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Abstract

The purpose of this research was to develop novel solid dispersions (SDs) of BCS class IV drug, canagliflozin hemihydrate (CFZ) using Eudragit ® E PO (EE PO) as a carrier, to enhance its solubility and dissolution rate. Solvent evaporation technique was used to prepare SDs. The SDs were evaluated for saturated solubility, in-vitro dissolution study, solidstate characterization using FTIR, DSC, XRD and SEM, and flow properties. The solubility of CFZ in SDs increased manifold as compared with pure CFZ. Low values of angle of repose, Carr"s index, and Hausner ratio indicated good flow properties. The difference factor (f 1) and similarity factor (f 2) values suggested that dissolution profiles of the SDs were dissimilar to market product and the comparative dissolution curves revealed that SDs released CFZ faster than the marketed product. XRD patterns and DSC thermographs suggested that the SDs were present in an amorphous form, unlike pure crystalline CFZ. SEM studies showed CFZ has discrete crystalline particles whereas SD2 has diffuse, irregular asymmetrical structure. The SDs was superior to pure CFZ as they showed substantial improvement in solubility and dissolution rate along with good flow properties. Hence, the amorphous form of CFZ was successfully achieved by formulating it into SDs using EE PO as the carrier, which has conferred an increase in solubility and dissolution rate.

Mechanochemical Approach to Obtaining a Multicomponent Fisetin Delivery System Improving Its Solubility and Biological Activity

“…According to the literature, the enhanced apparent solubility could have beneficial effects on the compound's biological properties [24,42,43,46,96,97]. In our investigation, the increased solubility of FIS upon incorporation into ASIs resulted in alterations to its antioxidant and neuroprotective capabilities (see Table 2).…”