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目的制备重酒石酸长春瑞滨(vinorelbine tartrate,VRT)热敏脂质体,建立脂质体中VRT含量和包封率的测定方法。方法 pH梯度法制备VRT热敏脂质体,HPLC测定脂质体中VRT的含量。微柱离心法分离脂质体与游离药,考察葡聚糖凝胶类型、洗脱溶剂、柱高、洗脱体积等因素对VRT游离药洗脱的影响。结果 VRT热敏脂质体的平均粒径为(94.6±1.6)nm,含量为(1.83±0.03)mg.mL-1。选择葡聚糖凝胶G-25制备微柱,最佳柱高4 cm,以PBS缓冲液为洗脱溶剂,梯度洗脱体积法分离脂质体与游离药,测得3批VRT热敏脂质体的包封率分别为(95.75±1.42)%、(91.12±1.21)%、(94.10±2.03)%,洗脱回收率分别为(98.3±2.42)%、(93.5±1.83)%、(96.6±1.65)%。结论 VRT脂质体的制备工艺稳定,载药量大,包封率高。含量及其包封率测定方法简单、快速、准确。本实验可为VRT静脉注射用热敏脂质体新制剂的开发提供研究基础。
OBJECTIVE: To prepare vinorelbine tartrate (VRT) thermosensitive liposomes and establish the method for determination of VRT content and entrapment efficiency in liposomes. Methods VRT thermosensitive liposomes were prepared by pH gradient method. The content of VRT in liposomes was determined by HPLC. The separation of liposomes and free drugs by microcolumn centrifugation was carried out to investigate the effects of dextran gel type, elution solvent, column height and elution volume on the elution of VRT free drug. Results The average size of VRT thermosensitive liposomes was (94.6 ± 1.6) nm, and the content was (1.83 ± 0.03) mg.mL-1. Sephadex G-25 was used to prepare microcolumn, the optimal column height was 4 cm, PBS buffer was used as the elution solvent, and the volume was used to separate the liposomes from the free drug. Three batches of VRT thermosensitive lipids The entrapment efficiencies of plastids were (95.75 ± 1.42)%, (91.12 ± 1.21)% and (94.10 ± 2.03)%, respectively. The recovery rates of the plastids were 98.3 ± 2.42% and 93.5 ± 1.83% 96.6 ± 1.65)%. Conclusion The preparation of VRT liposomes is stable, with high drug loading and high entrapment efficiency. Determination of content and encapsulation efficiency is simple, fast and accurate. This experiment can provide a research basis for the development of new formulations of thermal liposomes for intravenous injection of VRT.