主动载药法制备三氧化二砷脂质体

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。

Preparation of arsenic trioxide liposome by active drug-loading method

Objective To prepare arsenic trioxide (As₂O₃) liposome, to optimize the formulation of As₂O₃ liposomes, and to study the feasibility of As₂O₃ liposomes prepared by the active drug-loading. Methods Liposomes were prepared by the active drug-loading method. An orthogonal test was utilized to optimize the formulation and preparation of As₂O₃ liposomes. The unencapsulated As₂O₃ and liposomes were separated by Sephadex gel G-50 column, the entrapment efficiency (EE) was detected by atomic fluorescence spectrophotometry. The morphological examination of As₂O₃ liposomes was performed using transmission electron microscopy. The particle size and Zeta potential of the liposomes were measured. The advantage of As₂O₃ liposomes made by active drug-loading method was investigated. Results The EE of the liposomes was (72.3 ± 0.8)%, the morphology of liposomes was spherical or ellipsoidal shape with uniform particle size, the mean partical size was (193 ± 12) nm, and Zeta potential was (36.1 ± 3.0) mV. Liposomes have good safety and better stability. Conclusion The selected formulation and preparation technique of As₂O₃ liposomes could be rational and stable, and the prepared As₂O₃ liposomes have good safety.