芹菜素纳米结构脂质载体的制备及其体内抗肿瘤活性研究  

Preparation and in vivo anti-tumor activity of apigenin nanostructured lipid carriers

作　　者：王风云 李伟宏 WANG Feng-yun;LI Wei-hong(Henan Vocational College of Applied Technology,Zhengzhou 450042,China)

机构地区：[1]河南应用技术职业学院,河南郑州450042

出　　处：《中成药》2022年第7期2081-2087,共7页Chinese Traditional Patent Medicine

基　　金：河南省高等学校重点科研计划项目(18A320081)。

摘　　要：目的 制备芹菜素纳米结构脂质载体,并评价其体内抗肿瘤活性。方法 以脂药比、固液脂质比、表面活性剂用量为影响因素,包封率、粒径为评价指标,Box-Behnken响应面法优化制备工艺,测定载药量、Zeta电位、体外释药、介质稳定性,透射电镜下观察形态。建立MDA-MB-231荷瘤裸鼠模型,测定瘤体积、瘤重、抑瘤率。结果 最佳条件为脂药比14.3∶1,固液脂质比3.8∶1,表面活性剂用量1.3%,包封率为82.87%,粒径为164.8 nm。所得纳米结构脂质载体呈球形或椭圆形,平均载药量为5.13%,Zeta电位为-33.5 mV,72 h内累积释放度为79.08%,1.8%NaCl溶液为注射介质。与空白组比较,芹菜素纳米结构脂质载体各剂量组瘤体积增长趋势变缓,并呈剂量依赖性;中、高剂量组瘤重降低(P<0.01),抑瘤率分别为27.78%、37.04%。结论 纳米结构脂质载体可改善芹菜素溶解性,并具有明显的体内抗肿瘤活性。AIM To prepare apigenin nanostructured lipid carriers and to evaluate their in vivo anti-tumor activity.METHODS With lipid-drug ratio,solid-liquid lipid ratio and surfactant consumption as influencing factors,encapsulation efficiency and particle size as evaluation indices,the preparation process was optimized by Box-Behnken response surface method,after which drug loading,Zeta potential,in vitro drug release and medium stability were determined,and the morphology was observed under transmission electron microscope.MDA-MB-231 tumor-bearing nude mouse model was established,then tumor volume,tumor weight and tumor inhibition rate were determined.RESULTS The optimal conditions were determined to be 14.3∶1 for lipid-drug ratio,3.8∶1 for solid-liquid lipid ratio,1.3%for surfactant consumption,the encapsulation efficiency and particle size were 82.87%and 164.8 nm,respectively.The obtained spherical or oval nanostructured lipid carriers demonstrated the average drug loading,Zeta potential and accumulative release rate within 72 h of 5.13%,-33.5 mV and 79.08%,respectively,and 1.8%NaCl solution was selected as injection medium.Compared with the blank group,the various dose groups of apigenin nanostructured lipid carriers displayed alleviated increasing trends of tumor volume in a dose-dependent manner,and the medium-dose and high-dose groups exhibited decreased tumor weight(P<0.01)with the tumor inhibition rates of 27.78%and 37.04%,respectively.CONCLUSION Nanostructured lipid carriers can improve the solubility of apigenin,which have obvious in vivo anti-tumor activity.

关 键 词：芹菜素 纳米结构脂质载体 制备 体内抗肿瘤活性 Box-Behnken响应面法 MDA-MB-231细胞 

分 类 号：R944[医药卫生—药剂学]