咪喹莫特纳米结构脂质载体的可控制备及表征

采用高压均质法制备咪喹莫特纳米结构脂质载体(IMQD-NLC)，分别考察表面活性剂、高压均质操作参数及药物加入量对IMQD-NLC制备的影响，并对其形貌、物相、表面Zeta电位及体外释放特性等进行了表征. 结果表明，选取S-40和Span-20复配作为表面活性剂，随着S-40含量的增大，IMQD-NLC的平均粒径和Zeta电位的绝对值逐渐减小，而PI值呈现增大趋势；高的高压均质循环次数制备的IMQD-NLC平均粒径和PI值均比较低；药量增大，粒子平均粒径和PI值增大，而Zeta电位并没有发生明显变化；平均包封率为88.3%；IMQD-NLC呈无定型状态；IMQD-NLC在pH 1的释放介质中呈现先突释后缓释，而在pH 5.5的释放介质中呈现缓慢释放.

Controllable Preparation and Characterization of Imiquimod-loaded Nanostructured Lipid Carriers

Imiquimod-loaded nanostuctured lipid carriers(IMQD-NLC)were prepared by high pressure homogenization method.The influences of surfactant,high pressure homogenization parameter and capacity loading on the preparation of IMQD-NLC were explored.Additionally,its morphology,crystalline phase,Zeta potential and release in vitro were characterized.The results show that there was a trend toward increasing the particle size of IMQD-NLC and decreasing the absolute value of Zeta potential with increasing the content of S-40 in the combined surfactant of S-40 and Span-20.Both the particle size and PI value were lower with the many cycle times,while ascending with increasing the content loading.IMQD-NLC,characterized by XRD,was amorphous.It was confirmed that burst release occurred followed by a sustaining release at pH 1 and a sustaining release at pH 5.5 in vitro for IMQD-NLC.Consequently the preparation of IMQD?NLC can be controlled by altering the conditions of preparation to realize sustained release effect.