中山大学附属第三医院核医学科
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焦举, 邹琼, 邹旻红, 等. 适配子修饰靶向PLGA纳米基因载体的构建[J]. 分析测试学报, 2013,32(1):100-105.
Preparation of Aptamer Modified PLGA Nanoparticles for Targeted Gene Delivery[J]. 2013,32(1):100-105.
化学合成了功能性三嵌段复合物乳酸乙醇酸共聚物-聚乙二醇-适配子(PLGA-PEG-Apt)。使用双乳化挥发法制备包裹DNA片段的PLGA-PEG-Apt新型纳米基因药物载体,表征检测显示:制备的纳米基因载体粒径为(225.2±8.1)nm,Zeta电位约(-35.5±-3.3)mV。扫描电子显微镜下纳米颗粒形态呈圆形,表面光滑,粒径分布较均匀。纳米粒子对TFO的包封率为(25.4±3.1)%(n=3),载药量为(1.34±0.16)μg/mg。体外释放实验研究结果显示持续释放过程达23 d,且PLGA-PEG- Apt纳米粒子呈突释之后的持续缓释过程。细胞水平实验结果显示,A10适配子修饰的纳米基因载体能更多进入靶向的前列腺癌细胞株,进而发挥其抗前列腺癌增殖的作用。该研究成功制备了靶向PLGA纳米基因载体,结果满意。
An amphiphilic triblock copolymer poly(lactic-co-glycolic-acid) polyethyleneglycol-A10 aptamer(PLGA-PEG-Apt) was synthesized,and its characteristic peaks were investigated with 1H nuclear magnetic resonance(1H NMR).Nanoparticles gene delivery system was prepared by the water-in-oil-in-water(w1/o/w2)double emulsion solvent evaporation(DESE) method.Nanoparticle size measured by dynamic laser light scattering was (225.2±8.1) nm(Mean±SD,n=3),and zeta potential was (-35.5±-3.3) mV.SEM graphs show that the nanoparticles look round,and have smooth surfaces and uniform size distributions.The TFO encapsulation efficiency and drug loading percentage were (25.4±3.1)%(n=3) and (1.34±0.16) μg/mg,respectively.In vitro drug release study with TFO-NP-Apt,a sustained slow release was observed after an initial burst.A10 aptamer modified nanoparticles could penetrate into targeted LNCaP cells more efficiently,then inhibit the proliferation of cells.In this study,the targeted PLGA nanoparticles for gene delivery were prepared successfully.
乳酸乙醇酸共聚物聚乙二醇适配子纳米粒子基因载体
poly(lactic-co-glycolic-acid)polyethyleneglycolaptamernanoparticlegene vector
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