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Noninvasive imaging of c(RGD)29R as a potential delivery carrier for transfection of siRNA in malignant tumors

文献作者：Xue Qi Chen, Meng Liu, Rong Fu Wang, Ping Yan, Chun Li Zhang, Chao Ma, Qian Zhao, Lei Yin, Guang Yu Zhao, Feng Qin Guo   《Journal of Labelled Compounds and Radiopharmaceuticals》

ABSTRACTS
The purpose of our study was to develop and evaluate a novel integrin αvβ3specific delivery carrier for transfection of siRNA in malignant tumors. We adopted arginineglycineaspartate (RGD) motif as a tissue target for specific recognition of integrin ανβ3. A chimaeric peptide was synthesized by adding nonamer arginine residues (9arginine [9R]) at the carboxy terminus of cyclicRGD dimer, designated as c(RGD)29R, to enable small interfering RNA (siRNA) binding. To test the applicability of the delivery carrier in vivo, c(RGD)29R was labeled with radionuclide of technetium99m. Biodistribution and γcamera imaging studies were performed in HepG2 xenograftbearing nude mice. As results, an optimal 10:1 molar ratio of 99mTcc(RGD)29R to siRNA was indicated by the electrophoresis on agarose gels. 99mTcc(RGD)29R/siRNA remained stable under a set of conditions in vitro. For in vivo study, tumor radioactivity uptake of 99mTcc(RGD)29R/siRNA in nude mice bearing HepG2 xenografts was significantly higher than that of control probe (P < .05). The xenografts were clearly visualized at 4 hours till 6 hours noninvasively after intravenous injection of 99mTcc(RGD)29R/siRNA, while the xenografts were not visualized at any time after injection of control probe. It was concluded that c(RGD)29R could be an effective siRNA delivery carrier. Technetium99m radiolabeleddelivery carrier represents a potential imaging strategy for RNAibased therapy.
SCREENSHOT

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All the peptides were synthesized by ChinaPeptides Co, Ltd.
CHAINING
https://onlinelibrary.wiley.com/doi/full/10.1002/jlcr.3514
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