In-vivo microwave-aided spectrofluorimetric characterization of teneligliptin-loaded solid dispersion adsorbate using quality by design approach

Abstract

This study developed a microwave-aided spectrofluorimetric method for in-vivo characterizing teneligliptin-loaded solid dispersion adsorbate (TNG-SDA) using a quality by design approach. The microwave-aided chemical reaction was applied for derivatization of non-fluorescent teneligliptin with NBD-Cl (7-chloro-4-nitrobenzoxadiazole). TNG-SDA was prepared to enhance the solubility and bioavailability of teneligliptin, a BCS (Biopharmaceutical Classification System) class II drug. The method utilized environmentally friendly solvents and employed analytical quality by design principles for optimization. Critical method parameters were identified through failure mode impact analysis and optimized using response surface modelling. The fluorescence spectra of teneligliptin exhibited linearity across the concentration range of 50–250 ng/mL, with a correlation coefficient of 0.9978. The developed method was found to be accurate, precise, robust, specific and sensitive for estimation of teneligliptin. The method was applied to evaluate in vitro dissolution, pharmacokinetics, and pharmacodynamic of TNG-SDA compared to commercial formulations. Results showed significant improvements in teneligliptin solubility and bioavailability with the developed SDA. The microwave-aided derivatized fluorescent product was characterized by mass spectrometry. The method demonstrated environmental sustainability, robustness, sensitivity, cost-effectiveness, and user-friendliness when evaluated using white analytical chemistry approaches. It provided a sensitive and green alternative to existing hyphenated techniques for nanogram-level teneligliptin detection in pharmacokinetic studies.