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›› 2006, Vol. 6 ›› Issue (4): 598-602.

• 生化工程专栏 • 上一篇    下一篇

咪喹莫特纳米结构脂质载体的可控制备及表征

周华锋,马全红,丁艺,夏强,郝晓帧,顾宁   

  1. 沈阳化工学院应用化学学院
  • 出版日期:2006-08-20 发布日期:2006-08-20

Controllable Preparation and Characterization of Imiquimod-loaded Nanostructured Lipid Carriers

ZHOU Hua-feng,MA Quan-hong,DING-Yi,XIA Qiang,HAO Xiao-zhen,GU Ning   

  1. Applied Chemistry College Shenyang Institute of Chemical Technology
  • Online:2006-08-20 Published:2006-08-20

摘要: 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.

关键词: 咪喹莫特, 纳米结构脂质载体, 缓释

Abstract: 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.

Key words: imiquimod, nanostructured lipid carriers, sustained release