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目的采用主动载药法制备三氧化二砷(As2O3)脂质体,并优化处方组成,考察主动载药法制备As2O3脂质体的可行性。方法采用正交设计法筛选处方,主动载药法制备As2O3脂质体;用葡聚糖凝胶G-50柱分离脂质体和游离药物,用原子荧光分光光度法测定包封率;用电镜观察脂质体的外观形态,并用激光粒径分析仪测定脂质体的粒径和Zeta电位;并进一步考察其优势。结果所得脂质体的包封率为(72.3±0.8)%;形态为粒径均匀的球形或类球形,粒径为(193±12)nm,Zeta电位为(36.1±3.0)mV;脂质体具有良好的安全性与较好的稳定性。结论优选得到的As2O3脂质体处方和制备工艺合理,并且所制备的As2O3脂质体具有良好的安全性。
OBJECTIVE: To prepare arsenic trioxide (As2O3) liposomes by active drug loading method and to optimize the composition of the prescription. To investigate the feasibility of preparing As2O3 liposomes by active loading method. Methods Orthogonal design was used to screen prescriptions and active drug loading method was used to prepare liposomal As 2 O 3. Liposomes and free drugs were separated by Sephadex G-50 column. The entrapment efficiency was determined by atomic fluorescence spectrophotometry. The morphology of the liposomes was observed. The particle size and Zeta potential of the liposomes were measured by laser particle size analyzer. The advantages of the liposomes were also investigated. Results The encapsulation efficiency of the obtained liposomes was (72.3 ± 0.8)%. The morphology of the liposomes was spherical or spheroidal with a diameter of (193 ± 12) nm and a zeta potential of (36.1 ± 3.0) mV. Body has good safety and good stability. Conclusion As2O3 liposomes obtained prescription and preparation process is reasonable, and prepared As2O3 liposomes with good safety.