Enhancement of the Dissolution and Solubility of Canagliflozin Using Nanodispersion Systems

Abstract

Background: Self-nanomicellizing solid dispersion is a new formulation that combines the advantages of solid dispersion with nanomicelle methods to increase drug oral bioavailability. The technique employs an appropriate carrier to produce a solid dispersion that self-assembles into nanomicelles when in contact with gastrointestinal fluids, improving medication solubility and absorption. Objective: The study aims to develop a self-nanomicellizing solid dispersion of canagliflozin and compare it to non-nanomicellizing formulations. Methods: The solvent evaporation approach was chosen to create a solid dispersion system with soluplus and poloxamer 407 as carriers. Different canagliflozin-to-carrier ratios were investigated in order to develop nanomicellar systems with improved canagliflozin dissolving characteristics. Solid-state analysis was used to characterize the optimum self-nanomicellizing and non-self-nanomicellizing formulations. Results: The physicochemical tests revealed that canagliflozin's crystalline structure transitioned to an amorphous state in the solid dispersion system of both carriers, as evidenced by powder X-ray diffraction and differential scanning calorimetry. Particle size analysis reveals that only soluplus, in all ratios tested, produces a self-nanomicellizing solid dispersion of canagliflozin, whereas poloxamer 407 does not. Self-nanomicellizing systems incorporating Soluplus had a faster dissolving profile than pure drug and non-self-nanomicellizing formulas. Conclusions: Canagliflozin nanodispersion systems with Soluplus as a carrier may improve solubility, dissolving rate, and bioavailability.