Development of novel dapagliflozin loaded solid self-nanoemulsifying oral delivery system: Physiochemical characterization and in vivo antidiabetic activity

Abstract

Self-nanoemulsifying drug delivery system (SNEDDS) is one of the most promising nanoplatforms to enhance the oral efficacy of poorly-bioavailable therapeutics. The present study aimed to develop solid-SNEDDS (S-SNEDDS) for oral delivery of dapagliflozin. Dapagliflozin loaded SNEDDS was developed using eucalyptus oil, tween 80 and PEG 400 as the formulation components and then converted to S-SNEDDS using the biocompatible adsorbent avicel PH-101. The droplet size of SNEDDS and reconstituted S-SNEDDS was found to be 65.23 ± 5.54 nm and 74.23 ± 3.86 nm with negative zeta potential, respectively. The in-vitro drug release studies revealed that the release dapagliflozin was better from S-SNEDDS (93.79 ± 2.23% in 1 h) as compared to the pure drug (38.33 ± 1.78%) and exhibited zero order release kinetics. Solid-state characterization of S-SNEDDS revealed that dapagliflozin was compatible with formulation components and was converted in amorphous state inside S-SNEDDS. Moreover, dapagliflozin loaded SNEDDS and S-SNEDDS exhibited significantly higher hypoglycaemic effect in diabetic albino rats as compared to pure drug. Therefore, our findings strongly suggest that developed S-SNEDDS could serve as an efficient nanoplatform for oral delivery of dapagliflozin for better management of diabetes mellitus.