Nano-Emulsification and Soft Gel Encapsulation to Improve the Delivery of Anti-Diabetic Drug Ertugliflozin-L-Pyroglutamic Acid via SNEDDS: An In Vitro Assessment using RP-HPLC.

Objective

This study aim to develop and evaluate a novel soft gelatin capsule formulation of Ertugliflozin-L-Pyroglutamic Acid (ERT) using a self-nanoemulsifying drug delivery system (SNEDDS) to enhance its solubility, physicochemical stability, and in vitro drug dissolution relative to the commercial Steglatro® tablets.

Significance

Poor aqueous solubility and limited dissolution behavior are two major challenges that hinder the therapeutic performance of many antidiabetic drugs. Herein, for the first time we formulated ERT as a SNEDDS-based soft gelatin capsule, providing a promising strategy for enhancing oral drug delivery system that manages Type 2 diabetes more efficiently.

Methods

ERT was encapsulated in a SNEDDS formulation matrix of Labrasol® (surfactant), PEG-200 (co-surfactant) and cardamom oil in an optimized ratio. Stability studies were conducted across varied pH ranges, mimicking the gastrointestinal tract environment. Advanced characterization techniques, including AFM, DLS, Zetasizer and FT-IR spectroscopy confirmed consistent particle size and desirable morphological attributes. RP-HPLC as per ICH guidelines evaluated dissolution profile and assay recovery against the commercial Steglatro® tablets.

Results

The optimized ERT-SNEDDS soft gel formulation demonstrated high stability across various pH conditions, with an assay recovery of 98.78 ± 0.04%. The complete dissolution profile (CDP) at three different pH values (0.1 N HCl, pH 4.5 and pH 6.8 buffers) showed significantly superior in vitro drug release compared to established Steglatro® tablet.

Conclusion

The developed SNEDDS based soft gelatin capsule demonstrated favorable physicochemical characteristics and rapid in vitro dissolution of ERT, supporting its potential as an alternative lipid-based oral dosage form to the marketed tablet.