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›› 2005, Vol. 5 ›› Issue (1): 54-57.

• 过程与工艺 • 上一篇    下一篇

高压均质法制备载有维甲酸的纳米结构脂质载体

张晓佳,夏强,马全红,段磊,顾宁   

  1. 东南大学分子与生物电子学教育部重点实验室纳米科学与技术研究中心
  • 出版日期:2005-01-20 发布日期:2005-01-20

Preparation of Nanostructured Lipid Carriers Loaded with Retinoic Acid by the High Pressure Homogenization Method

ZHANG Xiao-jia,XIA Qiang,MA Quan-hong,DUAN Lei,GU Ning   

  1. Key Lab. Mol. Biomol. Electr., Ministry of Education, Res. Cent. Nano-scale Sci. & Technol., Southeast Univ.
  • Online:2005-01-20 Published:2005-01-20

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摘要： 采用高压均质法制备了载有维甲酸(RA)的纳米结构脂质载体(Nanostructured Lipid Carriers, NLC)，并用透射电镜(TEM)、粒度分析仪、 电位仪和高效液相色谱仪(HPLC)对其进行了表征. 结果表明，随高压均质循环次数的增加，NLC的均粒径从120 nm减小到10 nm，同时单分散性变差；NLC的微观形貌呈球形，表明其未结晶具有较好的载药能力；NLC将维甲酸浓度从20 g/mL(溶解于硅油)提高到56.26 g/mL，并能提高其光稳定性；NLC体系的稳定性良好， 电位高达( 30.9 0.6) mV，于4℃以10000 r/min冷冻离心120 min或避光保存6个月后粒径分布仍然基本不变，且可冷冻干燥( 40℃, 0.01 Pa)后长期保存.

关键词: 纳米结构脂质载体（NLC）, 高压均质, 维甲酸(RA)

Abstract: The poor aqueous solubility and instability of retinoic acid (RA) have limited its clinical use. Solid lipid nanoparticles (SLN) have a potential limitation which is the drug expulsion. This study was undertaken to overcome the limitation by loading RA in nanostructured lipid carriers (NLC). RA-loaded NLC was prepared by high pressure homogenization and characterized by transmission electronic microscope (TEM), particle size analyzer, zeta potential analyzer and high-performance liquid chromatography (HPLC). The results were as follows: (1) When the homogenization cycle number varied from 1 to 12, the mean particle size decreased from 120 nm to 10 nm, while P.I. (polydispersity index) increased from 0.26 to 0.69. (2) The spherical shape observed by TEM indicated a better drug loading capacity over SLN. (3) The concentration of all-trans retinoic acid (ATRA) in NLC reached 56.26 g/mL compared to 20 g/mL dissolved in silicone oil and the photostability of ATRA was improved so that the effective concentration of RA could keep for a longer time. (4) As far as the stability of NLC was concerned, its potential value was ( 30.9 0.6) mV and it remained stable after 120 min centrifugation (4℃, 10000 r/min) or 6 month light-proof storage. Furthermore, freezing-drying ( 40℃, 0.01 Pa), which increased its mean particle size and reduced its P.I., could also be used to increase the NLC stability. Taken together, RA-loaded NLC is a promising drug form for clinical use.

Key words: nanostructured lipid carriers (NLC), high pressure homogenization, retinoic acid (RA)