摘要
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。
AIM To prepare the pazufloxacin ultradeformable liposomes and study their properties. METHODS The reverse phase evaporation method was used to prepare the uhradeformable liposomes. The HPLC method was employed to determine the content of pazufloxacin in liposomes： the applied column was Waters Atlantis C18 （4.6 mm× 150 mm, 5 μm） at room temperature and the mobile phase consisted of acetonitrile- 0.02 mol ·L^-1 sodium dihydrogen phosphate solution （containing 0.05 mol·L^-1 Tetra-n-butylammonium bromide, pH 3.43 adjusted with phosphric acid） （10.2 ： 89.8, V/V） pumped at a flow rate of 1 mL ·min^-1. The drug entrapment efficiency and drug loading were calculated according to the measured results. Ultradeformable liposomes shape was observed in transmission electron microscopy （TEM）, and its particle size and zeta potential were measured with laser scattering method. The deformation properties of the ultradeformable liposomes were also investigated. RESULTS The pazufloxaein ultradeformable liposomes prepared were in the form of the multilamelar lipid vesicles with （71.45 ± 6.31） nm of particle size, （54.88 ± 3.76） mV of Zeta potential and （26.58 ± 5.24） % of entrapment efficiency, and the average drug loading （concentration） was 2.11 mg·mL^-1. The research confirmed that pazufloxacin ultradeformable liposome has high degree of deformation. CONCLUSION The preparation method of pazufloxacin uhradeformable liposomes is feasible, and the content determination method is simple and reliable with high stability and deformation. It may be an effective transdemal delivery carrier.
出处
《中国新药与临床杂志》
CAS
CSCD
北大核心
2016年第6期437-440,共4页
Chinese Journal of New Drugs and Clinical Remedies
关键词
帕珠沙星
脂质体
色谱法
高压液相
pazufloxacin
liposomes
chromatography, high pressure liquid
