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Proceedings Paper

New approach to optical imaging of tumors
Author(s): Samuel I. Achilefu; Joseph E. Bugaj; Richard B. Dorshow; Hermo N. Jimenez; Raghavan Rajagopalan
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Paper Abstract

Site specific delivery of drugs and contrast agents to tumors protects normal tissues from the cytotoxic effect of drugs, and enhances the contrast between normal and diseased tissues. In optical medicine, biocompatible dyes can be used as phototherapeutics or as contrast agents. Previous studies have shown that the use of covalent or non-covalent dye conjugates of carriers such as antibiodies, liposomes, and polysaccharides improves the delivery of such molecules to tumors. However, large biomolecules can elicit adverse immunogenic reactions and also result in long blood clearance times, delaying visualization of target tissues. A viable alternative to this strategy is to use small bioactive molecule-dye conjugates. These molecules have several advantages over large biomolecules, including ease of synthesis of a variety of high purity compounds for combinatorial screening of new targets, enhanced diffusivity to solid tumors, and the ability to affect the pharmacokinetics of the conjugates by minor structural changes. Thus, we conjugated a near infrared absorbing dye to several bioactive peptides that specifically target overexpressed tumor receptors in established rat tumor lines. High tumor uptake of the conjugates was obtained without loss of either the peptide receptor affinity or the dye fluorescence. These findings demonstrate the efficacy of a small peptide-dye conjugate strategy for in vivo tumor imaging. Site-specific delivery of photodynamic therapy agents may also benefit from this approach.

Paper Details

Date Published: 2 July 2001
PDF: 5 pages
Proc. SPIE 4259, Biomarkers and Biological Spectral Imaging, (2 July 2001); doi: 10.1117/12.432489
Show Author Affiliations
Samuel I. Achilefu, Mallinckrodt, Inc. (United States)
Joseph E. Bugaj, Mallinckrodt, Inc. (United States)
Richard B. Dorshow, Mallinckrodt, Inc. (United States)
Hermo N. Jimenez, Mallinckrodt, Inc. (United States)
Raghavan Rajagopalan, Mallinckrodt, Inc. (United States)

Published in SPIE Proceedings Vol. 4259:
Biomarkers and Biological Spectral Imaging
Gregory H. Bearman; Darryl J. Bornhop; Darryl J. Bornhop; Richard M. Levenson, Editor(s)

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