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目的制备载反义寡核苷酸(ASODNs)聚氰基丙烯酸丁酯阳离子纳米粒。方法以二乙氨乙基-葡聚糖(DEAE-Dextran)为修饰剂,采用乳化聚合法制备阳离子聚氰基丙烯酸丁酯纳米粒,采用吸附法制备载ASODNs纳米粒。用原子力显微镜观察其形态,用激光粒度仪测定Zeta电位及粒径,高效液相法测定药物的载药量和包封率,琼脂糖电泳分析抗核酸酶的能力。结果制得的纳米粒(NP),形态规整、大小均匀,平均粒径为90.2nm,Zeta电位值为+40.1mV,载药量达到84.3μm·mg-1时,几乎所有的药物被负载,DEAE-Dextran-(NP)所吸附的ODNs有较好的对抗核酶降解的能力。结论DEAE-Dextran-NP是一种稳定、高效的反义寡核苷酸传递系统。
Objective To prepare cationic polybutylcyanoacrylate nanoparticles loaded with antisense oligonucleotides (ASODNs). Methods Cationic polybutylcyanoacrylate nanoparticles were prepared by emulsion polymerization using DEAE-Dextran as modifier. ASODNs loaded nanoparticles were prepared by adsorption method. Morphology was observed with atomic force microscopy. Zeta potential and particle size were measured by laser particle size analyzer. Drug loading and entrapment efficiency were determined by HPLC. Agarose electrophoresis was used to analyze the resistance to nuclease. Results The nanoparticles (NPs) with uniform morphology and uniform size with an average particle diameter of 90.2 nm and a Zeta potential of + 40.1 mV and a drug loading of 84.3 μm · mg -1 were loaded on the nanoparticles. ODNs adsorbed by DEAE-Dextran- (NP) have a better ability to resist the degradation of ribozymes. Conclusion DEAE-Dextran-NP is a stable and efficient antisense oligonucleotide delivery system.