| 适配体C2min介导的可靶向2种前列腺癌基因的递送系统 |
| 投稿时间：2019-06-14 修订日期：2019-07-26 点此下载全文 |
| 引用本文：张晶,顾永卫,武鑫.适配体C2min介导的可靶向2种前列腺癌基因的递送系统[J].药学实践杂志,2020,38(1):47~51,66 |
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| 基金项目:国家自然科学基金（81072100）；上海市青年科技启明星计划资助（18QB1400400） |
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| 中文摘要:目的 通过合成可靶向两种前列腺癌的基因载体PAMAM-PEG-C2min，以提高基因的转染效率和肿瘤靶向性。方法 将双功能聚乙二醇的一端与聚酰胺-胺（PAMAM）相连，另一端与适配体（C2min）连接，并利用1H NMR技术对合成的PAMAM-PEG-C2min基因载体进行结构鉴定。通过两种前列腺癌PC3和LNCaP细胞的体外摄取和基因转染实验（包载siR-M基因），考察纳米复合物的生物学特性。并利用动物活体成像技术考察合成的纳米复合物的体内分布特征。结果 核磁共振结果表明，本研究成功合成了PAMAM-PEG-C2min。PC3和LNCaP细胞对PAMAM-PEG-C2min的摄取结果体现出浓度依赖性。且与不经C2min修饰的PAMA-PEGM相比，PAMAM-PEG-C2min递药系统的基因转染效率和肿瘤细胞靶向性明显提高。体内靶向性结果表明，PAMAM-PEG-C2min可实现同时靶向2种前列腺癌组织的作用。结论 本研究合成的PAMAM-PEG-C2min递送载体具有良好的肿瘤靶向性，为前列腺癌的综合治疗和靶向治疗提供了新的技术平台。 |
| 中文关键词:适配体 靶向 雄激素依赖型前列腺癌 雄激素非依赖型前列腺癌 基因载体 |
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| The C2min aptamer-modified gene delivery system for targeting ADPC/AIPC prostate cancer |
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| Abstract:Objective To synthesize a novel prostate cancer targeting gene vector PAMAM-PEG-C2min and improve gene transfection efficiency targeting on prostate cancer.Methods The aptamer (C2min) and polyamide-amine (PAMAM) were ligated by polyethylene glycol (PEG). The structure of the synthesized PAMAM-PEG-C2min was identified by NMR. The biological characteristics of the nanoparticles were examined by the uptake experiments and gene transfection experiments (the loaded gene was siR-M) with the prostate cancer cells (PC3 and LNCaP). Besides, the in vivo targeting was investigated using in vivo image system. The in vivo targeting results indicated that PAMAM-PEG-C2min can achieve the simultaneous targeting of two prostate cancer tissues.Results The PAMAM-PEG-C2min synthesis was confirmed by NMR. Cell uptake experiments showed that the cell uptake efficiency of PAMAM-PEG-C2min was concentration dependent. In vitro experiments showed that the PC3 and LNCaP cells transfection efficiency and targeting of PAMAM-PEG modified with C2min were significantly improved compared with the PEG modified PAMAM.Conclusion PAMAM-PEG-C2min is a potential targeted drug delivery vehicle. It provides a new technology platform for comprehensive and specific targeting treatment of prostate cancer. |
| keywords:adapter targeting drug delivery androgen-dependent prostate cancer androgen-independent prostate cancer gene vector |
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