmetin from soy lecithin based‐diosmetin phytosome

The Diosmetin Phytosome (Dt‐Ph) was developed to enhance the complex's aqueous solubility and in vitro drug release compared to pure Diosmetin (Dt). The process variables such as the reactants’ molar ratio, reaction time, stirring speed, and reaction temperature were varied to identify the most appropriate conditions for synthesis. The resulting Dt‐Ph possessed a particle size of 213.9 nm, a zeta potential of −115.1 mV, and a 95.6% encapsulation effectiveness, indicating the successful formation of the phytosome. Scanning electron microscopy (SEM) was used to analyze the morphology of the surface of Dt and Dt‐Ph. The in vitro dissolution in 24 h and normal cell cytotoxic activities of the selected formulation were evaluated. The solubility of Dt‐Ph in buffered media was four times higher than Dt, indicating greater hydrophilicity of Dt‐Ph in comparison to the more lipophilic‐free drug. Additionally, the formulation showed a noticeably increased rate and extent of dissolution studies on drug release, which was two times better than Dt. Cytotoxicity results on HEK‐293A cells showed that Dt‐Ph had less impact on normal cells compared to Dt. Diosmetin, a flavonoid aglycone that has diverse biological activities, was in combination with a lipid‐based delivery system—phytosome to improve its bioavailability. The complex was shown to have prospectively enhanced the solubility in different gastrointestinal environments for further application of oral administration.