两性霉素B立方液晶前体胶囊的制备及释放度考察

目的:制备两性霉素B立方液晶前体胶囊,并考察体外释放度。方法:以单油酸甘油酯为液晶材料、两性霉素B为主药制备了立方液晶前体胶囊;用偏光显微镜及小角衍射表征其吸水后的相态;采用高效液相色谱法测定体外释放度。结果:立方液晶前体胶囊吸水后在偏光显微镜下呈暗背景;小角衍射峰位符合q1∶q2=槡6∶槡8,显示其内部结构为Ia3d(Q230)型立方液晶;立方液晶前体胶囊在含有0.25%十二烷基硫酸钠(SDS)的pH 7.4磷酸盐缓冲液(PBS 7.4溶液)中持续释药达9 h。结论:立方液晶前体胶囊在生理温度下接触水介质后可快速吸水形成立方液晶,并具有一定的缓释作用。

Study on the preparation and in vitro drug release of amphotericin B cubic liquid crystalline precursor capsule

OBJECTIVE To prepare amphotericin B cubic liquid crystalline precursor capsule and investigate its in vitro drug release characteristic.METHODS Cubic liquid crystalline precursor capsule was formulated with glycerol monooleate and amphotericin B;Cross-Polarizing light microscopy(CPLM) and Small Angle X-ray Scattering(SAXS) method were used to study its phase transition after contacting with water;The in vitro drug release behavior was determined by HPLC analysis.RESULTS After water absorption,cubic liquid crystalline precursor capsule showed dark background under CPLM;SAXS intensity peaks corresponded with q1∶q2=6∶8,indicating the structure was Ia3d(Q230) cubic liquid crystalline;The cubic liquid crystalline precursor capsule could slowly release drug in phosphate-buffered saline(PBS pH7.4) containing 0.25% sodium dodecyl sulfate(SDS) within nine hours.CONCLUSION Cubic liquid crystalline precursor capsule can transform to cubic liquid crystalline phase at physiological temperature by means of water uptake and can control the rate of drug release.