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Journal of Biomedical Optics

Quantifying molecular specificity of αvβ3 integrin-targeted optical contrast agents with dynamic optical imaging
Author(s): Mikhail Gurfinkel; Shi Ke; Wei Wang; Chun Li; Eva Marie Sevick-Muraca
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Paper Abstract

Dynamic fluorescence images were obtained from a subcutaneous human Kaposi's sarcoma tumor (KS1767) model immediately following the intravenous injection of an integrin-targeting cyanine dye conjugate, Cy5.5-c(KRGDf). The fluorescence images, acquired via an intensified charge-coupled device detection system, were used in conjunction with a pharmacokinetic (PK) model to determine kinetic properties of target binding in the presence and absence of a competitive ligand, free c(KRGDf). The results indicate that the conjugate dye behaves similarly in normal tissue to the free Cy5.5 dye while it possesses increased uptake in tumor tissue. The change in pharmacokinetic parameters obtained from dynamic imaging of Cy5.5-c(KRGDf) after administration of c(KRGDf) as a competitive ligand to the integrin receptor suggests that (i) the increased uptake of Cy5.5-c(KRGDf) is molecularly specific and that (ii) receptor turnover occurs within 24 h. In addition, PK analysis enables quantification of an in vivo c(KRGDf) binding constant attributable to integrin binding. In vivo pharmacokinetic analysis based on rapid and dynamic optical imaging may be potentially useful for evaluating the presence and turnover rate of disease markers that are potential targets of molecular medicine.

Paper Details

Date Published: 1 May 2005
PDF: 9 pages
J. Biomed. Opt. 10(3) 034019 doi: 10.1117/1.1924696
Published in: Journal of Biomedical Optics Volume 10, Issue 3
Show Author Affiliations
Mikhail Gurfinkel, Texas A&M Univ. (United States)
Shi Ke, The Univ. of Texas M.D. Anderson Cancer Ctr. (United States)
Wei Wang, The Univ. of Texas M.D. Anderson Cancer Ctr. (United States)
Chun Li, The Univ. of Texas M.D. Anderson Cancer Ctr. (United States)
Eva Marie Sevick-Muraca, Baylor College of Medicine (United States)

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