Fabrication and Optimization of Regorafenib-loaded Solid Lipid Nano Carrier Using Box Behnken Design: In Vitro and Ex Vivo Intra-nasal Permeation Study
Background:
Over the last ten years, there has been little clinical progress in the treatment of glioblastoma, partially because there are no efficient drug delivery techniques that can pass across the blood-brain-tumor-barrier.
Objective:
The present study deals with the development optimization of Regorafenib-loaded Solid lipid na-noparticle(RF-SLN) for intranasal delivery of Regorafenib.
Method:
A Box-Behnken Design was employed to develop and optimize seventeen formulations using the solvent evaporation method, followed by ultrasonication. Each formulation was characterized in terms of particle size, entrapment efficiency (EE%), and zeta potential. The optimized SLN formulation was then con-verted into an in situ gel and assessed for intranasal ex vivo permeation.
Results:
The optimized formulation showed a particle size of 190.1nm, EE% of 81.3%, and zeta potential of -23.8 mV. The optimized Regorafenib-SLN in-situ gel showed enhanced drug permeability as compared to the Regorafenib-in-situ gel.
Conclusion:
It can be concluded that an SLN-based nanocarrier system can be successfully applied for the intranasal delivery of Regorafenib targeting to the brain.