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(NanostructuredLipidCarriers,NLC),并用透射电镜(TEM)、粒度分析仪、z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120nm减小到10nm,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20mg/mL(溶解于硅油)提高到56.26mg/mL,并能提高其光稳定性;NLC体系的稳定性良好,z电位高达(-30.90.6)mV,于4℃以10000r/min冷冻离心120min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℃,0.01Pa)后长期保存.
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 mg/mL compared to 20 mg/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 z potential value was (-30.90.6) 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.
出处
《过程工程学报》
EI
CAS
CSCD
北大核心
2005年第1期54-57,共4页
The Chinese Journal of Process Engineering
基金
江苏省计划发展委员会资助项目(编号:7607038009)
国家自然科学基金资助项目(编号:60371027)
