Visual targeted therapy of hepatic cancer using homing peptide modified calcium phosphate nanoparticles loading doxorubicin guided by T1 weighted MRI.
Visual targeted therapy of hepatic cancer using homing peptide modified calcium phosphate nanoparticles loading doxorubicin guided by T1 weighted MRI.
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DOI：
10.1016/j.nano.2018.06.014
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发表时间：
2018-10
期刊：
影响因子：
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通讯作者：
Nan-nan Zhang;R. Yu;Min Xu;Xingyao Cheng;Chun-miao Chen;Xiaoling Xu;Chen-ying Lu;Kong-jun Lu
中科院分区：
文献类型：
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作者：
Nan-nan Zhang;R. Yu;Min Xu;Xingyao Cheng;Chun-miao Chen;Xiaoling Xu;Chen-ying Lu;Kong-jun Lu
肝癌的有效治疗和实时监测至关重要。研制了一种多功能磷酸钙纳米粒（A54-CaP/Gd-DTPA/DOX），用于肝癌的T1加权MRI实时可视化靶向治疗。A54-CaP/Gd-DTPA/DOX的纵向弛豫率（6.02 mM− 1 s −1）高于市售MR造影剂Gd-DTPA（3.3765 mM− 1 s −1）。DOX从纳米颗粒的释放表现出pH依赖性行为。细胞摄取结果表明，A54-CaP/Gd-DTPA/DOX通过与A54的结合被BEL-7402细胞内化的速度是HepG 2细胞的1.9倍，体内实验表明，A54-CaP/Gd-DTPA/DOX在肿瘤组织中的分布和滞留时间均比CaP/Gd-DTPA/DOX和游离DOX高，并且显示出良好的抗肿瘤效果（95.38%的肿瘤抑制率）和较低的毒性。此外，包裹在纳米颗粒中的Gd-DTPA可以提供T1加权MRI，用于实时监测肿瘤治疗的进展。
Effective treatment and real-time monitoring of hepatic cancer are essential. A multifunctional calcium phosphate nanoparticles loading chemotherapeutic agent doxorubicin and magnetic resonance imaging contrast agent diethylenetriaminepentaacetic acid gadolinium (A54-CaP/Gd-DTPA/DOX) was developed for visual targeted therapy of hepatic cancer via T1-weighted MRI in real-time. A54-CaP/Gd-DTPA/DOX exhibited a higher longitudinal relaxivity (6.02 mM−1s−1) than commercial MR contrast agent Gd-DTPA (3.3765 mM−1s−1). The DOX release from the nanoparticles exhibited a pH dependent behavior. The cellular uptake results showed that the internalization of A54-CaP/Gd-DTPA/DOX into BEL-7402 cells was1.9-fold faster than that of HepG2 cells via A54 binding.In vivoexperiments presented that A54-CaP/Gd-DTPA/DOX had higher distribution and longer retention time in tumor tissue than CaP/Gd-DTPA/DOX and free DOX, and also displayed great antitumor efficacy (95.38% tumor inhibition rate) and lower toxicity. Furthermore, the Gd-DTPA entrapped in the nanoparticles could provide T1-weighted MRI for real-time monitoring the progress of tumor treatment.