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Abstract #1900

Organic radical contrast agents based on polyacetylenes containing 2,2,6,6-tetramethylpiperidine 1-oxyl (TEMPO): targeted MR /optical bimodal imaging of folate receptor expressing HeLa tumors in vitro and in vivo

Lixia Huang 1 , Chenggong Yan 1 , Danting Cui 1 , Xiang Liu 1 , Xiaodan Lu 1 , Yichen Yan 2 , Xiangliang Tan 1 , Jun Xu 3 , Yingjie Mei 4 , Xinwei Lu 2 , Yikai Xu 1 , and Ruiyuan Liu 2

1 Department of Medical Imaging Center, Nanfang Hospital, Southern Medical University, Guangzhou, Guangdong, China, 2 School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, Guangdong, China, 3 Department of Hematology, Nanfang Hospital, Southern Medical University, Guangzhou, Guangdong, China, 4 Philips Healthcare, Guangzhou, Guangdong, China

Polyacetylenes containing 2,2,6,6-tetramethyl-piperidinooxy and poly(ethylene glycol) conjugated with carboxyl fluorescein and folic acid (FA) are synthesized by metathesis polymerization of corresponding substituted acetylenes for targeted bimodal MRI /optical imaging of tumors. In vitro studies confirm excellent binding specificity and subsequent enhanced cellular internalization of the targeted ORCAs (PA-TEMPO-FI-FA). In vivo T1-weighted MRI and optical imaging demonstrate the active tumor targeting ability of PA-TEMPO-FI-FA to generate specific contrast enhancement in mice bearing HeLa tumors. These results indicate that the multifunctional ORCAs may provide a tumor-targeted delivery platform for further molecular imaging guided cancer therapy.

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