In vivo pharmacokinetic analysis for fluorescently labeled RGD peptide targeted to the alpha v beta 3 integrin in Kaposi’s sarcoma

Sunkuk Kwon; Shi Ke; Jessica P. Houston; Wei Wang; Qingping Wu; Chun Li; Eva M. Sevick Muraca

doi:10.1117/12.589399

8 April 2005 In vivo pharmacokinetic analysis for fluorescently labeled RGD peptide targeted to the α_vβ₃ integrin in Kaposi’s sarcoma

Sunkuk Kwon, Shi Ke, Jessica P. Houston, Wei Wang, Qingping Wu, Chun Li, Eva M. Sevick Muraca

Author Affiliations +

Proceedings Volume 5689, Optical Methods for Tumor Treatment and Detection: Mechanisms and Techniques in Photodynamic Therapy XIV; (2005) https://doi.org/10.1117/12.589399
Event: SPIE BiOS, 2005, San Jose, CA, United States

Abstract

The dose dependence of near-infrared (NIR) fluorescent labeled RGD peptide targeted to the α_vβ₃ integrin was assessed from xenografts bearing a subcutaneous human Kaposi’s sarcoma (KS1767) with dynamic NIR fluorescence optical imaging. The three-compartment pharmacokinetic (PK) model was used to determine PK parameters from fluorescence images acquired with an intensified charge-coupled device (ICCD) system. Dynamic imaging of Kaposi’s sarcoma bearing animals was conducted with i.v. administration of Cy5.5-c(KRGDf) at doses of 0.75 to 6 nmol/animal and at the doses of 300 or 600 nmol of c(KRGDf) administered 1 hour before the injection of 3 nmol dose of the conjugate. The results show early and rapid uptake of Cy5.5-c(KRGDf), which was mediated by the administration of c(KRGDf) 1 hour before administration at the conjugate agent. From the results we found a linear increase in PK uptake rates at doses of 0.75 to 1.5 nmol, reflecting unsaturated binding to the integrin receptor. However, the results show the dose independence at large dose amounts from 3 to 6 nmol per animal. The effects of cancer treatments as well as diagnostics may be evaluated by in vivo PK analysis with NIR fluorescence optical imaging.

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Sunkuk Kwon, Shi Ke, Jessica P. Houston, Wei Wang, Qingping Wu, Chun Li, and Eva M. Sevick Muraca "In vivo pharmacokinetic analysis for fluorescently labeled RGD peptide targeted to the α_vβ₃ integrin in Kaposi’s sarcoma", Proc. SPIE 5689, Optical Methods for Tumor Treatment and Detection: Mechanisms and Techniques in Photodynamic Therapy XIV, (8 April 2005); https://doi.org/10.1117/12.589399

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