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目的制备帕珠沙星柔性脂质体,并进行其相关性质研究。方法利用逆相蒸发制备帕珠沙星柔性脂质体。采用高效液相色谱法测定脂质体中帕珠沙星的含量,色谱条件为固定相:Waters Atlantis C18色谱柱(4.6 mm×150 mm,5μm);流动相:乙腈︰0.02 mol·L~(-1)磷酸二氢钠水溶液(含四丁基溴化铵0.05 mol·L~(-1),用磷酸调节pH值至3.43)的体积分数为10.2︰89.8;柱温:室温;流速:1 mL·min~(-1),并根据测定结果计算脂质体的药物包封率和载药量。通过透射电镜观察脂质体的形态,采用激光散射法测定其粒径和表面电位;并考察柔性脂质体的变形性。结果所制备的帕珠沙星柔性脂质体为多室脂质体;其平均粒径为(71.45±6.31)nm,Zeta-电位为(54.88±3.76)mV;平均包封率为(26.58±5.24)%,平均载药量(含量)为2.11 mg·mL~(-1);研究证实了帕珠沙星柔性脂质体具有高度的变形性。结论帕珠沙星柔性脂质体的制备方法可行,含量测定方法简单、可靠,稳定性和变形性高,可能成为透皮转运的有效载体。
Objective To prepare pazufloxacin flexible liposomes and study their related properties. Methods Pazufloxacin flexible liposomes were prepared by reverse phase evaporation. The content of pazufloxacin in liposomes was determined by HPLC. The chromatographic conditions were as follows: Waters Atlantis C18 column (4.6 mm × 150 mm, 5 μm); mobile phase: acetonitrile: 0.02 mol·L ~ (-1) -1) sodium dihydrogen phosphate aqueous solution (containing 0.05 mol·L -1 tetrabutylammonium bromide, pH adjusted to 3.43 with phosphoric acid) was 10.2: 89.8; column temperature: room temperature; flow rate: 1 mL · min ~ (-1), and the drug encapsulation efficiency and drug loading of the liposomes were calculated according to the measurement results. The morphology of the liposomes was observed by transmission electron microscopy. The particle size and surface potential were measured by laser light scattering. The deformability of the liposomes was also investigated. Results The flexible liposomes of pazufloxacin were multilocular liposomes with an average diameter of (71.45 ± 6.31) nm and a Zeta-potential of (54.88 ± 3.76) mV. The average encapsulation efficiency was (26.58 ± 5.24)%, and the average drug loading (content) was 2.11 mg · mL -1. The study confirmed that pazufloxacin flexible liposomes have a high degree of deformability. Conclusion The preparation method of pazufloxacin flexible liposomes is feasible, the assay method is simple, reliable, stable and deformable, which may become an effective carrier of transdermal delivery.