SOLUBILITY ENHANCEMENT OF REGORAFENIB VIA SOLID DISPERSION STRATEGY USING HYDROPHILIC CARRIERS
K. M. Lokamatha Swamy*, Punati Narendra
ABSTRACT
The present study investigated the molecular interactions governing the solid dispersion behavior of BCS Class-II drug Regorafenib using hydrophilic carriers, with the aim of enhancing its solubility. Solid dispersions at 1:1 and 1:2 drug-to-carrier weight ratios were prepared using PEG 4000 and PVP K90 by kneading method. Fourier-transform infrared (FTIR) spectroscopy was employed to investigate functional-group interactions and structural modifications associated with solubility enhancement, while saturation solubility and dissolution profiles were evaluated using USP Apparatus II. Distinct shifts and broadening of characteristic absorption bands, including N–H/O–H stretching at approximately 3400 cm⁻¹, C=O stretching at 1718–1720 cm⁻¹, Amide II vibration around 1550 cm⁻¹, and C–O–C stretching at 1200–1250 cm⁻¹, indicated hydrogen-bonding interactions between Regorafenib and the polymer matrices. Comparative analysis revealed greater amorphous character in PVP K90-based systems than in PEG 4000-based systems. These findings demonstrate the important role of polymer–drug hydrogen bonding in modulating the solubility and structural characteristics of Regorafenib in solid dispersions. Pure RGF exhibited extremely slow dissolution owing to its poor aqueous solubility. In contrast, all SDs showed a significant enhancement in the dissolution rate. The dissolution parameter analysis confirmed that F4 (RGF:PVP K90, 1:2 ratio) was the optimized formulation, exhibiting the shortest T50, highest DE, and greatest RDR. Overall, the study confirms that the solid dispersion technique can be effectively employed to enhance the solubility and dissolution of poorly soluble drug Regorafenib.
Keywords: Regorafenib, Solid dispersions, PVP K90, PEG 4000, FTIR, Solubility studies.
[Full Text Article]
[Download Certificate]
Impact Factor : 8.181 
