Transforming canagliflozin solubility using lipidic carrier and its pharmacokinetic study

The European Medicine Agency has approved canagliflozin (CGF) drug to improve glycemic control in patients with type II diabetes. Our study aimed to enhance the solubility and pharmacokinetics of canagliflozin. Since crystalline canagliflozin is insoluble in water, its absolute bioavailability is less than 65%. Gelucire 50/13 was used as a lipid-based drug carrier to create solid dispersions of canagliflozin. SEM, PXRD, and DSC analysis all pointed to canagliflozin as having a crystal structure. Fusion and solvent evaporation methods were used to prepare the solid dispersions. In solid dispersions, the medication was found to be amorphized according to SEM, DSC, and PXRD studies. The water solubility of canagliflozin increased significantly by 11-23 fold using the solvent evaporation approach and by 12-25 fold using the fusion method. The pharmacokinetic parameters are improved at higher concentrations of gelucire. With pure canagliflozin, the AUC values climbed over 4 h (t_max) to 23440 µgh/mL, while with GDF 1:7, they grew to 52217. Gelucire 50/13 is an excellent option as a biomaterial carrier for drug delivery systems that use solid dispersion because it enhances biological membrane penetration. By dispersing the canagliflozin and gelucire, bioavailability may be enhanced by the fusion process that achieves molecular binding.