Preparation of silymarin-loaded zein polysaccharide core–shell nanostructures and evaluation of their biological potentials

Abstract Silymarin-loaded zein polysaccharide core–shell nanoparticles (SZPCS-NPs) were synthesized where sodium alginate and pectin offer stability and controlled release qualities to zein, a maize protein, having excellent biocompatibility. The present study is an attempt to develop zein–silymarin polysaccharide core–shell nanostructures to enhance water solubility, thereby improving bioavailability and producing enhanced biological responses in living systems. SZPCS-NPs were prepared using pH-induced antisolvent precipitation method. Five different types of SZPCS-NPs were synthesized using different combinations of sodium alginate and pectin, namely P100–A00 (non-uniform size ranging from 20 to 100 nm), P70–A30 (spherical and uniform size measuring approximately 80 nm in diameter), P50–A50, P30–A70, and P00–A100 exhibited irregular shapes with the presence of some triangular and oval structures and non-uniform size ranging from 20 to 100 nm. The SZPCS-NPs P70–A30 possessed the best results in terms of shape, size, and other characterization studies. Furthermore, the SZPCS-NPs possessed a percent drug loading of 72.5% and entrapment efficiency of 51.7%, respectively. The resulting SZPCS-NPs exhibited an excellent relative bioavailability percentage of 97.4% in comparison to commercial silymarin, having 58.1%, and crude silymarin, having 46.97% bioavailability percentage, correspondingly. In addition, SZPCS-NPs possessed an almost two folds’ increase in antioxidant activity in comparison to crude and commercially available silymarin. Similarly, SZPCS-NPs also showed better stabilization in hepatic biomarker enzymes and possessed better hepatoprotective activity for a period of 6 weeks, in contrast to commercial and crude silymarin formulations.