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Lingxiao Chen,1,* Wei He,1,* Huichuan Jiang,1,* Longxiang Wu,1 Wei Xiong,1 Bolun Li,1 Zhihua Zhou,2 Yuna Qian3–5 1Department of Urology, Xiangya Hospital, Central South University, Changsha, Hunan 410008, China; 2School of Chemistry and Chemical Engineering, Hunan University of Science and Technology, Xiangtan, Hunan 411201, China; 3Wenzhou Institute of Biomaterials and Engineering, Chinese Academy of Science, Wenzhou, Zhejiang 325001, China; 4School of Ophthalmology and Optometry, School of Biomedical Engineering, Wenzhou Medical University, Wenzhou, Zhejiang 325035, China; 5Key Laboratory of Biorheological Science and Technology (Chongqing University), Ministry of Education, Chongqing 400045, China *These authors contributed equally to this work Purpose: PB is one of the most severe complications of late stage prostate cancer and negatively impacts patient quality of life. A major challenge for the treatment of cancer bone metastasis is the management of efficient drug delivery to metastatic bone lesion. We aimed to explore the use of aptamers as promising tools to develop a targeted drug delivery system for PBs. Materials and methods: In vivo SELEX was applied to identify bone targeting aptamer in a mouse model with PBs. Results: The aptamer (designated as “PB”) with the highest bone targeting frequency in mice bearing PC3 PB was selected for further analysis. The PB aptamer specifically targeted modulated endothelial cells in response to cancer cells in the bones of mice bearing PC3 PBs. The targeting efficiency of the PB aptamer conjugated to gold particles was verified in vivo. Conclusion: This investigation highlights the promise of in vivo SELEX for the discovery of bone targeting aptamers for use in drug delivery. Keywords: aptamer, tumor endothelial targeting, drug delivery

Lingxiao Chen,1,* Wei He,1,* Huichuan Jiang,1,* Longxiang Wu,1 Wei Xiong,1 Bolun Li,1 Zhihua Zhou,2 Yuna Qian3–5 1Department of Urology, Xiangya Hospital, Central South University, Changsha, Hunan 410008, China; 2School of Chemistry and Chemical Engineering, Hunan University of Science and Technology, Xiangtan, Hunan 411201, China; 3Wenzhou Institute of Biomaterials and Engineering, Chinese Academy of Science, Wenzhou, Zhejiang 325001, China; 4School of Ophthalmology and Optometry, School of Biomedical Engineering, Wenzhou Medical University, Wenzhou, Zhejiang 325035, China; 5Key Laboratory of Biorheological Science and Technology (Chongqing University), Ministry of Education, Chongqing 400045, China *These authors contributed equally to this work Purpose: PB is one of the most severe complications of late stage prostate cancer and negatively impacts patient quality of life. A major challenge for the treatment of cancer bone metastasis is the management of efficient drug delivery to metastatic bone lesion. We aimed to explore the use of aptamers as promising tools to develop a targeted drug delivery system for PBs. Materials and methods: In vivo SELEX was applied to identify bone targeting aptamer in a mouse model with PBs. Results: The aptamer (designated as “PB”) with the highest bone targeting frequency in mice bearing PC3 PB was selected for further analysis. The PB aptamer specifically targeted modulated endothelial cells in response to cancer cells in the bones of mice bearing PC3 PBs. The targeting efficiency of the PB aptamer conjugated to gold particles was verified in vivo. Conclusion: This investigation highlights the promise of in vivo SELEX for the discovery of bone targeting aptamers for use in drug delivery. Keywords: aptamer, tumor endothelial targeting, drug delivery