Nanosuspension of Poorly Soluble Anti-Diabetic Drug for Enhancement of Solubility and Dissolution

Canagliflozin is an anti-diabetic drug used in the adjuvant therapy for type-II diabetes as the inhibitor of sodium‐glucose co‐transporter-2 in the renal tubules. The poor solubility and permeability of the drug show limitations in the formulation development and therapeutic plasma concentration. The objective of the work was to improve the solubility and dissolution of the BCS class IV drug through surfactant stabilized nanosuspension formulation. Nanoparticles were developed by Nano precipitation-solvent evaporation method using Poly vinyl alcohol and Pluronic as surfactants at 1%, 3% and 5% concentration. Formulation optimized with Pluronic exhibited nano size particles (81-117 nm) with monodisperse nature and high stability zeta potential. The nanosuspension prepared using 1% and 3% Pluronic F127 showed 2-fold and 5- fold increase in the drug dissolution compared to the pure drug aqueous dispersion. The drug and surfactant exhibited mild interactions due to hydrogen bonding and hydrophobic interactions as confirmed by the FTIR and TG-DSC analysis, which favoured the formation of stable nanoparticles. The SEM proved the formation of smooth surface spherical shaped nanoparticles. Hence, the development of Canagliflozin nano-formulation was evidenced be an optimized approach to enhance the dissolution of the drug.