黄芩苷壳寡糖纳米粒的制备及其对MCF-7乳腺癌细胞的抑制作用研究  

Preparation of Baicalin-Chitosan Oligosaccharide-Nanoparticles and Its Inhibitory Effect on MCF-7 Breast Cancer Cells

作　　者：吕凤娇 蔡菊虹 宋婧雯 孙丽丹 谢晓兰 LüFeng-jiao;CAI Ju-hong;SONG Jing-wen;SUN Li-dan;XIE Xiao-lan(College of Chemical Engineering and Materials,Quanzhou Normal University,Quanzhou 362000,China)

机构地区：[1]泉州师范学院化工与材料学院,福建泉州362000

出　　处：《中国药学杂志》2023年第8期708-716,共9页Chinese Pharmaceutical Journal

基　　金：福建省自然科学基金项目资助(2021J01967);泉州市科技计划项目资助(2018Z021);大学生创新训练项目资助(S202110399039)。

摘　　要：目的 制备负载黄芩苷的壳寡糖纳米粒,优化制备工艺,研究其对MCF-7乳腺癌细胞的抑制作用。方法 以黄芩苷为模型药物,采用离子凝胶法制备黄芩苷壳寡糖纳米粒。以包封率为指标,采用单因素考察壳寡糖溶液pH值、黄芩苷加入量、搅拌时间、壳寡糖加入量、三聚磷酸钠加入量等因素的影响,设计L18(35)正交试验进一步优化黄芩苷壳寡糖纳米粒的制备工艺;采用CCK8法对载药壳寡糖纳米粒在体外乳腺癌细胞株MCF-7的细胞抑制作用进行评价。结果 最佳制备工艺条件为:壳寡糖溶液pH值为4.5,黄芩苷加入量为1.4 mg,壳寡糖加入量为140 mg,三聚磷酸钠加入量为4 mg,搅拌时间为10 min。黄芩苷壳寡糖纳米粒包封率(82.87±1.54)%,载药量(6.01±0.24)%,平均粒径(63.2±2.7)nm, Zeta电位(+19.6±0.6)mV。透射电镜下纳米粒呈球形或类球形,形态较为完整,分布均匀。体外细胞抑制实验表明对MCF-7细胞的增殖抑制,黄芩苷壳寡糖纳米粒较黄芩苷高;且随着时间的延长和浓度的增加,两者的抑制率差异越来越显著(P<0.05)。结论 制得的黄芩苷壳寡糖纳米粒粒径较小,对MCF-7乳腺癌细胞具有较好的抑制作用。OBJECTIVE To prepare chitosan oligosaccharide nanoparticles loaded with baicalin,optimize the preparation process,and study the inhibitory effect on MCF-7 breast cancer cells.METHODS Nanoparticles were prepared by the method of ionic cross-linking with baicalin as model drug.Based on results from the single factor tests,orthogonal experimental design method was used to investigate the factors influence on encapsulation rate of nanoparticels.The cytotoxicity of drug-loaded nanoparticles to MCF-7 cells in vitro were also investigated by CCK8 assay.RESULTS The optimum conditions for the preparation of baicalin-chitosan oligosaccharide-nanoparticels were:pH of chitosan oligosaccharide solution was 4,baicalin dosage was 1.4 mg,the dosage of chitosan oligosaccharide was 140 mg,the dosage of sodium tripolyphosphate was 4 mg,and the stirring time was 10 min.The mean diameter was(63.2±2.7)nm,encapsulation rate(82.87±1.54)%and the drug loading(6.01±0.24)%.TEM photos showed that nanoparticles were spherical or quasi-spherical,with relatively complete morphology and uniform distribution.In vitro cell inhibition experiments indicated that baicalin-chitosan oligosaccharide-nanoparticles showed stronger inhibition against MCF-7 cells.With the increase of concentration and time,the inhibitory rate of baicalin-chitosan oligosaccharide-nanoparticles on MCF-7 cells showed significant difference compared with baicalin(P<0.05).CONCLUSION The particle size of baicalin-chitosan oligosaccharide-nanoparticles prepared by this method is small,and it had better inhibitory effect on MCF-7 breast cancer cells.

关 键 词：黄芩苷 壳寡糖 纳米粒 制备 MCF-7细胞 

分 类 号：R944[医药卫生—药剂学] R965[医药卫生—药学]