摘要
背景:异甘草素是一种异黄酮化合物,有着很强的药理活性如抗癌、抗病毒、抗糖尿病等,但水溶性差,这极大地限制了其临床应用。目的:制备异甘草素壳聚糖纳米粒,探讨其在体外对人肺癌细胞A549生长的抑制作用。方法:以壳聚糖为载体材料,异甘草素为模型药物,三聚磷酸钠为离子交联剂,利用离子交联法制备异甘草素壳聚糖纳米粒,测定其粒径、分散度和Zeta电位,通过透射电镜观察纳米粒形态,通过离心测定其包封率和载药量。将异甘草素与甘草素壳聚糖纳米粒分别置于透析袋内,以PBS为释放介质,动态观察其体外释放。分别以含不同质量浓度(1,5,25 mg/L)异甘草素、甘草素壳聚糖纳米粒及壳聚糖纳米粒的培养液培养人肺癌细胞A549,培养48 h后,采用MTT法检测细胞增殖,计算细胞生长抑制率。结果与结论:(1)异甘草素壳聚糖纳米粒为球形或类球形,结构完整,大小较为均一,纳米粒平均粒径为(159±20)nm,Zeta电位为+17.2m V,分散度为0.243,包封率和载药量分别为(85.28±1.31)%和(13.28±0.53)%;(2)游离异甘草素在8 h内释放完毕;异甘草素壳聚糖纳米粒具有缓慢释放特性,72 h累积释放量达83.98%,体外释药过程符合一级动力学方程;(3)不同质量浓度的壳聚糖纳米粒对A549细胞生长无抑制作用;异甘草素、异甘草素壳聚糖纳米粒均呈浓度依赖性抑制A549细胞的生长,并且相同质量浓度下,异甘草素壳聚糖纳米粒对A549细胞生长的抑制作用强于异甘草素(P <0.05);(4)结果表明采用离子交联法制备的异甘草素壳聚糖纳米粒,具有良好的缓释性能,提高了异甘草素在体外对A549细胞增殖的抑制作用。
BACKGROUND: Isoliquiritigenin, one kind of isoflavone compounds, has a wide range of biological activities, such as anti-cancer, anti-virus,and anti-diabetes, but its clinical application is limited by its poor water solubility.OBJECTIVE: To prepare chitosan/isoliquiritigenin nanoparticles and investigate their inhibitory effects on human lung cancer cell line A549 in vitro.METHODS: The chitosan/isoliquiritigenin nanoparticles were prepared by ionic gelation method with chitosan as the carrier material,isoliquiritigenin as the model drug, and sodium tripolyphosphate as the ionic crosslinking agent. The nanoparticle size, dispersion, and Zeta potential were investigated by malvern laser particle size analyzer. The morphology of the nanoparticles was observed by transmission electron microscopy. The encapsulation efficiency and cumulative release rate of the nanoparticles were measured by centrifugation.Isoliquiritigenin and chitosan/isoliquiritigenin nanoparticles were placed in dialysis bags and their dynamic release was determined in PBS buffer. Human lung cancer cell line A549 was cultured in different concentrations(1, 5, 25 mg/L) of isoliquiritigenin, chitosan/isoliquiritigenin nanoparticles, and chitosan nanoparticles. MTT assay was used to investigate the inhibitory effects of chitosan/isoliquiritigenin nanoparticles on human lung cancer cell A549 in vitro after 48 hours of culture. The growth-inhibitory rate was calculated.RESULTS AND CONCLUSION: The chitosan/isoliquiritigenin nanoparticles were spherical or quasi spherical in shape with complete structure and of relatively uniform size. The average particle size, dispersion and Zeta potential of chitosan/isoliquiritigenin nanoparticles were(159±20) nm, 0.243 and +17.2 mV, respectively. The encapsulation efficiency and cumulative release rate of the nanoparticles were(85.28±1.31)% and(13.28±0.53)% respectively.The release of free isoliquiritigenin was completed within 8 hours, while the chitosan/isoliquiritigenin nanoparticles had sustained release prop
作者
吕文娟
刘福定
王桃姣
万浪
陈芳
Lü Wenjuan;Liu Fuding;Wang Taojiao;Wan Lang;Chen Fang(Department of Cardiology, Renmin Hospital of Wuhan University, Wuhan 430060, Hubei Province,China;Hospital Infection Office,Huangshi Central Hospital, Edong Healthcare, Huangshi 435000,Hubei Province,China;Department of Otolaryngology, Huangshi Central Hospital, Edong Healthcare, Huangshi 435000, Hubei Province,China)
出处
《中国组织工程研究》
CAS
北大核心
2019年第26期4200-4205,共6页
Chinese Journal of Tissue Engineering Research
基金
湖北省卫计委科研项目(WJ2017M253),项目负责人:陈芳~~
