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Oral Sessions
Day 2, June 23（Mon.） 16:10-16:25
Room A (Maesato West)
- 2A-O3-1610
Comparative Distribution of Free Eribulin and Eribulin Liposomal Formulation in Mouse Syngeneic Tumors Using Desorption Electrospray Ionization Mass Spectrometry Imaging
(1Eisai, DMPK, 2Eisai, DCV function)
oTomomi Ishida1, Yuki Niwa2, Koichiro Hotta1, Taro Semba2, Yuji Mano1
A liposomal formulation of eribulin, which is a tubulin and microtubule dynamics inhibitor, is under development. The liposomal formulation allows the encapsulated drug to accumulate in tumors through the enhanced permeability, resulting in enhanced antitumor activity. Mass spectrometry imaging (MSI) is a novel technology that quantitatively visualizes the spatial distribution of drugs in tissues. In this study, we visualized localization of eribulin in syngeneic mouse tumors to compare distribution after intravenous administration of free eribulin and eribulin-liposomal formulation (LF) using desorption electrospray ionization (DESI)-MSI.
Tumors collected at seven time points were split in half; one half was used for quantification of eribulin by LC-MS/MS, and the other for MSI and immunohistochemistry (IHC) staining for CD31. The samples were snap-frozen in liquid nitrogen, followed by sectioning. The localization of eribulin in tumor sections was investigated using DESI-MSI.
At 2 h postdose, eribulin was homogeneously distributed in the tumor after free eribulin was dosed, while the vascular localization was noted for eribulin-LF. Concentrations of eribulin were well correlated when assayed by DESI-MSI and LC-MS/MS. These results indicate that DESI-MSI is a useful semi-quantitative technique to explore changes in the intra-tissue distribution of drugs by liposomal formulation in drug development.