Mg-Based Micromotor Enhanced Targeted Delivery and DESI Mass Spectrometry Imaging of Canagliflozin.

Desorption electrospray ionization (DESI) mass spectrometry (MS) is an increasingly indispensable tool for the analysis and imaging of drug molecules. However, the drug tracked by DESI MS is subjected to poor signal sensitivity due to the low drug dosage and tissue distribution. In this work, a Mg-based micromotor active drug delivery carrier (Mg/PLGA/CANA/CHI) was proposed for the successful encapsulation of canagliflozin (CANA). Compared to the persral and passive drug administration, this active drug delivery vector significantly improved the sensitivity for renal detection of CANA at m/z 489.1378 and 479.1089, determined as [CANA+HCOO]- and [CANA+Cl]- by both UPLC-HRMS and DESI MS. Furthermore, the drug delivery carrier was adopted for the DESI MS imaging (DESI MSI) of CANA in the mouse kidney section, which resulted in higher sensitivity than those with persral and passive drug administration attributed to the intensive micromotor‑enhanced gastric mucosal adhesion, thus contributing to high oral bioavailability. Meanwhile, this Mg-based micromotor has no interference with MS and MSI detection of the drug. Overall, the strategy of combining the active drug delivery of Mg-based micromotors with mass spectrometry detection provides a new method for the detection of low-dose drugs, their localization in tissues, and the evaluation of therapeutic efficacy.