摘要
目的:研究不同载药量姜黄素自纳米乳(CUR-SNEDDS)在人工胃肠液中分散相行为与纳米乳稳定性的关系。方法:以CUR过饱和度-时间曲线的变化趋势表示CUR-SNEDDS分散后沉淀生长速度,分别采用紫外-可见光谱法和偏振光显微镜考察载药量对晶体成核与生长的影响,利用X射线粉末衍射(XRD)和差示扫描量热法(DSC)分析不同载药量CURSNEDDS在人工胃肠液中沉淀存在形式,同时考察载药量对CUR-SNEDDS在人工胃肠液中形成的纳米乳稳定性的影响。结果:在人工胃肠液中,随着载药量的提高,CUR过饱和度-时间曲线下面积越大(100%载药量≈90%载药量>75%载药量),结晶成核与生长速度加快(100%载药量>90%载药量>75%载药量),沉淀组成中无定型比例减小,分散后形成的纳米乳滴黏连且分布不均匀、粒径与分散性增大。结论:高载药量促进了晶体成核与生长,增大了沉淀组成中晶型比例,从而导致形成的纳米乳稳定性下降,建议CUR-SNEDDS载药量控制在90%以下。
Objective: To investigate the relationship between phase behavior of curcumin(CUR from self-nanoemulsion drug delivery system(SNEDDS)and stability of the formed nanoemulsion in artificial gastrointestinal fluid. Method: The growth rate of precipitation after dispersion of CUR-SNEDDS was expressed by the change tendency of CUR supersaturation-time curve. The effect of drug loading on crystal nucleation and growth was investigated by ultraviolet-visible spectrometry and polarized light microscope,respectively. X-ray powder diffraction(XRD)and differential scanning calorimetry(DSC)were used to analyze the precipitation forms of CUR-SNEDDS with different drug loading in artificial gastrointestinal fluid. At the same time,the effect of drug loading on the quality stability of nanoemulsion formed by CUR-SNEDDS in artificial gastrointestinal fluid was investigated. Result: In the artificial gastrointestinal fluid,with the increase of drug loading,the area under the supersaturation-time curve of CUR was increased(100% drug loading≈90%drug loading>75% drug loading),the crystallization nucleation and growth rate were accelerated(100% drug loading>90% drug loading>75% drug loading),the amorphous proportion in the precipitation composition decreased,the nanoemulsion droplets adhered and distributed unevenly,the particle size and dispersivity were increased. Conclusion: High drug loading promotes the nucleation and growth of crystals,and increases the proportion of crystal forms in the precipitation composition,which leads to the decrease in the stability of the formed nanoemulsion. Therefore,it is suggested that the drug loading of CUR-SNEDDS needs to be controlled below 90%.
作者
陈绪龙
梁新丽
刘欢
赵国巍
温佳豪
欧阳料淇
蒋且英
廖正根
CHEN Xu-long;LIANG Xin-li;LIU Huan;ZHAO Guo-wei;WEN Jia-hao;OUYANG Liao-qi;JIANG Qie-ying;LIAO Zheng-gen(Key Laboratory of Modern Preparation of Traditional Chinese Medicine(TCM),Ministry of Education,Experimental Animal Science and Technology Center,Jiangxi University of TCM,Nanchang 330004,China)
出处
《中国实验方剂学杂志》
CAS
CSCD
北大核心
2021年第1期154-161,共8页
Chinese Journal of Experimental Traditional Medical Formulae
基金
江西省一流学科建设项目(JXSYLXK-ZHYAO059)
江西省卫生计生委科技计划项目(20181140)
江西省卫生计生委中医药科研课题(2016A021)。
关键词
姜黄素
自纳米乳
载药量
人工胃肠液
相行为
过饱和度
结晶
curcumin
self-nanoemulsion
drug loading
artificial gastrointestinal fluid
phase behavior
supersaturation
crystal
