›› 2005, Vol. 5 ›› Issue (1): 54-57.
• 过程与工艺 • Previous Articles Next Articles
ZHANG Xiao-jia,XIA Qiang,MA Quan-hong,DUAN Lei,GU Ning
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张晓佳,夏强,马全红,段磊,顾宁
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)
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)
ZHANG Xiao-jia;XIA Qiang;MA Quan-hong;DUAN Lei;GU Ning. Preparation of Nanostructured Lipid Carriers Loaded with Retinoic Acid by the High Pressure Homogenization Method[J]. , 2005, 5(1): 54-57.
张晓佳;夏强;马全红;段磊;顾宁. 高压均质法制备载有维甲酸的纳米结构脂质载体[J]. , 2005, 5(1): 54-57.
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