| siRNA的体内递送及药物代谢动力学特性 |
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| 引用本文： | 郭佳佳,王建军,徐根兴. siRNA的体内递送及药物代谢动力学特性[J]. 药学与临床研究, 2010, 18(4): 363-365 |
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| 作者姓名： | 郭佳佳 王建军 徐根兴 |
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| 作者单位： | 1. 南京大学,生命科学院,南京,210093
2. 南京大学,医学院公共健康医学中心生命分析化学教育部重点实验室,南京,210093;江苏省基因药物工程技术研究中心,苏州,215128 |
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| 基金项目： | 国家重大新药创制项目，江苏省自然科学基金 |
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| 摘 要： | siRNA作为一种高效的RNA干扰药物在疾病治疗方面前景广阔。但其临床应用还需解决由于高负电荷和分子量等引起的体内递送系统、脱靶效应、免疫激活、毒副作用、改善其药物代谢动力学特性等问题。本文简要综述了siRNA的作用原理、体内递送方式、药代动力学特性、安全问题及临床应用展望。
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| 关 键 词： | 小干扰RNA RNA干扰 药物代谢动力学 |
| 收稿时间： | 2010-04-14 |
| 修稿时间： | 2010-05-11 |
Pharmacokinetic Perspective and the Delivery of siRNA in vivo |
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| GUO Jia-ji,WANG Jian-jun and XU Gen-xing. Pharmacokinetic Perspective and the Delivery of siRNA in vivo[J]. Pharmacertical and Clinical Research, 2010, 18(4): 363-365 |
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| Authors: | GUO Jia-ji WANG Jian-jun XU Gen-xing |
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| Affiliation: | School of Life Sciences, Nanjing University, Nanjing 210093, China;School of Life Sciences, Nanjing University, Nanjing 210093, China;Key Laboratory of Analytical Chemistry for Life Science, Center for Public Health Research, Nanjing University, Nanjing 210093, China; Jiangsu Research Center for Gene Pharmaceutical Engineering and Technology, Suzhou 215128, China |
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| Abstract: | As an effective RNA interference(RNAi) drugs, small interfering RNAs(siRNA) point to a bright future for siRNA-based therapeutics. However, the overall negative charge of siRNA molecules, the off-target effects, immune activation, side effects and the relatively high molecular weight prevented siRNA from functional uptake for its clinical application. To overcome these limitations, delivery technologies for synthetic siRNAs are currently being developed to improve their pharmacokinetic properties. This paper provides a brief overview of the actions of siRNA, its in vivo mode of delivery, pharmacokinetics, safety, and prospects of clinical application. |
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| Keywords: | siRNA RNAi Pharmacokinetics |
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