Imaging Dose-dependent Pharmacokinetics of an RGD-Fluorescent Dye Conjugate Targeted to αβ Receptor Expressed in Kaposi's Sarcoma

Dynamic fluorescence images were obtained from xenografts bearing a subcutaneous human Kaposi's sarcoma (KS1767) immediately following the intravenous injection of an integrin-receptor targeting Cy5.5-c(KRGDf) at a dose ranging from 0.75 to 6 nmol/mouse. The fluorescence images were acquired us...

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Main Authors: Sunkuk Kwon, Shi Ke, Jessica P. Houston, Wei Wang, Qingping Wu, Chun Li, Eva M. Sevick-Muraca
Format: Article
Language:English
Published: SAGE Publishing 2005-04-01
Series:Molecular Imaging
Online Access:https://doi.org/10.1162/15353500200505103
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author Sunkuk Kwon
Shi Ke
Jessica P. Houston
Wei Wang
Qingping Wu
Chun Li
Eva M. Sevick-Muraca
author_facet Sunkuk Kwon
Shi Ke
Jessica P. Houston
Wei Wang
Qingping Wu
Chun Li
Eva M. Sevick-Muraca
author_sort Sunkuk Kwon
collection DOAJ
description Dynamic fluorescence images were obtained from xenografts bearing a subcutaneous human Kaposi's sarcoma (KS1767) immediately following the intravenous injection of an integrin-receptor targeting Cy5.5-c(KRGDf) at a dose ranging from 0.75 to 6 nmol/mouse. The fluorescence images were acquired using an intensified charge-coupled device system and were analyzed with a three-compartment pharmacokinetic (PK) model to determine uptake parameters in the tumor and normal tissue regions of interest as a function of administered dose. Our results show that the uptake of Cy5.5-c(KRGDf) in tumor regions were: (i) significantly greater than the contralateral normal tissue regions; (ii) linearly increased with dose of Cy5.5-c(KRGDf) up to 1.5 nmol/mouse; and (iii) blocked by preinjection of c(KRGDf). Above doses of 1.5 nmol/mouse, the uptake no longer increased with dose, suggesting integrin receptor saturation. In normal tissues, the PK uptake parameters were not influenced by Cy5.5-c(KRGDf) dose nor by the preadministration of c(KRGDf).
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spelling doaj.art-8f6268496f894dc38f40eedc47c400602025-01-03T00:12:14ZengSAGE PublishingMolecular Imaging1536-01212005-04-01410.1162/1535350020050510310.1162_15353500200505103Imaging Dose-dependent Pharmacokinetics of an RGD-Fluorescent Dye Conjugate Targeted to αβ Receptor Expressed in Kaposi's SarcomaSunkuk Kwon0Shi Ke1Jessica P. Houston2Wei Wang3Qingping Wu4Chun Li5Eva M. Sevick-MuracaTexas A&M UniversityTexas A&M UniversityTexas A&M UniversityUniversity of Texas M.D. Anderson Cancer CenterUniversity of Texas M.D. Anderson Cancer CenterUniversity of Texas M.D. Anderson Cancer CenterDynamic fluorescence images were obtained from xenografts bearing a subcutaneous human Kaposi's sarcoma (KS1767) immediately following the intravenous injection of an integrin-receptor targeting Cy5.5-c(KRGDf) at a dose ranging from 0.75 to 6 nmol/mouse. The fluorescence images were acquired using an intensified charge-coupled device system and were analyzed with a three-compartment pharmacokinetic (PK) model to determine uptake parameters in the tumor and normal tissue regions of interest as a function of administered dose. Our results show that the uptake of Cy5.5-c(KRGDf) in tumor regions were: (i) significantly greater than the contralateral normal tissue regions; (ii) linearly increased with dose of Cy5.5-c(KRGDf) up to 1.5 nmol/mouse; and (iii) blocked by preinjection of c(KRGDf). Above doses of 1.5 nmol/mouse, the uptake no longer increased with dose, suggesting integrin receptor saturation. In normal tissues, the PK uptake parameters were not influenced by Cy5.5-c(KRGDf) dose nor by the preadministration of c(KRGDf).https://doi.org/10.1162/15353500200505103
spellingShingle Sunkuk Kwon
Shi Ke
Jessica P. Houston
Wei Wang
Qingping Wu
Chun Li
Eva M. Sevick-Muraca
Imaging Dose-dependent Pharmacokinetics of an RGD-Fluorescent Dye Conjugate Targeted to αβ Receptor Expressed in Kaposi's Sarcoma
Molecular Imaging
title Imaging Dose-dependent Pharmacokinetics of an RGD-Fluorescent Dye Conjugate Targeted to αβ Receptor Expressed in Kaposi's Sarcoma
title_full Imaging Dose-dependent Pharmacokinetics of an RGD-Fluorescent Dye Conjugate Targeted to αβ Receptor Expressed in Kaposi's Sarcoma
title_fullStr Imaging Dose-dependent Pharmacokinetics of an RGD-Fluorescent Dye Conjugate Targeted to αβ Receptor Expressed in Kaposi's Sarcoma
title_full_unstemmed Imaging Dose-dependent Pharmacokinetics of an RGD-Fluorescent Dye Conjugate Targeted to αβ Receptor Expressed in Kaposi's Sarcoma
title_short Imaging Dose-dependent Pharmacokinetics of an RGD-Fluorescent Dye Conjugate Targeted to αβ Receptor Expressed in Kaposi's Sarcoma
title_sort imaging dose dependent pharmacokinetics of an rgd fluorescent dye conjugate targeted to αβ receptor expressed in kaposi s sarcoma
url https://doi.org/10.1162/15353500200505103
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