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Updated: Feb 19, 2026
Computed Tomography-guided Time-domain Diffuse Fluorescence Tomography in Small Animals for Localization of Cancer Biomarkers
Published on: July 17, 2012
Mapping of drug distribution in the rabbit liver tumor model by complementary fluorescence and mass spectrometry
Katrin Fuchs1, Andras Kiss2, Pierre E Bize3
1School of Pharmaceutical Sciences, University of Geneva, University of Lausanne, Geneva, Switzerland.
Abstract:
This study describes the use of fluorescence imaging and mass spectrometry imaging, for imaging the anti-angiogenic drug sunitinib, used to treat liver cancer. These techniques allowed for the assessment of local delivery of the unlabeled therapeutic drug. More specifically, the spatial distribution of the drug and its metabolites after local administration was investigated, and drug levels in tumor and liver tissue over time were quantified. For this purpose, sunitinib-eluting microspheres were locoregionally injected into the tumor feeding arteries of rabbits bearing liver tumors. In adjacent areas of tumor and non-targeted contralateral liver tissue, sunitinib distribution was mapped around beads in occluded vessels 7, 12, 13 and 14days after embolization by means of the two imaging methods. Presence of sunitinib metabolites was assessed by mass spectrometry imaging. Sunitinib was found around microspheres in the tumor at day 7, 12, and 13. The drug was retained by the necrotic tumor tissue, resulting in homogeneously distributed and high levels of up to 40μg/g tissue in a 1.5mm radius around the beads. The drug was almost completely eliminated from the contralateral liver tissue. Several of the drug's metabolites, including its primary active metabolite SU12662, were detected in the tumor tissue over 13days. Sunitinib diffused from the beads and was retained at high, therapeutic levels during 13days. This was confirmed independently by complementary fluorescence and mass spectrometry imaging, which served as tools to confirm effective drug delivery after hepatic transarterial administration in situ. Compound: Sunitinib: PubChem CID 5329102.
Insights
Fluorescence and mass spectrometry imaging confirmed effective local delivery of sunitinib, an anti-cancer drug, to liver tumors in rabbits. The drug was retained in the tumor for 13 days, achieving high therapeutic levels.
Area of Science:
- Oncology
- Pharmacology
- Medical Imaging
Background:
- Liver cancer treatment often involves targeted drug delivery.
- Assessing drug distribution and retention is crucial for treatment efficacy.
- Sunitinib is an anti-angiogenic drug used for liver cancer.
Purpose of the Study:
- To evaluate the local delivery and spatial distribution of sunitinib using fluorescence and mass spectrometry imaging.
- To quantify drug levels in tumor and liver tissue over time after administration.
- To investigate the retention and metabolism of sunitinib in liver cancer models.
Main Methods:
- Sunitinib-eluting microspheres were administered via hepatic transarterial injection in rabbits with liver tumors.
- Fluorescence imaging and mass spectrometry imaging were used to map drug distribution around microspheres.
- Drug levels and metabolites were quantified in tumor and contralateral liver tissue at various time points (7, 12, 13, 14 days).
Main Results:
- Sunitinib was successfully localized around microspheres within the tumor tissue.
- High drug concentrations (up to 40μg/g) were maintained within a 1.5mm radius of the beads for 13 days.
- Sunitinib metabolites, including SU12662, were detected in tumor tissue, while the drug was largely eliminated from healthy liver tissue.
Conclusions:
- Fluorescence and mass spectrometry imaging are effective tools for assessing local drug delivery in liver cancer.
- Sunitinib-eluting microspheres provide sustained drug release and high local concentrations in the tumor.
- This approach demonstrates effective in situ drug delivery for liver cancer treatment.
