用色谱法测定脂质纳米结构中的碘乙酸酯

D. Korshunov, I. A. Kondakova, E. Sidenko, E. Sereda, N. Y. Zolotukhina
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引用次数: 0

摘要

抗癌药物的脂质体形式通常用于改善药物的药代动力学,降低药物的全身毒性。本研究的目的是开发一种方法,用于定量分析具有明显抗肿瘤活性的糖酵解抑制剂碘乙酸钠(IA)的脂质体形式。脂质体是在氩气压力为 2 至 10 兆帕斯卡、温度为 25 至 55 摄氏度的条件下挤压制备的。获得的脂质体通过透析从非结合成分中纯化出来。采用高效液相色谱法分析脂质体中的抑制剂溶液。亲水相互作用色谱法显示,以氨基丙基硅胶为固定相,碘乙酸酯的选择性很高。分析的最佳选择是使用分光光度检测器。分析结果表明,无论脂质体大小如何,1 毫升脂质体中的抑制剂剂量为 0.20 - 0.23 毫克。按动物体重计算,碘乙酸盐的用量为 8 - 9 毫克/千克。用所开发的方法对脂质体进行的分析表明,在低温(不超过 40°C)和透析时间约为 3 小时的情况下,脂质体的产量和纯度最高。
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Chromatographic determination of iodoacetate in lipid nanostructures
A liposomal form of anticancer drugs is often used to improve pharmacokinetics and reduce systemic toxicity of the drugs. The goal of the study is to develop a method for quantitative analysis of a liposomal form of sodium iodoacetate (IA), glycolysis inhibitor, which exhibits a pronounced antitumor activity. Liposomes were prepared by extrusion at a temperature of 25 – 55°C under argon pressure ranged from 2 to 10 MPa. The obtained liposomes were purified from the non-incorporated component using dialysis. The method of HPLC was used to analyze the inhibitor solution in liposomes. The method of hydrophilic interaction chromatography revealed a high selectivity of iodoacetate with aminopropyl silica gel as a stationary phase. The best option for analysis was to use a spectrophotometric detector. The results of analysis showed that the dose of the inhibitor in 1 ml of liposomes was 0.20 – 0.23 mg regardless of the liposome size. In terms of the weight of an animal, the amount of iodoacetate was 8 – 9 mg/kg. The analysis of liposomes by the developed method showed that the highest yield and a high degree of purification is attained at low temperature (no more than 40°C) and duration of dialysis for about 3 h. For these purposes, the use of liposomes with a diameter of 400 nm turned out to be the best option.
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