姜黄素纳米胶束的制备及体外抗肿瘤作用研究  

Preparation of curcumin nano-micelles and the antitumor effect in vitro

作　　者：孙吴倩 郭秋红 贾玉倩 刘兴超 李少鹏 左赛杰 周莉 SUN Wuqian;GUO Qiuhong;JIA Yuqian;LIU Xingchao;LI Shaopeng;ZUO Saijie;ZHOU Li(College of Pharmacy,Hebei University of Traditional Chinese Medicine,Shjiazhuang,Hebei,050091 P.R.China;Hebei Technology Innovation Center of TCM Formula Preparations,Hebei Higher Education Institute Applied Technology Research Center on TCM Development and Industrialization,Shjiazhuang,Hebei,050091 P.R.China)

机构地区：[1]河北中医学院药学院,河北石家庄050091 [2]河北省中药组方制剂技术创新中心、河北省高校中药开发与产业化应用技术研发中心,河北石家庄050091

出　　处：《华西药学杂志》2023年第1期7-11,共5页West China Journal of Pharmaceutical Sciences

基　　金：河北省自然科学基金项目(H2020423006);河北省高等学校青年拔尖人才计划项目(BJK2022034);河北中医学院博士科研基金项目(BSZ2019004);河北中医学院优秀青年教师基础研究计划项目(YQ2019010)。

摘　　要：目的 制备姜黄素(Cur)/甲氧基聚乙二醇-聚己内酯(MP)载药纳米胶束,并研究其体外抗肿瘤作用。方法 采用薄膜分散法制备Cur/MP纳米胶束,筛选不同药材质量比优化处方,在扫描电镜下观察载药纳米胶束的形态;采用CCK-8法考察Cur、Cur/MP胶束对人非小细胞肺癌A549细胞的抑制率;以香豆素6为荧光探针考察细胞对胶束的摄取行为。结果 按最优处方制备3批胶束的平均粒径为35.71±0.2 nm,平均电位为-16.8±0.2 mV,平均包封率为97.52%±1.00%,平均载药量5.25%±0.80%;Cur/MP胶束在72 h内释放度最大可达74.16%,释放缓慢,无突释现象,遵循一级动力学方程;与Cur溶液比较,Cur/MP纳米胶束对A549细胞的抑制作用增强;荧光显微镜下可观察到,随着时间的延长,细胞对药物的摄取增加。结论 Cur/MP胶束制备工艺简单,可增强药物对A549细胞的抑制作用;聚合物纳米胶束的pH敏感性有利于其在体内肿瘤组织中的蓄积及肿瘤细胞内的摄取。OBJECTIVE To prepare curcumin(Cur)/methoxy polyethylene glycol-polycaprolactone(MP) nanoparticles and to study the antitumor effects in vitro.METHODS Cur/MP nano-micelles were prepared by thin film dispersion method.Different medicinal materials were screened to optimize the prescription.The morphology of drug-loaded nano-micelles was observed under scanning electron microscope.The inhibition rate of Cur and Cur/MP micelles on human non-small cell lung cancer A549 cells was investigated by CCK8 method.Coumarin 6 was used as a fluorescent probe to investigate the uptake behavior of micelles.RESULTS The average size of the micelles prepared was 35.71±0.2 nm;the average potential was-16.8±0.2 mV;the average encapsulation efficiency was 97.52%±1.0%;and the average drug loading was 5.25%±0.8%.The Cur/MP micelles reached the maximum release of 74.16% within 72 h, the release was slow, and there was no burst release phenomenon, following the first order Kinetic equation.Cur/MP nano-micelles had enhanced inhibitory effect on A549 cells compared with Cur solution.The uptake behavior of A549 cells to nano-micelles was observed under the fluorescence microscope.The results showed that drug uptake increased with time.CONCLUSION The Cur/MP micelles can be prepared in a simple way, which can enhance the inhibitory effect of drugs on A549 cells.The pH sensitivity of the polymer nano-micelles is conducive to its accumulation in tumor tissues and uptake in tumor cells.

关 键 词：姜黄素 甲氧基聚乙二醇-聚己内酯 纳米胶束 薄膜分散法 体外释放 A549细胞 细胞毒性 细胞摄取 

分 类 号：R94[医药卫生—药剂学]