Monodispersed magnetographene quantum dot nanocomposites for delivery of silibinin

Abstract

Silibinin shows multi-applications and therapeutic activities such as anticancer, antioxidant, hypocholesterolemic, cardioprotective, neuroprotective and hepatoprotective but exhibits limited clinical applications due to poor oral bioavailability and in-vitro in-vivo biological correlation. The present study focused on the characterization of magnetic graphene quantum dot nanocomposites for silibinin delivery with a specific interest in kidney cancer treatment optimized by a central composite design. The effect of the composition of polylactic-co-glycolic acid (PLGA), polyvinyl alcohol (PVA) and silibinin on the mean particle size and encapsulation efficiency was studied. The properties of the synthesized magnetic graphene nanocomposites by using silibinin magnetic nanoparticles determined by central composite design method revealed particle size below 300 nm, high encapsulation efficiency (81.27 %) and cumulative in-vitro drug release exhibited in sustained manner. In vitro cellular uptake studies with kidney cancer cell line (A-498) demonstrated that the magnetic graphene quantum dot nanocomposites presented higher cellular uptake of silibinin and cytotoxicity than graphene quantum dots. The in-vivo pharmacokinetic study demonstrated a significant improvement in drug bioavailability with better mean residence time due to prolong exposure in systemic circulation. Therefore, monodispersed magnetic graphene quantum dot nanocomposites are considered as an interesting alternative for silibinin delivery against kidney cancer cell line A-498.