摘要
目的制备白屈菜红碱固体脂质纳米粒(CHE-SLN),考察其理化性质,并评价其体外释放作用。方法采用乳化蒸发法制备CHE-SLN,单因素分析和正交试验设计优化处方工艺,对最优处方加以明确,并对制得的CHE-SLN进行理化性质考察;借助动态透析法对CHE-SLN与药物溶液的体外释药性能展开考察。采用高效液相色谱法测定白屈菜红碱的含量,之后在累积释药百分率基础上,对各释药模型进行有效拟合处理。并采用MTT法检测CHESLN对肝癌HepG2细胞的毒性。结果CHE-SLN显示白色外观,具均一、滑润表面。可迅速分散为乳白色且可见乳光的胶体溶液,具有良好的再分散特征,经电镜发现,固体脂质纳米粒(SLN)为类球状实体粒子,具良好的分散性,外观较为圆整,粒径分布均匀。平均粒径、包封率、电位依次为(106.3±2.5)nm、(63.84±3.9)%、(-21.4±1.8)mV,其体外释放试验符合一级动力学过程,细胞毒性实验表明白屈菜红碱固体脂质纳米粒对肝癌HepG2细胞有明显的抑制作用。结论成功制备了CHE-SLN,其再分散性、形态与外观皆符合要求;在体外释放行为方面,与一级动力学方程一致。其对肝癌细胞有明显的抑制作用。
Objective To prepare chelerythrine solid lipid nanoparticles(CHE-SLN),determine its physical and chemical properties,and evaluate its in vitro release.Methods Emulsification evaporation method was used to prepare CHE-SLN.Single factor analysis and orthogonal test design were used to optimize the prescription.The physical and chemical properties of CHE-SLN were determined.The in vitro release performance of CHE-SLN and the drug solution were investigated by dynamic dialysis.The content of chelerythrine(CHE)was determined by high performance liquid chromatography.On the basis of cumulative drug release percentage,effective fitting processing was performed on each drug release model.The MTT method was used to detect the toxicity of CHESLN to liver cancer HepG2 cells.Results CHE-SLN was white,with a uniform and smooth surface.When the sample was reconstituted,it was quickly dispersed into a milky white and visible opalescent colloidal solution,showing good redispersion characteristics.Electron microscopy found that solid lipid nanoparticles(SLN)were sphere-like solid particles with good dispersibility.The appearance was round and the particle size distribution was even.The average particle size,encapsulation efficiency,and potential were(106.3±2.5)nm,(63.84±3.9)%,and(-21.4±1.8)mV respectively.The in vitro release conformed to the first-order kinetic process,and the cytotoxicity test showed that the leucorrhea Caesarine solid lipid nanoparticles had a significant inhibitory effect on the liver cancer HepG2 cells.Conclusion The CHE-SLN is successfully prepared,and its redispersibility,morphology and appearance all meet the requirements.Its in vitro release behavior,is consistent with the first-order kinetic equation.Its encapsulation efficiency and stability,facilitate the inhibitory effect on the liver cancer cells.
作者
赵义军
叶晓楠
林春盛
孙健
车明徽
侯立强
ZHAO Yi-jun;YE Xiao-nan;LIN Chun-sheng;SUN Jian;CHE Ming-hui;HOU Li-qiang(The Second Affiliated Hospital of Heilongjiang University of Traditional Chinese Medicine,Harbin 150001)
出处
《中南药学》
CAS
2021年第11期2348-2353,共6页
Central South Pharmacy
关键词
白屈菜红碱
固体脂质纳米粒
正交实验
制备工艺
体外释放
chelerythrine
solid lipid nanoparticle
orthogonal experiment
preparation process
in vitro release
